payload_ID payload_name efficacy_type efficacy_Symbols IC50_value_d Administration_Times Administration_Dosage payload_model pdc_cell_disease pdc_cell_name Efficacy_Description REF_ID DRG00012 Paclitaxel Percent survival = 0% 20 days 17.3 mg/kg MDA-MB-231BR mouse model. Breast adenocarcinoma MDA-MB-231 cell "As shown in Figure 7D, PTX did not increase survival, while the PDC M1-RGD-PTX markedly increased survival. " REF00077 DRG00012 Paclitaxel Percent survival = 0% 25 days 17.3 mg/kg U87MG-Luc-bearing xenograft model. Glioblastoma U87MG-Luc cell "The survival of the PTX group was markedly lower than that of the Vehicle group. M1-PTX did not improve survival, whereas the survival of the M1-RGD-PTX group was increased." REF00077 DRG00020 Docetaxel Tumor Growth Inhibition value (TGI) = 0% 20 days 3.75 mg/kg Nude mice hTNBCSC cells xenograft tumor model. Triple-negative breast cancer Human triple-negative breast cancer stem cell (hTNBCSC) "In vivo assessment in tumor-bearing animal models classically complements cell cultures data for comparing cancer treatment efficacies. For this reason, hTNBCSC and hOvCSC xenografts were implanted subcutaneously into immunodeficient mice as described in the Methods section with only 1000 cells given their highly tumorigenic nature. Three days later, the animals began receiving weekly IV bolus administration of either vehicle, docetaxel, or TH1902. Docetaxel was administered at a dose (15 mg/kg/week; for 3 cycles) in accordance with the estimated maximal tolerated dose (MTD) for mice, as well as at of the MTD (3.75 mg/kg/week). TH1902 was administered at doses (35 and 8.75 mg/kg/week) which contained quantities of docetaxel equivalent to those in the two administrations of free docetaxel. From the size of the hTNBCSC and hOvCSC tumors, it is apparent that docetaxel had little impact on xenografts growth when administered neither at its MTD, for both hTNBCSC and hOvCSC, nor at of this dosage as reflected by the growth curves. TH1902, when administered at a dosage equivalent to docetaxel at its MTD, provided greater tumor growth inhibition than did docetaxel for both xenograft models. Furthermore, higher dosage of administered TH1902 (up to 1.5 equivalent of docetaxel MTD) did not generate significant differences in terms of hOvCSC tumor inhibition without affecting mice body weights suggesting that TH1902, even at higher doses, is better tolerated compared to docetaxel. Then, in order to statistically compare the effects of docetaxel and TH1902 on tumor growth, the tumor sizes measured at the vehicle group endpoint were compared and statistically significant differences between the tumor sizes in vehicle-treated animals found in TH1902-treated animals for hTNBCSC and hOvCSC. Mouse body weight was used as an indicator of the morbidity associated with administration of docetaxel or TH1902. Administration of docetaxel at its MTD provoked a weight loss that approached 10% after the treatments, which is often observed in xenograft models with administration of docetaxel at this level. The body weights of animals treated with an equivalent quantity or a 1.5-fold equivalent of TH1902 were maintained at a roughly constant level throughout the experiment. The animals treated with vehicle recorded a slight weight gain (~5%) over this period while animals treated with the lower dosages of docetaxel or TH1902 were similar to the animals treated with vehicle. The body weight data indicates that TH1902 appears to be better tolerated than the equivalent quantity of free docetaxel, in addition to the fact that TH1902 is more efficacious than docetaxel when administered in vivo in the murine models of CSC tested." REF00234 DRG00023 Tesaglitazar HbA1C change = 0.55% Every day 2.5 μM db/db mice model. . . "Whereas in the vehicle/untreated mice, the HbA1C values increased by approximately 2%, a graduated reduced increase was seen for [F7, P34]-NPY (2), peptide conjugate (3), and tesa (Figure 8A). Body temperature, which decreased to 35 C in the vehicle/untreated db/db controls, was normalized to 36 C in all of the treated mice including the mice treated with [F7, P34]-NPY (2) (Figure 8B). Treatment with tesa and tesa-NPY (3) led to normalization of the plasma concentration of ketone bodies and adiponectin, whereas [F7, P34]-NPY (2) and vehicle/untreated showed no effect (Figure 8C/E). Treatment had no major influence on the insulin and Mcp-1 levels (Figure 8D/G). The serum leptin concentration was reduced in the mice treated with tesa, whereas no reduction was detectable in all of the other treated mice (Figure 8F)." REF00088 DRG00011 Doxorubicin Cell viability > 1% 48 h 1.87 μM . Ovarian serous cystadenocarcinoma SK-OV-3 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00011 Doxorubicin Cell viability = 1% 48 h 15 μM . Breast adenocarcinoma MDA-MB-231 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00011 Doxorubicin Cell viability > 1% 48 h 15 μM . Ovarian serous cystadenocarcinoma SK-OV-3 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00011 Doxorubicin Cell viability > 1% 48 h 3.75 μM . Ovarian serous cystadenocarcinoma SK-OV-3 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00011 Doxorubicin Cell viability > 1% 48 h 7.5 μM . Ovarian serous cystadenocarcinoma SK-OV-3 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00011 Doxorubicin Cell viability = 2% 48 h 7.5 μM . Breast adenocarcinoma MDA-MB-231 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00023 Tesaglitazar Body weigth change = 3% Every day; over 8 days 2.5 μM db/db mice model. . . "The mice treated with tesa and tesa-NPY (3) did not change significantly, whereas their littermates treated with [F7, P34]-NPY (2) or vehicle/untreated lost approximately 3% of their body weight (Figure 7A)." REF00088 DRG00011 Doxorubicin Cell viability = 3% 48 h 3.75 μM . Breast adenocarcinoma MDA-MB-231 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00011 Doxorubicin Cell viability = 6% 48 h 0.94 μM . Ovarian serous cystadenocarcinoma SK-OV-3 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00011 Doxorubicin Cell viability = 9% 48 h 1.87 μM . Breast adenocarcinoma MDA-MB-231 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00011 Doxorubicin Cell survival rate = 20% 24 h 20 μg/mL . Invasive breast carcinoma MCF-7 cell "Subsequently, the cell toxicity of the DOX, DOX-SH, and PNS-SS-DOX was also investigated using the CCK-8 method. As shown in Figure8b, all three materials display significant concentration-dependent cytotoxicity. Additionally, it can be observed that at the same concentration, the cytotoxicity of DOX-SH to MCF-7 cells was nearly identical to that of DOX, indicating that thiolation did not affect the efficacy of DOX. Furthermore, the PNS-SS-DOX group exhibited stronger cytotoxicity to MCF-7 cells. Particularly, at a material concentration of 20µgmL1, the cell survival rate for the PNS-SS-DOX group was only 12%, while that of the DOX-SH group was 20%. We suggest that this effect is possibly due to the modification of PNSs with DOX-SH. On one hand, the hydrophilic peptides effectively improved the solubility of the hydrophobic drug DOX-SH, and on the other hand, the positively charged PNSs enhanced the drug uptake by cancer cells, thus increasing the cancer cell killing efficacy." REF00302 DRG00011 Doxorubicin Cell viability = 21% 48 h 0.94 μM . Breast adenocarcinoma MDA-MB-231 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00014 Baicalin Fe2+ decrease ratio = 25% 24 h . . Normal H9c2 cell "The accumulation of iron is a characteristic feature of ferroptosis. Intracellular iron, especially labile ferrous iron, can react with oxidants to generate cytotoxic hydroxyl radicals via Fenton reactions, thereby promoting ferroptosis. FerroOrange staining revealed significantly increased intracellular Fe2+ levels in DOX-treated H9c2 cells compared to controls, indicating DOX induced iron dyshomeostasis, resulting in ferrous iron buildup and subsequent ferroptosis. BA-NFs alleviated the accumulation of intracellular ferrous ions, suppressing ferroptosis. Fe2+ accumulation may disrupt the balance between LPO and oxygen homeostasis. We observed that BA-NFs efficiently attenuated DOX-induced elevation in malondialdehyde (MDA), a lipid peroxidation end-product, while increased antioxidant glutathione (GSH) levels. These findings suggested that BA-NFs can prevent DOX-induced ferroptosis in cardiomyocytes. Furthermore, protein expression of SLC7A11 and GPX4, key components of the antioxidant defense system against ferroptosis, was examined. DOX significantly decreased SLC7A11 and GPX4 expression in H9c2 cells compared to controls, suggesting DOX disrupts cellular antioxidant systems leading to ferroptosis. BA and BA-NFs partially restored SLC7A11 and GPX4 expression versus DOX treatment, with BA-NFs exhibiting the most significant impact. Together, these results indicate BA-NFs specifically inhibits DOX-induced cardiomyocyte ferroptosis by reducing intracellular iron accumulation and enhancing antioxidant system gene expression. In addition, the cardiotoxic effects of DOX are mediated via excessive oxidative stress and induced mitochondrial damage, thereby activating intrinsic apoptosis as an additional pathway. Flow cytometric analysis using Annexin V-Fitc/PI staining revealed that BA-NFs potently attenuated DOX-induced cardiomyocyte apoptosis, with a more pronounced effect than BA alone. DOX enhanced the green fluorescent signal of cleaved caspase-3 (as a biomarker of apoptosis) in H9c2 cells, whereas BA-NFs significantly inhibited this upregulation. These results provided further evidence that BA-NFs serve as potential therapeutic approaches for DIC." REF00290 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 25% . . . Colon cancer HT29 cell . REF102391 DRG00031 Mertansine DM1 Tumor Growth Inhibition value (TGI) = 27.10% . . B16-F10 tumor-bearing mouse model. Mouse melanoma B16-F10 cell "To examine the therapeutic effects of M-DM1 in mice, we used the B16F10 tumor-bearing mouse model. We subcutaneously injected cancer cells into C57BL/6 mice and treated them with 20 nmol/kg M, DM1, or M-DM1 via intraperitoneal injections every 3 days. While slight growth inhibition was observed with M and DM1, M-DM1 was found to significantly suppress tumor growth. None of the mice showed any weight loss until the end of the study period, suggesting that there were no significant toxicities due to the drug treatments. At 21 days after tumor cell inoculation, the mice were sacrificed, and tumor volumes and weights were measured. A marked decrease in the tumor volumes and weights was observed in the M-DM1-treated mice group compared to that in the other groups. In addition, we determined the survival rate of B16-bearing mice following treatment with each peptide. The median survival of the M-DM1 group was significantly higher than that of the other groups. These results demonstrate that M-DM1 is highly effective in inhibiting tumor growth and prolonging survival in melanoma." REF00262 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 28.47% 16 days 4 mg/kg Female BALB/c mice 4T1-mCherry-Luc cells xenograft model. Malignant neoplasms of the mouse mammary gland 4T1-mCherry-Luc cell "The mice TNBC 4T1-mCherry-Luc model was constructed by subcutaneous inoculation to study the anti-tumor effect of PTX-SM-TAR NPs in vivo. 4T1-mCherry-Luc cells reacted with D-luciferin potassium salt to produce bioluminescence, which was determined by an IVIS spectrum imaging system. The intensity of the fluorescence signal is related to tumor size, hence tumor growth in mice can be monitored in real-time. As shown in Figure 9a, the tumor growth rate of the PTX-SM-TAR NPs group was lower than that of the NS, TAR, and PTX groups. At the end of the experiment, the tumor tissue was weighed, and the results were consistent with the trend of fluorescence intensity. The tumor inhibition rate was 43.24% in the PTX-SM-TAR NPs, 28.47% in the PTX, and 7.81% in the TAR. The tumor inhibitory effect of the PTX-SM-TAR NPs group was stronger than that of the PTX group, and the difference was significant." REF00255 DRG00007 Temozolomide Survival rate = 30% 46 h/day for 5 consecutive days 10 μmol/L . Pancreatic serotonin-producing neuroendocrine tumor BON-1 cell "TMZ is an alkylating agent that causes cell death through DNA-damaging mechanisms. To determine whether MMC(TMZ)-TOC induces the same cytotoxic effects through a receptor-dependent process, we first studied its DNA-damaging properties in IMR-32 cells that endogenously express SSTR2. We performed an alkaline comet assay to evaluate the ability of our drug conjugate to produce single- and double-stranded DNA breaks. As shown in Figure 3A,B, the targeted agent-induced DNA breaks that were similar to free TMZ, resulting in migrating DNA fragments (comet tail) from the nucleoid (comet head). The damaging effects of MMC(TMZ)-TOC were significantly reduced (P < 0.0001) when cells were preincubated with blocking doses of the high-affinity SSTR2 antagonist JR11, indicating receptor-dependent cytotoxicity. Next, we used a colony formation assay to assess the long-term survival and reproductive capability of the cells after treatment with the PDC. We treated BON1 (receptor-negative) and BON1-SSTR2 (receptor-positive) cells with 2 µmol/L MMC(TMZ)-TOC or 10 µmol/L TMZ for 5 consecutive days, seeded the cells at a low-density number, and allowed them to grow and form colonies for 14 days. The clonogenic survival data showed that MMC(TMZ)-TOC produced cytotoxic effects in the receptor-positive BON1-SSTR2 cells (P < 0.01) similar to clinically relevant doses of TMZ. Conversely, no cytotoxicity was observed in receptor-negative BON1 cells following treatment with the drug conjugate, further illustrating the receptor-dependent effects of the PDC." REF00297 DRG00020 Docetaxel Tumor Growth Inhibition value (TGI) = 30% 15 days 15 mg/kg Nude mice hOvCSC cells xenograft tumor model. Ovarian cancer Ovarian cancer stem cell (hOvCSC) "In vivo assessment in tumor-bearing animal models classically complements cell cultures data for comparing cancer treatment efficacies. For this reason, hTNBCSC and hOvCSC xenografts were implanted subcutaneously into immunodeficient mice as described in the Methods section with only 1000 cells given their highly tumorigenic nature. Three days later, the animals began receiving weekly IV bolus administration of either vehicle, docetaxel, or TH1902. Docetaxel was administered at a dose (15 mg/kg/week; for 3 cycles) in accordance with the estimated maximal tolerated dose (MTD) for mice, as well as at of the MTD (3.75 mg/kg/week). TH1902 was administered at doses (35 and 8.75 mg/kg/week) which contained quantities of docetaxel equivalent to those in the two administrations of free docetaxel. From the size of the hTNBCSC and hOvCSC tumors, it is apparent that docetaxel had little impact on xenografts growth when administered neither at its MTD, for both hTNBCSC and hOvCSC, nor at of this dosage as reflected by the growth curves. TH1902, when administered at a dosage equivalent to docetaxel at its MTD, provided greater tumor growth inhibition than did docetaxel for both xenograft models. Furthermore, higher dosage of administered TH1902 (up to 1.5 equivalent of docetaxel MTD) did not generate significant differences in terms of hOvCSC tumor inhibition without affecting mice body weights suggesting that TH1902, even at higher doses, is better tolerated compared to docetaxel. Then, in order to statistically compare the effects of docetaxel and TH1902 on tumor growth, the tumor sizes measured at the vehicle group endpoint were compared and statistically significant differences between the tumor sizes in vehicle-treated animals found in TH1902-treated animals for hTNBCSC and hOvCSC. Mouse body weight was used as an indicator of the morbidity associated with administration of docetaxel or TH1902. Administration of docetaxel at its MTD provoked a weight loss that approached 10% after the treatments, which is often observed in xenograft models with administration of docetaxel at this level. The body weights of animals treated with an equivalent quantity or a 1.5-fold equivalent of TH1902 were maintained at a roughly constant level throughout the experiment. The animals treated with vehicle recorded a slight weight gain (~5%) over this period while animals treated with the lower dosages of docetaxel or TH1902 were similar to the animals treated with vehicle. The body weight data indicates that TH1902 appears to be better tolerated than the equivalent quantity of free docetaxel, in addition to the fact that TH1902 is more efficacious than docetaxel when administered in vivo in the murine models of CSC tested." REF00234 DRG00020 Docetaxel Tumor Growth Inhibition value (TGI) = 30% 20 days 15 mg/kg Nude mice hTNBCSC cells xenograft tumor model. Triple-negative breast cancer Human triple-negative breast cancer stem cell (hTNBCSC) "In vivo assessment in tumor-bearing animal models classically complements cell cultures data for comparing cancer treatment efficacies. For this reason, hTNBCSC and hOvCSC xenografts were implanted subcutaneously into immunodeficient mice as described in the Methods section with only 1000 cells given their highly tumorigenic nature. Three days later, the animals began receiving weekly IV bolus administration of either vehicle, docetaxel, or TH1902. Docetaxel was administered at a dose (15 mg/kg/week; for 3 cycles) in accordance with the estimated maximal tolerated dose (MTD) for mice, as well as at of the MTD (3.75 mg/kg/week). TH1902 was administered at doses (35 and 8.75 mg/kg/week) which contained quantities of docetaxel equivalent to those in the two administrations of free docetaxel. From the size of the hTNBCSC and hOvCSC tumors, it is apparent that docetaxel had little impact on xenografts growth when administered neither at its MTD, for both hTNBCSC and hOvCSC, nor at of this dosage as reflected by the growth curves. TH1902, when administered at a dosage equivalent to docetaxel at its MTD, provided greater tumor growth inhibition than did docetaxel for both xenograft models. Furthermore, higher dosage of administered TH1902 (up to 1.5 equivalent of docetaxel MTD) did not generate significant differences in terms of hOvCSC tumor inhibition without affecting mice body weights suggesting that TH1902, even at higher doses, is better tolerated compared to docetaxel. Then, in order to statistically compare the effects of docetaxel and TH1902 on tumor growth, the tumor sizes measured at the vehicle group endpoint were compared and statistically significant differences between the tumor sizes in vehicle-treated animals found in TH1902-treated animals for hTNBCSC and hOvCSC. Mouse body weight was used as an indicator of the morbidity associated with administration of docetaxel or TH1902. Administration of docetaxel at its MTD provoked a weight loss that approached 10% after the treatments, which is often observed in xenograft models with administration of docetaxel at this level. The body weights of animals treated with an equivalent quantity or a 1.5-fold equivalent of TH1902 were maintained at a roughly constant level throughout the experiment. The animals treated with vehicle recorded a slight weight gain (~5%) over this period while animals treated with the lower dosages of docetaxel or TH1902 were similar to the animals treated with vehicle. The body weight data indicates that TH1902 appears to be better tolerated than the equivalent quantity of free docetaxel, in addition to the fact that TH1902 is more efficacious than docetaxel when administered in vivo in the murine models of CSC tested." REF00234 DRG00014 Baicalin MDA increase rate = 30% 24 h . . Normal H9c2 cell "The accumulation of iron is a characteristic feature of ferroptosis. Intracellular iron, especially labile ferrous iron, can react with oxidants to generate cytotoxic hydroxyl radicals via Fenton reactions, thereby promoting ferroptosis. FerroOrange staining revealed significantly increased intracellular Fe2+ levels in DOX-treated H9c2 cells compared to controls, indicating DOX induced iron dyshomeostasis, resulting in ferrous iron buildup and subsequent ferroptosis. BA-NFs alleviated the accumulation of intracellular ferrous ions, suppressing ferroptosis. Fe2+ accumulation may disrupt the balance between LPO and oxygen homeostasis. We observed that BA-NFs efficiently attenuated DOX-induced elevation in malondialdehyde (MDA), a lipid peroxidation end-product, while increased antioxidant glutathione (GSH) levels. These findings suggested that BA-NFs can prevent DOX-induced ferroptosis in cardiomyocytes. Furthermore, protein expression of SLC7A11 and GPX4, key components of the antioxidant defense system against ferroptosis, was examined. DOX significantly decreased SLC7A11 and GPX4 expression in H9c2 cells compared to controls, suggesting DOX disrupts cellular antioxidant systems leading to ferroptosis. BA and BA-NFs partially restored SLC7A11 and GPX4 expression versus DOX treatment, with BA-NFs exhibiting the most significant impact. Together, these results indicate BA-NFs specifically inhibits DOX-induced cardiomyocyte ferroptosis by reducing intracellular iron accumulation and enhancing antioxidant system gene expression. In addition, the cardiotoxic effects of DOX are mediated via excessive oxidative stress and induced mitochondrial damage, thereby activating intrinsic apoptosis as an additional pathway. Flow cytometric analysis using Annexin V-Fitc/PI staining revealed that BA-NFs potently attenuated DOX-induced cardiomyocyte apoptosis, with a more pronounced effect than BA alone. DOX enhanced the green fluorescent signal of cleaved caspase-3 (as a biomarker of apoptosis) in H9c2 cells, whereas BA-NFs significantly inhibited this upregulation. These results provided further evidence that BA-NFs serve as potential therapeutic approaches for DIC." REF00290 DRG00011 Doxorubicin Cell viability = 32% 48 h 0.47 μM . Ovarian serous cystadenocarcinoma SK-OV-3 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00020 Docetaxel Tumor Growth Inhibition value (TGI) = 35.90% Once a week for 4 weeks 20 mg/kg A549 cells mouse xenograft model. Lung adenocarcinoma A-549 cell "Intraperitoneal administration of 20 mg/kg DTX-P7 (equivalent to DTX dose calculated as DTX) reduced tumor growth by 93.2% compared with control mice, whereas the tumor growth inhibition of DTX was only 35.9%. " REF00222 DRG00029 Morphine Maximal antinociceptive effect = 36% Intravenous administration 120min 1.5 mg/kg Male CD1 mice. . . "Similar results were also obtained in the hot-plate test using male CD1 mice. Over a 2-hour period, both morphine and An2-morphine caused similar increases in hot-plate latencies. Likewise, mice receiving An2-M6G (6 mg/kg i.v.) also exhibited a sustained and superior analgesic effect compared with equimolar doses of either morphine or M6G." REF00100 DRG00011 Doxorubicin Cell viability = 37% 48 h 0.47 μM . Breast adenocarcinoma MDA-MB-231 cell "Analysis of dot-plots suggests that the rL-A9 peptide alone does not exert any significant cytotoxic effects on either HER2-positive, SKOV3 cells or HER2-negative, MDA-MB-231 cells at any of the investigated concentrations. In contrast, incubation of drug DOX with either of the cells resulted in enhanced cell death with a negligible viable population even at lower concentrations. However, it was observed that the peptide-drug conjugate, rL-A9-DOX had a concentration-dependent impact on cell death (SKOV3 cells). Notably, nearly half of the cell population died at 3.75µM. At a concentration of 15µM, there were only 5% viable SKOV3 cells. The higher percent of the viable cell population was observed at corresponding concentrations in the case of incubation of rL-A9-DOX with HER2-negative, MDA-MB-231 cells. Comparative data of viability in two different cell lines is presented in Figure 6 for the peptide-drug conjugate, rL-A9-DOX." REF00309 DRG00011 Doxorubicin Cell survival rate = 37% 24 h 15 μg/mL . Invasive breast carcinoma MCF-7 cell "Subsequently, the cell toxicity of the DOX, DOX-SH, and PNS-SS-DOX was also investigated using the CCK-8 method. As shown in Figure8b, all three materials display significant concentration-dependent cytotoxicity. Additionally, it can be observed that at the same concentration, the cytotoxicity of DOX-SH to MCF-7 cells was nearly identical to that of DOX, indicating that thiolation did not affect the efficacy of DOX. Furthermore, the PNS-SS-DOX group exhibited stronger cytotoxicity to MCF-7 cells. Particularly, at a material concentration of 20µgmL1, the cell survival rate for the PNS-SS-DOX group was only 12%, while that of the DOX-SH group was 20%. We suggest that this effect is possibly due to the modification of PNSs with DOX-SH. On one hand, the hydrophilic peptides effectively improved the solubility of the hydrophobic drug DOX-SH, and on the other hand, the positively charged PNSs enhanced the drug uptake by cancer cells, thus increasing the cancer cell killing efficacy." REF00302 DRG00029 Morphine Maximal antinociceptive effect = 37% Subcutaneous administration 30min 3 mg/kg Rat model. . . "We also measured the analgesic effect of An2-morphine and An2-M6G after subcutaneous injections. Despite similar MPE at the peak effect, subcutaneous injection of 20 mg/kg An2-morphine (equivalent to 5.5 mg/kg of morphine) produced an analgesic effect that was more prolonged over the time than what was observed with an equimolar dose of morphine." REF00100 DRG00009 Camptothecin Tumor Growth Inhibition value (TGI) = 39% Injected via tail vein every three days 8 μmol/kg SK-BR-3 tumor-bearing nude mice xenograft model. Breast adenocarcinoma SK-BR-3 cell "To study the in vivo anti-tumor activity of Z8, SK-BR-3 tumor bearing nude mice were administered once every three days. As shown in Fig. 11A-11D, CPT and Z8 demonstrated significant inhibitory effects on SK-BR-3 tumor growth, with the Z8 group exhibiting more pronounced inhibition compared to CPT. Notably, the average tumor volume and weight in the Z8 group were the smallest among all groups, including the control and CPT groups. Moreover, to further study the toxicity of CPT and Z8, serums of mice were collected for blood biochemical analysis. As shown in Fig. 11E-H, treatment with both CPT and Z8 resulted in increased levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST), but the effect of Z8 group was relatively low, indicating that Z8 was safer than CPT in vivo. Furthermore, in CPT group, urea nitrogen levels increased significantly, whereas no significant change was observed in the Z8 group, indicating potential renal function impairment following CPT treatment, whereas Z8 showed better safety in this regard. Additionally, the levels of alkaline phosphatase (ALP), total protein (TP), albumin (ALB), globulin (GLOB) and creatinine (CREA) did not significantly differ between the control group and the treatment groups. Finally, compared to the control group, histological examination using H&E staining (Hematoxylin and Eosin staining) of the major organs in the treatment group did not reveal obvious cell necrosis and inflammatory cell infiltration, indicating that Z8 would not bring additional toxicity." REF00312 DRG00039 Morphine-6-glucuronide Maximal antinociceptive effect = 40% Intravenous administration 30min 3 mg/kg Male CD1 mice. . . "Similar results were also obtained in the hot-plate test using male CD1 mice. Over a 2-hour period, both morphine and An2-morphine caused similar increases in hot-plate latencies. Likewise, mice receiving An2-M6G (6 mg/kg i.v.) also exhibited a sustained and superior analgesic effect compared with equimolar doses of either morphine or M6G." REF00100 DRG00014 Baicalin GSH/GSSG increase ratio = 40% 24 h . . Normal H9c2 cell "The accumulation of iron is a characteristic feature of ferroptosis. Intracellular iron, especially labile ferrous iron, can react with oxidants to generate cytotoxic hydroxyl radicals via Fenton reactions, thereby promoting ferroptosis. FerroOrange staining revealed significantly increased intracellular Fe2+ levels in DOX-treated H9c2 cells compared to controls, indicating DOX induced iron dyshomeostasis, resulting in ferrous iron buildup and subsequent ferroptosis. BA-NFs alleviated the accumulation of intracellular ferrous ions, suppressing ferroptosis. Fe2+ accumulation may disrupt the balance between LPO and oxygen homeostasis. We observed that BA-NFs efficiently attenuated DOX-induced elevation in malondialdehyde (MDA), a lipid peroxidation end-product, while increased antioxidant glutathione (GSH) levels. These findings suggested that BA-NFs can prevent DOX-induced ferroptosis in cardiomyocytes. Furthermore, protein expression of SLC7A11 and GPX4, key components of the antioxidant defense system against ferroptosis, was examined. DOX significantly decreased SLC7A11 and GPX4 expression in H9c2 cells compared to controls, suggesting DOX disrupts cellular antioxidant systems leading to ferroptosis. BA and BA-NFs partially restored SLC7A11 and GPX4 expression versus DOX treatment, with BA-NFs exhibiting the most significant impact. Together, these results indicate BA-NFs specifically inhibits DOX-induced cardiomyocyte ferroptosis by reducing intracellular iron accumulation and enhancing antioxidant system gene expression. In addition, the cardiotoxic effects of DOX are mediated via excessive oxidative stress and induced mitochondrial damage, thereby activating intrinsic apoptosis as an additional pathway. Flow cytometric analysis using Annexin V-Fitc/PI staining revealed that BA-NFs potently attenuated DOX-induced cardiomyocyte apoptosis, with a more pronounced effect than BA alone. DOX enhanced the green fluorescent signal of cleaved caspase-3 (as a biomarker of apoptosis) in H9c2 cells, whereas BA-NFs significantly inhibited this upregulation. These results provided further evidence that BA-NFs serve as potential therapeutic approaches for DIC." REF00290 DRG00014 Baicalin SLC7A11/GAPDH increase rate = 41% 24 h . . Normal H9c2 cell "The accumulation of iron is a characteristic feature of ferroptosis. Intracellular iron, especially labile ferrous iron, can react with oxidants to generate cytotoxic hydroxyl radicals via Fenton reactions, thereby promoting ferroptosis. FerroOrange staining revealed significantly increased intracellular Fe2+ levels in DOX-treated H9c2 cells compared to controls, indicating DOX induced iron dyshomeostasis, resulting in ferrous iron buildup and subsequent ferroptosis. BA-NFs alleviated the accumulation of intracellular ferrous ions, suppressing ferroptosis. Fe2+ accumulation may disrupt the balance between LPO and oxygen homeostasis. We observed that BA-NFs efficiently attenuated DOX-induced elevation in malondialdehyde (MDA), a lipid peroxidation end-product, while increased antioxidant glutathione (GSH) levels. These findings suggested that BA-NFs can prevent DOX-induced ferroptosis in cardiomyocytes. Furthermore, protein expression of SLC7A11 and GPX4, key components of the antioxidant defense system against ferroptosis, was examined. DOX significantly decreased SLC7A11 and GPX4 expression in H9c2 cells compared to controls, suggesting DOX disrupts cellular antioxidant systems leading to ferroptosis. BA and BA-NFs partially restored SLC7A11 and GPX4 expression versus DOX treatment, with BA-NFs exhibiting the most significant impact. Together, these results indicate BA-NFs specifically inhibits DOX-induced cardiomyocyte ferroptosis by reducing intracellular iron accumulation and enhancing antioxidant system gene expression. In addition, the cardiotoxic effects of DOX are mediated via excessive oxidative stress and induced mitochondrial damage, thereby activating intrinsic apoptosis as an additional pathway. Flow cytometric analysis using Annexin V-Fitc/PI staining revealed that BA-NFs potently attenuated DOX-induced cardiomyocyte apoptosis, with a more pronounced effect than BA alone. DOX enhanced the green fluorescent signal of cleaved caspase-3 (as a biomarker of apoptosis) in H9c2 cells, whereas BA-NFs significantly inhibited this upregulation. These results provided further evidence that BA-NFs serve as potential therapeutic approaches for DIC." REF00290 DRG00007 Temozolomide Survival rate = 45% 46 h/day for 5 consecutive days 10 μmol/L . SSR2 positive neuroendocrine tumour BON1-SSTR2 cell "TMZ is an alkylating agent that causes cell death through DNA-damaging mechanisms. To determine whether MMC(TMZ)-TOC induces the same cytotoxic effects through a receptor-dependent process, we first studied its DNA-damaging properties in IMR-32 cells that endogenously express SSTR2. We performed an alkaline comet assay to evaluate the ability of our drug conjugate to produce single- and double-stranded DNA breaks. As shown in Figure 3A,B, the targeted agent-induced DNA breaks that were similar to free TMZ, resulting in migrating DNA fragments (comet tail) from the nucleoid (comet head). The damaging effects of MMC(TMZ)-TOC were significantly reduced (P < 0.0001) when cells were preincubated with blocking doses of the high-affinity SSTR2 antagonist JR11, indicating receptor-dependent cytotoxicity. Next, we used a colony formation assay to assess the long-term survival and reproductive capability of the cells after treatment with the PDC. We treated BON1 (receptor-negative) and BON1-SSTR2 (receptor-positive) cells with 2 µmol/L MMC(TMZ)-TOC or 10 µmol/L TMZ for 5 consecutive days, seeded the cells at a low-density number, and allowed them to grow and form colonies for 14 days. The clonogenic survival data showed that MMC(TMZ)-TOC produced cytotoxic effects in the receptor-positive BON1-SSTR2 cells (P < 0.01) similar to clinically relevant doses of TMZ. Conversely, no cytotoxicity was observed in receptor-negative BON1 cells following treatment with the drug conjugate, further illustrating the receptor-dependent effects of the PDC." REF00297 DRG00009 Camptothecin Cell survival rate = 46% 72 h 10 μM . Mouse melanoma B16-F10 cell "Subsequently, the cytotoxicity of these conjugates against B16-F10 cells was determined. As shown in Fig. 4B, CPT-AAM-1 and CPT-AAM-2 displayed significant pH-dependent antitumor activity after 72 h of treatment, whereas the cytotoxicity of CPT showed no obvious difference at pH 7.4 and 5.5. Notably, CPT-AAM-1 and CPT-AAM-2 exhibited greater cytotoxicity than free CPT under acidic conditions, particularly at high concentrations. Compared to CPT-AAM-2, CPT-AAM-1 displayed strong antitumor activity, suggesting that AAM-1 could deliver more CPT molecules into cells. In addition, this result further demonstrates that the C-terminus of AAM is more suitable for drug conjugation than the N-terminus." REF00300 DRG00029 Morphine Maximal antinociceptive effect = 49.70% Intravenous administration 30min 1 mg/kg Rat model. . . "When equimolar doses of morphine conjugated to An2 (An2-morphine; 3 mg/kg) were compared with unconjugated morphine (1 mg/kg) at the peak effect, similar levels of antinociception were observed, reaching 46% and 49.7% of MPE, respectively." REF00100 DRG00020 Docetaxel Tumor Growth Inhibition value (TGI) = 50% 12 days . SORT1-positive B16-F10 cells female CD1 nude mice xenograft tumor models. . . "B16-F10 melanoma syngeneic tumors were generated, with tumor sizes monitored as described in the Methods section. Tumors in xenograft-bearing, vehicle-treated mice grew at an exponential rate. Partial inhibition of tumor growth was observed after IV administration of 15 mg/kg/wk docetaxel, whereas treatment with a docetaxel-equivalent quantity of TH1902 (35 mg/kg/wk) induced tumor regression after two treatments over the period measured. Due to rapid tumor growth, only two administrations of the test articles could be performed on a weekly schedule. B16-F10 melanoma tumors from the mice treated with either vehicle, docetaxel, or TH1902 were then excised, fixed in formalin, and immunohistochemically examined." REF00303 DRG00407 Combretastatin A4 Half Maximal Effective Dosage (ED50) = 12:00 PM . . . Colon cancer HT29 cell . REF100147 DRG00011 Doxorubicin Cell survival rate = 55% 24 h 10 μg/mL . Invasive breast carcinoma MCF-7 cell "Subsequently, the cell toxicity of the DOX, DOX-SH, and PNS-SS-DOX was also investigated using the CCK-8 method. As shown in Figure8b, all three materials display significant concentration-dependent cytotoxicity. Additionally, it can be observed that at the same concentration, the cytotoxicity of DOX-SH to MCF-7 cells was nearly identical to that of DOX, indicating that thiolation did not affect the efficacy of DOX. Furthermore, the PNS-SS-DOX group exhibited stronger cytotoxicity to MCF-7 cells. Particularly, at a material concentration of 20µgmL1, the cell survival rate for the PNS-SS-DOX group was only 12%, while that of the DOX-SH group was 20%. We suggest that this effect is possibly due to the modification of PNSs with DOX-SH. On one hand, the hydrophilic peptides effectively improved the solubility of the hydrophobic drug DOX-SH, and on the other hand, the positively charged PNSs enhanced the drug uptake by cancer cells, thus increasing the cancer cell killing efficacy." REF00302 DRG00009 Camptothecin Apoptosis rate = 55.80% 24 h 2 μM . Breast adenocarcinoma SK-BR-3 cell "SK-BR-3 cells (2 105 cells/well) in the logarithmic phase were collected and seeded in 6-well plates and cultured overnight at 37 C and 5 % CO2. 1 µM and 2 µM Z8 and 1 µM CPT were added to the cells and incubated for 24 h. Then cells were collected and washed three times with cold PBS. Annexin-V-FITC/PI Detection Kit (Vazyme, Nanjing, China) was used to stain the cells and the fluorescences were detected by flow cytometry within 1 h. FlowJo software was used to analyze the data." REF00312 DRG00011 Doxorubicin Cell viability = 62.90% 24 h . . Cutaneous melanoma OCM-3 cell "In order to investigate whether AEZS-108 inhibits cell proliferation and its extent, OCM3 cells were treated either with 5 M AEZS-108 or equal amount of doxorubicin. MTS assay was performed after 24 and 48 hours of treatment. AEZS-108 and doxorubicin have been shown to reduce cell proliferation by 36.3% (p< 0.001) and 62.9% (p< 0.001) respectively after 24 hours, and by 84.7% (p< 0.001) and 89.7% (p< 0.001) respectively after 48 hours, (Figure 2)." REF00091 DRG00009 Camptothecin Cell survival rate = 67% 72 h 5 μM . Mouse melanoma B16-F10 cell "Subsequently, the cytotoxicity of these conjugates against B16-F10 cells was determined. As shown in Fig. 4B, CPT-AAM-1 and CPT-AAM-2 displayed significant pH-dependent antitumor activity after 72 h of treatment, whereas the cytotoxicity of CPT showed no obvious difference at pH 7.4 and 5.5. Notably, CPT-AAM-1 and CPT-AAM-2 exhibited greater cytotoxicity than free CPT under acidic conditions, particularly at high concentrations. Compared to CPT-AAM-2, CPT-AAM-1 displayed strong antitumor activity, suggesting that AAM-1 could deliver more CPT molecules into cells. In addition, this result further demonstrates that the C-terminus of AAM is more suitable for drug conjugation than the N-terminus." REF00300 DRG00039 Morphine-6-glucuronide Maximal antinociceptive effect = 68% Subcutaneous administration 60min 4.5 mg/kg Rat model. . . "We also measured the analgesic effect of An2-morphine and An2-M6G after subcutaneous injections. Despite similar MPE at the peak effect, subcutaneous injection of 20 mg/kg An2-morphine (equivalent to 5.5 mg/kg of morphine) produced an analgesic effect that was more prolonged over the time than what was observed with an equimolar dose of morphine." REF00100 DRG00014 Baicalin GPX4/GAPDH increase ratio = 70% 24 h . . Normal H9c2 cell "The accumulation of iron is a characteristic feature of ferroptosis. Intracellular iron, especially labile ferrous iron, can react with oxidants to generate cytotoxic hydroxyl radicals via Fenton reactions, thereby promoting ferroptosis. FerroOrange staining revealed significantly increased intracellular Fe2+ levels in DOX-treated H9c2 cells compared to controls, indicating DOX induced iron dyshomeostasis, resulting in ferrous iron buildup and subsequent ferroptosis. BA-NFs alleviated the accumulation of intracellular ferrous ions, suppressing ferroptosis. Fe2+ accumulation may disrupt the balance between LPO and oxygen homeostasis. We observed that BA-NFs efficiently attenuated DOX-induced elevation in malondialdehyde (MDA), a lipid peroxidation end-product, while increased antioxidant glutathione (GSH) levels. These findings suggested that BA-NFs can prevent DOX-induced ferroptosis in cardiomyocytes. Furthermore, protein expression of SLC7A11 and GPX4, key components of the antioxidant defense system against ferroptosis, was examined. DOX significantly decreased SLC7A11 and GPX4 expression in H9c2 cells compared to controls, suggesting DOX disrupts cellular antioxidant systems leading to ferroptosis. BA and BA-NFs partially restored SLC7A11 and GPX4 expression versus DOX treatment, with BA-NFs exhibiting the most significant impact. Together, these results indicate BA-NFs specifically inhibits DOX-induced cardiomyocyte ferroptosis by reducing intracellular iron accumulation and enhancing antioxidant system gene expression. In addition, the cardiotoxic effects of DOX are mediated via excessive oxidative stress and induced mitochondrial damage, thereby activating intrinsic apoptosis as an additional pathway. Flow cytometric analysis using Annexin V-Fitc/PI staining revealed that BA-NFs potently attenuated DOX-induced cardiomyocyte apoptosis, with a more pronounced effect than BA alone. DOX enhanced the green fluorescent signal of cleaved caspase-3 (as a biomarker of apoptosis) in H9c2 cells, whereas BA-NFs significantly inhibited this upregulation. These results provided further evidence that BA-NFs serve as potential therapeutic approaches for DIC." REF00290 DRG00009 Camptothecin Cell survival rate = 71% 72 h 2.5 μM . Mouse melanoma B16-F10 cell "Subsequently, the cytotoxicity of these conjugates against B16-F10 cells was determined. As shown in Fig. 4B, CPT-AAM-1 and CPT-AAM-2 displayed significant pH-dependent antitumor activity after 72 h of treatment, whereas the cytotoxicity of CPT showed no obvious difference at pH 7.4 and 5.5. Notably, CPT-AAM-1 and CPT-AAM-2 exhibited greater cytotoxicity than free CPT under acidic conditions, particularly at high concentrations. Compared to CPT-AAM-2, CPT-AAM-1 displayed strong antitumor activity, suggesting that AAM-1 could deliver more CPT molecules into cells. In addition, this result further demonstrates that the C-terminus of AAM is more suitable for drug conjugation than the N-terminus." REF00300 DRG00029 Morphine Maximal antinociceptive effect = 74% Subcutaneous administration 30min 5 mg/kg Rat model. . . "We also measured the analgesic effect of An2-morphine and An2-M6G after subcutaneous injections. Despite similar MPE at the peak effect, subcutaneous injection of 20 mg/kg An2-morphine (equivalent to 5.5 mg/kg of morphine) produced an analgesic effect that was more prolonged over the time than what was observed with an equimolar dose of morphine." REF00100 DRG00012 Paclitaxel Cell viability = 75% 24 h 200 nM . Glioblastoma U-87MG cell Both PDCs showed higher in vitro cytotoxicity than free PTX (Figure 4B). REF00077 DRG00011 Doxorubicin Cell survival rate = 76% 24 h 5 μg/mL . Invasive breast carcinoma MCF-7 cell "Subsequently, the cell toxicity of the DOX, DOX-SH, and PNS-SS-DOX was also investigated using the CCK-8 method. As shown in Figure8b, all three materials display significant concentration-dependent cytotoxicity. Additionally, it can be observed that at the same concentration, the cytotoxicity of DOX-SH to MCF-7 cells was nearly identical to that of DOX, indicating that thiolation did not affect the efficacy of DOX. Furthermore, the PNS-SS-DOX group exhibited stronger cytotoxicity to MCF-7 cells. Particularly, at a material concentration of 20µgmL1, the cell survival rate for the PNS-SS-DOX group was only 12%, while that of the DOX-SH group was 20%. We suggest that this effect is possibly due to the modification of PNSs with DOX-SH. On one hand, the hydrophilic peptides effectively improved the solubility of the hydrophobic drug DOX-SH, and on the other hand, the positively charged PNSs enhanced the drug uptake by cancer cells, thus increasing the cancer cell killing efficacy." REF00302 DRG00009 Camptothecin Cell survival rate = 82% 72 h 1.25 μM . Mouse melanoma B16-F10 cell "Subsequently, the cytotoxicity of these conjugates against B16-F10 cells was determined. As shown in Fig. 4B, CPT-AAM-1 and CPT-AAM-2 displayed significant pH-dependent antitumor activity after 72 h of treatment, whereas the cytotoxicity of CPT showed no obvious difference at pH 7.4 and 5.5. Notably, CPT-AAM-1 and CPT-AAM-2 exhibited greater cytotoxicity than free CPT under acidic conditions, particularly at high concentrations. Compared to CPT-AAM-2, CPT-AAM-1 displayed strong antitumor activity, suggesting that AAM-1 could deliver more CPT molecules into cells. In addition, this result further demonstrates that the C-terminus of AAM is more suitable for drug conjugation than the N-terminus." REF00300 DRG00039 Morphine-6-glucuronide Maximal antinociceptive effect = 87% Intravenous administration 45min 4.5 mg/kg Rat model. . . The intravenous injection of 1.54.5 mg/kg M6G induced a %MPE ranging from 30% to 87% REF00100 DRG00029 Morphine Maximal antinociceptive effect = 88.60% Intravenous administration 30min 3 mg/kg Rat model. . . "Our results show that the administration of morphine (0.33 mg/kg, i.v.) produced a maximal antinociceptive effect (%MPE) of 88.6% at the highest dose tested." REF00100 DRG00011 Doxorubicin Cell viability = 89.70% 48 h . . Normal OCM-4 cell "In order to investigate whether AEZS-108 inhibits cell proliferation and its extent, OCM3 cells were treated either with 5 M AEZS-108 or equal amount of doxorubicin. MTS assay was performed after 24 and 48 hours of treatment. AEZS-108 and doxorubicin have been shown to reduce cell proliferation by 36.3% (p< 0.001) and 62.9% (p< 0.001) respectively after 24 hours, and by 84.7% (p< 0.001) and 89.7% (p< 0.001) respectively after 48 hours, (Figure 2)." REF00091 DRG00029 Morphine Maximal antinociceptive effect = 91% Intravenous administration 30min 10 mg/kg Male CD1 mice. . . "Similar results were also obtained in the hot-plate test using male CD1 mice. Over a 2-hour period, both morphine and An2-morphine caused similar increases in hot-plate latencies. Likewise, mice receiving An2-M6G (6 mg/kg i.v.) also exhibited a sustained and superior analgesic effect compared with equimolar doses of either morphine or M6G." REF00100 DRG00076 Estradiol Half Maximal Effective Concentration (EC50) = 10:00 PM . . . Endometrial adenocarcinoma Ishikawa cell . REF102044 DRG00009 Camptothecin Cell survival rate = 95% 72 h 0.625 μM . Mouse melanoma B16-F10 cell "Subsequently, the cytotoxicity of these conjugates against B16-F10 cells was determined. As shown in Fig. 4B, CPT-AAM-1 and CPT-AAM-2 displayed significant pH-dependent antitumor activity after 72 h of treatment, whereas the cytotoxicity of CPT showed no obvious difference at pH 7.4 and 5.5. Notably, CPT-AAM-1 and CPT-AAM-2 exhibited greater cytotoxicity than free CPT under acidic conditions, particularly at high concentrations. Compared to CPT-AAM-2, CPT-AAM-1 displayed strong antitumor activity, suggesting that AAM-1 could deliver more CPT molecules into cells. In addition, this result further demonstrates that the C-terminus of AAM is more suitable for drug conjugation than the N-terminus." REF00300 DRG00005 Primaquine Half Maximal Inhibitory Concentration (IC50) ≥ ≥100 uM . . . Colon adenocarcinoma SW620 cell . REF102190 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) ≥ ≥20 ug/mL . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF102104 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) < <0.1 nM . . . Mammary gland malignant neoplasms EMT6 cell . REF100182 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) < <0.1 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF102105 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <0.1 ug/mL . . . Lymphoblastic leukemia L1210 cell . REF100247 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <0.1 ug/mL . . . Melanoma B16 cell . REF100486 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <0.5 ug/mL . . . Gastric adenocarcinoma SNU-1 cell . REF101913 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <0.55 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100697 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <0.55 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100697 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <1 ng/mL . . . Osteosarcoma MG-22A cell . REF100416 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) < <1 ng/mL . . . Astrocytoma SF268 cell . REF102269 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <1 nM . . . Lung adenosquamous carcinoma NCI-H647 cell . REF100305 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <1 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101133 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <1 nM . . . Stomach adenocarcinoma BGC-823 cell . REF101133 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) < <1 nM . . . Colon carcinoma HCT 116 cell . REF100448 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) < <1 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100067 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) < <1 ug/mL . . . Endocervical adenocarcinoma L132 cell . REF100095 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) < <1 ug/mL . . . Glioblastoma SF-295 cell . REF100058 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) < <1 ug/mL . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100058 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <1.1 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100329 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <1.8 nM . . . Invasive breast carcinoma MCF-7 cell . REF101450 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) < <10 nM . . . Melanoma UACC-62 cell . REF101494 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <10 nM . . . Breast adenocarcinoma SK-BR-3 cell . REF101108 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <10 nM . . . Colon carcinoma HCT 116 cell . REF101108 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <10 nM . . . Invasive breast carcinoma MCF-7 cell . REF101108 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <10 nM . . . Invasive breast carcinoma ZR-75-1 cell . REF101108 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <10 nM . . . Normal MCF-12A cell . REF101108 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <10 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101761 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <10 nM . . . Lung adenocarcinoma A-549 cell . REF101761 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) < <10 nM . . . Invasive breast carcinoma MCF-7 cell . REF101761 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) < <10 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101407 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) < <10 nM . . . Lung adenocarcinoma A-549 cell . REF101407 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) < <10 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF100523 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) < <10 nM . . . Lung large cell carcinoma NCI-H460 cell . REF102203 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) < <10 nM . . . Colon adenocarcinoma HCT 15 cell . REF102130 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) < <10 pM . . . Skin squamous cell carcinoma A431 cell . REF100724 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) < <10 ug/mL . . . Pleural epithelioid mesothelioma NCI-H226 cell . REF101942 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <10 ug/mL . . . Pleural epithelioid mesothelioma NCI-H226 cell . REF101942 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <10 uM . . . Colon cancer HT29 cell . REF100957 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <100 nM . . . Hepatoblastoma Hep-G2 cell . REF101053 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <100 nM . . . Hepatocellular carcinoma Huh-7 cell . REF101053 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <100 nM . . . Invasive breast carcinoma MCF-7 cell . REF101053 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) < <100 nM . . . Melanoma G-361 cell . REF101983 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <100 nM . . . Endocervical adenocarcinoma HeLa cell . REF101930 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <100 nM . . . Invasive breast carcinoma MCF-7 cell . REF101842 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <100 nM . . . Prostate carcinoma PC-3 cell . REF101842 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <100 nM . . . Melanoma B16 cell . REF101048 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <100 nM . . . Invasive breast carcinoma ZR-75-1 cell . REF101019 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <100 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101019 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <100 nM . . . Prostate carcinoma DU145 cell . REF100979 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <100 nM . . . Normal COLO205 cell . REF100971 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <1000 nM . . . Hepatoblastoma Hep-G2 cell . REF101393 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <1000 nM . . . Colon carcinoma HCT 116 cell . REF101093 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <1000 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101979 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <1000 nM . . . Endocervical adenocarcinoma HeLa cell . REF101938 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <1000 nM . . . Colon carcinoma HCT 116 cell . REF101884 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <1000 nM . . . Lung adenocarcinoma A-549 cell . REF101788 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) < <16 nM . . . Endocervical adenocarcinoma HeLa cell . REF101761 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) < <16 nM . . . Hepatoblastoma Hep-G2 cell . REF101761 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) < <16 nM . . . Prostate carcinoma DU145 cell . REF101761 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <2 ug/mL . . . Lung adenocarcinoma A-549 cell . REF100649 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) < <2.3 ng/mL . . . Lung adenocarcinoma A-549 cell . REF101384 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <20 ng/mL . . . Colon carcinoma HCT 116 cell . REF101937 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <20 ng/mL . . . Melanoma B16 cell . REF101937 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <25 ng/mL . . . Astrocytoma U-251MG cell . REF101395 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <25 ng/mL . . . Normal HaCaT cell . REF101395 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <25 ng/mL . . . Lung large cell carcinoma NCI-H460 cell . REF101251 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <3 ng/mL . . . Colon adenocarcinoma WiDr cell . REF100311 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <3 ng/mL . . . Invasive breast carcinoma MCF-7 cell . REF100311 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <3 ng/mL . . . Melanoma M19-MEL cell . REF100311 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <3 ng/mL . . . Pleural epithelioid mesothelioma NCI-H226 cell . REF100311 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <3 ng/mL . . . Renal carcinoma A498 cell . REF100311 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) < <3 uM . . . Normal NIH3T3 cell . REF102215 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) < <30 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100006 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) < <30 nM . . . Colon cancer HT29 cell . REF101218 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) < <30 nM . . . Prostate carcinoma PC-3 cell . REF101218 DRG00012 Paclitaxel 90% Growth Inhibition (GI90) < <4 ng/mL . . . Lung adenocarcinoma A-549 cell . REF101402 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <46 nM . . . Invasive breast carcinoma MCF-7 cell . REF101851 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) < <46 nM . . . Astrocytoma U-251MG cell . REF101370 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) < <5 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100431 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) < <5 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100109 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) < <5 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100109 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) < <5 ng/mL . . . Prostate carcinoma DU145 cell . REF100109 DRG00019 Methotrexate Half Maximal Effective Dosage (ED50) < <50 nM . . . Acute myeloid leukemia HL-60 cell . REF100164 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) < <50 nM . . . Pancreatic ductal adenocarcinoma BxPC-3 cell . REF102306 DRG00011 Doxorubicin Half Maximal Cytotoxicity Concentration (CC50) < <500 nM . . . Prostate carcinoma PC-3 cell . REF101723 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <6.25 uM . . . Normal TERT-RPE1 cell . REF101627 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) < <6.25 uM . . . Normal hTERT-BJ cell . REF101627 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <8 nM . . . Colon adenocarcinoma SW480 cell . REF101824 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <8 nM . . . Normal NCM460 cell . REF101824 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <8 nM . . . Hepatocellular carcinoma SMMC-7721 cell . REF101601 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <8 nM . . . Lung adenocarcinoma A-549 cell . REF101591 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <8 nM . . . Acute myeloid leukemia HL-60 cell . REF101590 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <8 nM . . . Invasive breast carcinoma MCF-7 cell . REF101331 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <8 nM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF100825 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) < <80 nM . . . Clear cell renal cell carcinoma OS-RC-2 cell . REF100854 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) > >0.1 ug/mL . . . Acute myeloid leukemia HL-60 cell . REF102014 DRG00403 Fluconazole Half Maximal Cytotoxicity Concentration (CC50) > >0.128 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF102507 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >1 mM . . . Normal Vero cell . REF102374 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) > >1 ng/mL . . . Glioblastoma SF-295 cell . REF100062 DRG00221 Acyclovir Half Maximal Effective Dosage (ED50) > >1.3 nM . . . Normal Vero cell . REF102009 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) > >1.862 mM . . . Colon adenocarcinoma KM12 cell . REF102352 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >10 nM . . . Lung adenocarcinoma A-549 cell . REF101662 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >10 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100352 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >10 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100329 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) > >10 ug/mL . . . Lymphoma P388 cell . REF102113 DRG00403 Fluconazole Half Maximal Inhibitory Concentration (IC50) > >10 ug/mL . . . Normal Vero cell . REF100526 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) > >10 uM . . . Colon carcinoma HCT 116 cell . REF102500 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Colon carcinoma RKO cell . REF102494 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) > >10 uM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF102187 DRG00009 Camptothecin Half Maximal Effective Dosage (ED50) > >10 uM . . . Invasive breast carcinoma MCF-7 cell . REF100683 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Bladder carcinoma T24 cell . REF100340 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Invasive breast carcinoma MCF-7 cell . REF101769 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Breast ductal carcinoma HCC1937 cell . REF101313 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Colon cancer HT29 cell . REF101193 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) > >10 uM . . . Invasive breast carcinoma MCF-7 cell . REF100683 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) > >10 uM . . . Prostate carcinoma LNCaP cell . REF100683 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Endocervical adenocarcinoma HeLa cell . REF102228 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Burkitt lymphoma DG-75 cell . REF101576 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Diffuse large B-cell lymphoma OCI-Ly3 cell . REF101576 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Mantle cell lymphoma JeKo-1 cell . REF101576 DRG00065 Irinotecan Half Maximal Growth Inhibition (GI50) > >10 uM . . . Lung adenocarcinoma A-549 cell . REF101017 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101656 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Colon cancer HT29 cell . REF101656 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Normal Vero cell . REF100090 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >10 uM . . . Normal MT-2 cell . REF102119 DRG00406 Monastrol Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Gastric adenocarcinoma AGS cell . REF102250 DRG00406 Monastrol Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Lung adenocarcinoma A-549 cell . REF102250 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Gastric carcinoma NUGC-3 cell . REF102115 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Colon cancer HT29 cell . REF101012 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) > >10 uM . . . Lung adenocarcinoma A-549 cell . REF101012 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) > >100 nM . . . Hepatoblastoma Hep-G2 cell . REF100848 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) > >100 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF100924 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) > >100 nM . . . Hepatoblastoma Hep-G2 cell . REF100912 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) > >100 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF100912 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) > >100 nM . . . Sezary syndrome H9 cell . REF102210 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >100 ug/mL . . . Lung squamous cell carcinoma PC-10 cell . REF102014 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) > >100 ug/mL . . . Colon adenocarcinoma SW480 cell . REF102028 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) > >100 ug/mL . . . Esophageal squamous cell carcinoma TE-2 cell . REF102014 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) > >100 ug/mL . . . Lung squamous cell carcinoma PC-10 cell . REF102014 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) > >100 ug/mL . . . Bladder carcinoma T24 cell . REF102013 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >100 ug/mL . . . Normal Vero cell . REF100070 DRG00221 Acyclovir Half Maximal Infective Dose (ID50) > >100 ug/mL . . . EBV-related Burkitt lymphoma Raji cell . REF100013 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >100 ug/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102058 DRG00003 Fluorouracil Half Maximal Lethal Concentration (IC50) > >100 uM . . . Colon adenocarcinoma KM12 cell . REF102520 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Hepatoblastoma Hep-G2 cell . REF102470 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Lung adenocarcinoma A-549 cell . REF102460 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . HPV-related endocervical adenocarcinoma Bel7402/5-FU cell . REF102380 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Colon adenocarcinoma SW620 cell . REF102236 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF102231 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Chronic myeloid leukemia K562 cell . REF102166 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Endocervical adenocarcinoma HeLa cell . REF102166 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Colon cancer HT29 cell . REF101965 DRG00004 Gemfibrozil Half Maximal Cytotoxicity Concentration (CC50) > >100 uM . . . Normal MT4 cell . REF102347 DRG00009 Camptothecin Half Maximal Lethal Concentration (IC50) > >100 uM . . . Invasive breast carcinoma MCF-7 cell . REF101161 DRG00009 Camptothecin Half Maximal Lethal Concentration (IC50) > >100 uM . . . Chronic myeloid leukemia K562 cell . REF100902 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Pancreatic adenocarcinoma SW1990 cell . REF101042 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) > >100 uM . . . Prostate carcinoma DU145 cell . REF100979 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) > >100 uM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100822 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Chronic myeloid leukemia K562 cell . REF101995 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF101654 DRG00012 Paclitaxel Half Maximal Lethal Concentration (IC50) > >100 uM . . . Chronic myeloid leukemia K562 cell . REF100902 DRG00012 Paclitaxel Half Maximal Lethal Concentration (IC50) > >100 uM . . . Invasive breast carcinoma MCF-7 cell . REF100902 DRG00019 Methotrexate Half Maximal Growth Inhibition (GI50) > >100 uM . . . Colon cancer HT29 cell . REF101536 DRG00019 Methotrexate Half Maximal Growth Inhibition (GI50) > >100 uM . . . Endocervical adenocarcinoma HeLa cell . REF101536 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Endocervical adenocarcinoma HeLa cell . REF101462 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101414 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Colon carcinoma HCT 116 cell . REF101832 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Hepatoblastoma Hep-G2 cell . REF101832 DRG00075 Ibuprofen Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Cervical carcinoma L02 cell . REF102380 DRG00075 Ibuprofen Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Hepatoma Bel-7402 cell . REF102380 DRG00075 Ibuprofen Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . HPV-related endocervical adenocarcinoma Bel7402/5-FU cell . REF102380 DRG00076 Estradiol Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Normal CHO cell . REF102332 DRG00107 Betulinic acid Half Maximal Cytotoxicity Concentration (CC50) > >100 uM . . . Normal Vero cell . REF102344 DRG00149 Quinine Half Maximal Cytotoxicity Concentration (CC50) > >100 uM . . . Hepatoblastoma Hep-G2 cell . REF102453 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >100 uM . . . Normal MT4 cell . REF102347 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >100 uM . . . Normal Vero cell . REF102156 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >100 uM . . . Burkitt lymphoma Daudi cell . REF100092 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >100 uM . . . Normal MT4 cell . REF102267 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) > >100 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102102 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102075 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >100 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102075 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Leukemia C8166 cell . REF100074 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) > >100 uM . . . Normal Vero cell . REF100005 DRG00406 Monastrol Half Maximal Inhibitory Concentration (IC50) > >100 uM . . . Lung adenocarcinoma A-549 cell . REF102481 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100917 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) > >1000 nM . . . T acute lymphoblastic leukemia CEM/C2 cell . REF100558 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Lung small cell carcinoma H69AR cell . REF100544 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Lung adenocarcinoma NCI-H1650 cell . REF101539 DRG00012 Paclitaxel Half Maximal Lethal Concentration (IC50) > >1000 nM . . . Glioblastoma SNB-75 cell . REF100197 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) > >1000 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100197 DRG00012 Paclitaxel Half Maximal Lethal Concentration (IC50) > >1000 nM . . . Lung small cell carcinoma DMS 114 cell . REF100197 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) > >1000 nM . . . Non-small cell lung carcinoma HOP-62 cell . REF100197 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Normal R2 cell . REF101262 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Acute monocytic leukemia MV4-11 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Breast ductal carcinoma BT-549 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Cutaneous melanoma SK-MEL-28 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Invasive breast carcinoma Hs 578T cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Invasive breast carcinoma T-47D cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Melanoma SK-MEL-2 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Melanoma Malme-3M cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Non-small cell lung carcinoma HOP-92 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Ovarian adenocarcinoma OVCAR-4 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Renal carcinoma RXF 393 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Glioblastoma SNB-75 cell . REF100246 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF102452 DRG00065 Irinotecan Half Maximal Growth Inhibition (GI50) > >1000 nM . . . Invasive breast carcinoma MCF-7 cell . REF100558 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >1000 nM . . . Normal MT4 cell . REF100066 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >1000 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100066 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) > >1000 nM . . . Colon cancer HT29 cell . REF100544 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >11.4 ug/mL . . . Normal MT4 cell . REF102098 DRG00078 Cholesterol Half Maximal Inhibitory Concentration (IC50) > >128 ug/mL . . . Normal Vero cell . REF102173 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) > >15 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100276 DRG00010 Daunorubicin Half Maximal Lethal Concentration (IC50) > >17.2 uM . . . Colon cancer HT29 cell . REF102204 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) > >17.2 uM . . . Colon cancer HT29 cell . REF101471 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >2 uM . . . Hepatoma Bel-7402 cell . REF101128 DRG00149 Quinine Half Maximal Effective Dosage (ED50) > >20 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102129 DRG00149 Quinine Half Maximal Inhibitory Concentration (IC50) > >20 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102059 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >20 uM . . . Breast adenocarcinoma SK-BR-3 cell . REF102234 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >20 uM . . . Lung adenocarcinoma A-549 cell . REF102234 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) > >20 uM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF101227 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) > >20 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101227 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) > >20 uM . . . Sezary syndrome H9 cell . REF102060 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >20 uM . . . Normal MT4 cell . REF102037 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) > >20 uM . . . Lung adenocarcinoma A-549 cell . REF102407 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >200 ug/mL . . . Erythroleukemia HEL cell . REF102099 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) > >200 ug/mL . . . Erythroleukemia HEL cell . REF100043 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) > >200 ug/mL . . . Erythroleukemia HEL cell . REF100042 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >200 ug/mL . . . Leukemia C8166 cell . REF102160 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >200 uM . . . Normal Vero cell . REF102159 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >200 uM . . . Erythroleukemia HEL cell . REF102082 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >200 uM . . . Normal MT-2 cell . REF100101 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >222 uM . . . Burkitt lymphoma Daudi cell . REF102119 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >250 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102311 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) > >287 uM . . . Osteosarcoma U2OS cell . REF101092 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) > >287 uM . . . Prostate carcinoma PC-3 cell . REF101092 DRG00403 Fluconazole Half Maximal Inhibitory Concentration (IC50) > >294.1 uM . . . Normal L6 cell . REF102335 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >3 uM . . . Colon carcinoma RKO cell . REF100606 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >3 uM . . . Cervical epithelial carcinoma KB 3-1 cell . REF100433 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >3.3 ug/mL . . . Lung squamous cell carcinoma Calu-1 cell . REF100008 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >3.3 ug/mL . . . Osteosarcoma G-292 cell . REF100008 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >3.74 uM . . . Normal MT4 cell . REF101648 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >30 uM . . . Lung adenocarcinoma A-549 cell . REF101640 DRG00407 Combretastatin A4 Half Maximal Cytotoxicity Concentration (CC50) > >300 uM . . . Normal HEK-293T cell . REF102429 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) > >375 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102106 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) > >4 uM . . . Lung large cell carcinoma NCI-H460 cell . REF102219 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) > >40 uM . . . Normal TERT-RPE1 cell . REF101579 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) > >40 uM . . . Normal BJ cell . REF101579 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) > >40 uM . . . Prostate carcinoma PC-3 cell . REF101579 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) > >400 nM . . . Colon adenocarcinoma HCT 15 cell . REF100544 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >400 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF101765 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) > >400 uM . . . Colon adenocarcinoma LoVo cell . REF100623 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) > >400 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100623 DRG00121 Naproxen Half Maximal Inhibitory Concentration (IC50) > >400 uM . . . Invasive breast carcinoma MCF-7 cell . REF101879 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >400 uM . . . Erythroleukemia HEL cell . REF102244 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >400 uM . . . Endocervical adenocarcinoma HeLa cell . REF102122 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) > >410 uM . . . Lung squamous cell carcinoma QG-95 cell . REF102046 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) > >410 uM . . . Colon adenocarcinoma SW48 cell . REF102046 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) > >5 uM . . . Invasive breast carcinoma MCF-7 cell . REF100920 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >5 uM . . . Lymphoblastic leukemia L1210 cell . REF100963 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >5 uM . . . Lymphoma P388 cell . REF100963 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >5 uM . . . Lymphoma P388/ADR cell . REF100394 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) > >5 uM . . . Clear cell renal cell carcinoma Caki-1 cell . REF100061 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >5.092 mM . . . Leukemia C8166 cell . REF102145 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Colon cancer HT29 cell . REF102355 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Lung adenocarcinoma A-549 cell . REF102354 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100890 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) > >50 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100289 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Normal BJ cell . REF102433 DRG00075 Ibuprofen Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102353 DRG00075 Ibuprofen Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Colon cancer HT29 cell . REF102353 DRG00078 Cholesterol Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Colon cancer HT29 cell . REF100737 DRG00121 Naproxen Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102353 DRG00121 Naproxen Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Colon cancer HT29 cell . REF102353 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Normal Vero cell . REF102084 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) > >50 uM . . . Erythroleukemia HEL cell . REF100059 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) > >50 uM . . . Normal Vero cell . REF100041 DRG00065 Irinotecan Half Maximal Infective Dose (ID50) > >500 nM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF102097 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >500 nM . . . Normal MT4 cell . REF102386 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) > >500 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101568 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) > >500 uM . . . Laryngeal carcinoma HEp-2 cell . REF101568 DRG00107 Betulinic acid Half Maximal Cytotoxicity Concentration (CC50) > >500 uM . . . Prostate carcinoma DU145 cell . REF101568 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >500 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102053 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >500 uM . . . T acute lymphoblastic leukemia Jurkat cell . REF100035 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >6 uM . . . Invasive breast carcinoma MCF-7 cell . REF100358 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > >60 ug/mL . . . Invasive breast carcinoma ZR-75-1 cell . REF100572 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) > >62.5 ug/mL . . . Normal NIH3T3 cell . REF100103 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >7.48 uM . . . Normal MT4 cell . REF102503 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >749 uM . . . Leukemia C8166 cell . REF100105 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >80 uM . . . Normal MT4 cell . REF102060 DRG00221 Acyclovir Half Maximal Infective Dose (ID50) > >800 uM . . . Normal WI-38 cell . REF100045 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) > >85 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100810 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >890 uM . . . Erythroleukemia HEL cell . REF100102 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) > >890 uM . . . Normal Vero cell . REF100097 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) > >93.55 uM . . . Normal MT4 cell . REF102174 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) > >970 uM . . . Normal MT-2 cell . REF100010 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.006 µg/mL 72 h . . Colon carcinoma HCT 116 cell "The cytotoxicity of PPP in MCF-7, HCT116, and 4T1 cells was investigated by MTT assay. The half maximal inhibitory concentration (IC50) of PPP NPs and free PTX was calculated to be 0.066 and 0.028 g/mL on MCF-7 cells, 0.044 and 0.006 g/mL on HCT116, 0.212 and 0.01 g/mL on 4T1 cells which indicated a lower cell growth inhibition ability than free PTX. The result may be owing to the extremely stable property of PPP and low legumain expression in vitro leading to incomplete release of PTX and PTP-7 (Edgington et al., 2013). Moreover, the holographic microscopy studies showed the changes in cellular morphology of MCF-7 cells after treated with PPP for 3h. Notably, PPP led to the morphological features of apoptosis such as shrinkage, losing contact with neighboring cells and floating relative to control." REF00221 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.01 µg/mL 72 h . . Mammary carcinoma 4T1 cell "The cytotoxicity of PPP in MCF-7, HCT116, and 4T1 cells was investigated by MTT assay. The half maximal inhibitory concentration (IC50) of PPP NPs and free PTX was calculated to be 0.066 and 0.028 g/mL on MCF-7 cells, 0.044 and 0.006 g/mL on HCT116, 0.212 and 0.01 g/mL on 4T1 cells which indicated a lower cell growth inhibition ability than free PTX. The result may be owing to the extremely stable property of PPP and low legumain expression in vitro leading to incomplete release of PTX and PTP-7 (Edgington et al., 2013). Moreover, the holographic microscopy studies showed the changes in cellular morphology of MCF-7 cells after treated with PPP for 3h. Notably, PPP led to the morphological features of apoptosis such as shrinkage, losing contact with neighboring cells and floating relative to control." REF00221 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.02±0.001 µM 72 h . . Ovarian endometrioid adenocarcinoma A2780 cell "To investigate the anticancer activity of the GnRH-III drug conjugates, cell viability studies have been performed on A2780 ovarian cancer and Panc-1 pancreatic cancer cells. The GnRH-R expression of these cell lines was determined by Western blot studies. In the case of the A2780 cells, a distinct band at 38 kDa could be detected which corresponds to the full-length human GnRH-R. In contrast, the signal intensity of the 38 kDa band was much lower for Panc-1 pancreatic cancer cells being in line with our previous results. Thus, the antiproliferative activity of the GnRH-drug conjugates was studied on high-GnRH-R-expressing A2780 cells and low-GnRH-R-expressing Panc-1 cells. Since the release of free Dau and PTX can be assumed, both drugs were used as controls. The cells were treated for either 24 h (Dau conjugates) or six hours (PTX compounds), followed by additional incubation with fresh growth medium until 72 h after treatment initiation. The obtained results reveal, on the one hand, that the non-cleavable linker-containing conjugates possess a reduced anticancer activity in comparison to the cleavable conjugates and, on the other hand, that the activity of the all GnRH-III-drug conjugates was substantially reduced compared to the free drug. Moreover, all compounds displayed a lower biological activity on Panc-1 cells than on A2780. In the case of the cleavable GnRH-III-Dau conjugates, the IC50 values varied between 2.8511.18 M on A2780 cells, whereby the best activity was obtained for compound 13 (2.85 M) which contained the cathepsin B-cleavage site Val-Ala and the GnRH-III-[2δHis-3D-Tic-4Lys(Bu)] peptide carrier. Apart from that, the IC50 values of the cleavable PTX conjugates on A2780 cells are in the same sub-micromolar range and vary between 0.510.77 M, while the activity of these conjugates was approximately 10 times lower on Panc-1 cells (5.038.15 M)." REF00219 DRG00026 Maytansine Half Maximal Inhibitory Concentration (IC50) = 0.026 µM 48 h . . Colon carcinoma HCT 116 cell "To determine the activity of the compounds, we analyzed the effects of them on cell growth and migration in HCT116 cells. We found that LWJ-M30 displayed significant inhibition of cell proliferation and clone formation ability. The IC50 of LWJ-M30 was 0.047 µM which was close to DM1 (0.026 µM). According to the results of wound-healing assay and transwell migration assay, LWJ-M30 also dramatically showed a inhibitory effect on cells migration. These results suggested that LWJ-M30 could inhibit the cells proliferation and migration." REF00257 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.026±0.008 µM 24 h . . Melanoma B16 cell "In vitro studies of the antiproliferative effect showed that melanoma-targeting Dau-conjugates have significantly higher efficacy on B16 murine melanoma cell lines in comparison to human melanoma cell lines (A2058, M24, and WM983B). The IC50 values were detected between 2 and 2.9 M on B16 cells, where the highest activity was detected in the case of conjugate Conj3, followed by Conj2 and Conj1. Moreover, the relative potencies of conjugates to free Dau were also calculated as independent values from cell lines. A higher value of relative potency indicated the elevated targeting capacity of the conjugate on particular cell lines. Considering relative potencies, the best targeting capacity was shown to be Conj3 on all four cell lines, followed by Conj2 and Conj1. The highest antitumor activity of Conj3 on cells can be explained by the presence of two Dau molecules in this conjugate in comparison with Conj2 and Conj1, which contain only one drug molecule." REF00294 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.028 µg/mL 72 h . . Invasive breast carcinoma MCF-7 cell "The cytotoxicity of PPP in MCF-7, HCT116, and 4T1 cells was investigated by MTT assay. The half maximal inhibitory concentration (IC50) of PPP NPs and free PTX was calculated to be 0.066 and 0.028 g/mL on MCF-7 cells, 0.044 and 0.006 g/mL on HCT116, 0.212 and 0.01 g/mL on 4T1 cells which indicated a lower cell growth inhibition ability than free PTX. The result may be owing to the extremely stable property of PPP and low legumain expression in vitro leading to incomplete release of PTX and PTP-7 (Edgington et al., 2013). Moreover, the holographic microscopy studies showed the changes in cellular morphology of MCF-7 cells after treated with PPP for 3h. Notably, PPP led to the morphological features of apoptosis such as shrinkage, losing contact with neighboring cells and floating relative to control." REF00221 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.03 µM 48 h . . Normal Human umbilical vein endothelial cell "The coupling of peptides with chemotherapeutic drugs often increased the solubility of the drugs, so the solubility of peptide-drug conjugates was determined, and the results were shown in Fig. S9. DOX free base exhibited poor solubility, with a solubility of approximately 0.22 0.03 mg/mL in PBS. However, upon formation of a peptide-drug conjugate, the hydrophilicity of the peptide significantly enhanced the solubility of DOX. The solubility of pHA-AHX-VAP-DOX and pHA-AOHX-VAP-DOX drastically increased to 7.09 0.15 mg/mL and 17.29 0.43 mg/mL, which was 32-fold and 78-fold higher than that of the DOX free base, respectively. The improved solubility performance was consistent with their LogP values predicted by the ALOGPS 2.1 program." REF00308 DRG00407 Combretastatin A4 Half Maximal Effective Dosage (ED50) = 0.03 pM . . . Cutaneous melanoma SK-MEL-5 cell . REF100147 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.04±0.007 µM 24 h . . Melanoma A2058 cell "In vitro studies of the antiproliferative effect showed that melanoma-targeting Dau-conjugates have significantly higher efficacy on B16 murine melanoma cell lines in comparison to human melanoma cell lines (A2058, M24, and WM983B). The IC50 values were detected between 2 and 2.9 M on B16 cells, where the highest activity was detected in the case of conjugate Conj3, followed by Conj2 and Conj1. Moreover, the relative potencies of conjugates to free Dau were also calculated as independent values from cell lines. A higher value of relative potency indicated the elevated targeting capacity of the conjugate on particular cell lines. Considering relative potencies, the best targeting capacity was shown to be Conj3 on all four cell lines, followed by Conj2 and Conj1. The highest antitumor activity of Conj3 on cells can be explained by the presence of two Dau molecules in this conjugate in comparison with Conj2 and Conj1, which contain only one drug molecule." REF00294 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.045±0.12 µM 24 h . . Melanoma SK-MEL-202 cell "The in vitro cytostatic effects of Dauα-MSH conjugates were compared with the PrestoBlue assay, which has a higher specificity and efficacy that of the previously used MTT assay, using the same six human melanoma cell lines used in the real-time qPCR assay. According to our results, free daunomycin exhibited the lowest IC50 values, and therefore the highest cytostatic effect, due to the fact that free daunomycin passively diffuses into cells. Our Dauα-MSH conjugates showed similar trends in the effectiveness of the tested cell lines. Conj2 and Conj4 resulted in IC50 values in the low µM range. A calculation of the targeting indices showed that compound Conj2 had an over 2-times higher targeting efficiency in most cell lines compared to the A2058 cell line. Interestingly, WM983A showed the lowest TI among the high-MC1R-expressing cell lines compared to A2058, and WM983B exhibited high TI regardless of the relatively low MC1R expression on the mRNA level. In the case of Conj4, the treatment resulted in the highest TIs with OCM-1 and WM983B cell lines." REF00294 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.050±0.023 µM 24 h . . Melanoma WM983B cell "In vitro studies of the antiproliferative effect showed that melanoma-targeting Dau-conjugates have significantly higher efficacy on B16 murine melanoma cell lines in comparison to human melanoma cell lines (A2058, M24, and WM983B). The IC50 values were detected between 2 and 2.9 M on B16 cells, where the highest activity was detected in the case of conjugate Conj3, followed by Conj2 and Conj1. Moreover, the relative potencies of conjugates to free Dau were also calculated as independent values from cell lines. A higher value of relative potency indicated the elevated targeting capacity of the conjugate on particular cell lines. Considering relative potencies, the best targeting capacity was shown to be Conj3 on all four cell lines, followed by Conj2 and Conj1. The highest antitumor activity of Conj3 on cells can be explained by the presence of two Dau molecules in this conjugate in comparison with Conj2 and Conj1, which contain only one drug molecule." REF00294 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.06 µM 48 h . . Glioblastoma U87 cell "The coupling of peptides with chemotherapeutic drugs often increased the solubility of the drugs, so the solubility of peptide-drug conjugates was determined, and the results were shown in Fig. S9. DOX free base exhibited poor solubility, with a solubility of approximately 0.22 0.03 mg/mL in PBS. However, upon formation of a peptide-drug conjugate, the hydrophilicity of the peptide significantly enhanced the solubility of DOX. The solubility of pHA-AHX-VAP-DOX and pHA-AOHX-VAP-DOX drastically increased to 7.09 0.15 mg/mL and 17.29 0.43 mg/mL, which was 32-fold and 78-fold higher than that of the DOX free base, respectively. The improved solubility performance was consistent with their LogP values predicted by the ALOGPS 2.1 program." REF00308 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.1 ng/mL . . . Invasive breast carcinoma MCF-7 cell . REF102103 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 0.1 nM . . . Colon cancer HT29 cell . REF100931 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 0.1 nM . . . Acute myeloid leukemia HL-60 cell . REF102224 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 0.1 ug/mL . . . Colon cancer HT29 cell . REF100299 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.1 ug/mL . . . Colon cancer HT29 cell . REF102103 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.1 ug/mL . . . Glioma XF498 cell . REF101936 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.1 ug/mL . . . Colon adenocarcinoma DLD-1 cell . REF100480 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.1 ug/mL . . . Lung adenocarcinoma A-549 cell . REF100480 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.1 ug/mL . . . Colon adenocarcinoma SW620 cell . REF100285 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.1 ug/mL . . . Lung adenocarcinoma NCI-H23 cell . REF100285 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.1 ug/mL . . . Melanoma SK-MEL-2 cell . REF100277 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 0.1 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF102032 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) = 0.1 ug/mL . . . Erythroleukemia HEL cell . REF100051 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.104 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100203 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.105 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100133 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.11 pM . . . Colon carcinoma HCT 116 cell . REF101758 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.11 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101936 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.11 ug/mL . . . Gastric carcinoma NUGC-3 cell . REF100613 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.11 ug/mL . . . Colon carcinoma HCT 116 cell . REF100361 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.11 ug/mL . . . Melanoma LOX IMVI cell . REF100328 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.11 ug/mL . . . Melanoma B16 cell . REF100328 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.11 ug/mL . . . Melanoma SK-MEL-2 cell . REF100257 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.11 ug/mL . . . Normal CHO cell . REF100252 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.11 ug/mL . . . Colon cancer HT29 cell . REF100151 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.112 ng/ml . . . Colon cancer HT29 cell . REF100133 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.113 ug/ml . . . Renal carcinoma A498 cell . REF100254 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.119±0.025 µM 24 h . . Amelanotic melanoma M24 cell "In vitro studies of the antiproliferative effect showed that melanoma-targeting Dau-conjugates have significantly higher efficacy on B16 murine melanoma cell lines in comparison to human melanoma cell lines (A2058, M24, and WM983B). The IC50 values were detected between 2 and 2.9 M on B16 cells, where the highest activity was detected in the case of conjugate Conj3, followed by Conj2 and Conj1. Moreover, the relative potencies of conjugates to free Dau were also calculated as independent values from cell lines. A higher value of relative potency indicated the elevated targeting capacity of the conjugate on particular cell lines. Considering relative potencies, the best targeting capacity was shown to be Conj3 on all four cell lines, followed by Conj2 and Conj1. The highest antitumor activity of Conj3 on cells can be explained by the presence of two Dau molecules in this conjugate in comparison with Conj2 and Conj1, which contain only one drug molecule." REF00294 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.12 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100743 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.12 ug/mL . . . Colon adenocarcinoma WiDr cell . REF100546 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.12 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100479 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.12 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100435 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.12 ug/mL . . . Glioma XF498 cell . REF100425 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.12±0.07 µM 24 h . . Melanoma A2058 cell "The in vitro cytostatic effects of Dauα-MSH conjugates were compared with the PrestoBlue assay, which has a higher specificity and efficacy that of the previously used MTT assay, using the same six human melanoma cell lines used in the real-time qPCR assay. According to our results, free daunomycin exhibited the lowest IC50 values, and therefore the highest cytostatic effect, due to the fact that free daunomycin passively diffuses into cells. Our Dauα-MSH conjugates showed similar trends in the effectiveness of the tested cell lines. Conj2 and Conj4 resulted in IC50 values in the low µM range. A calculation of the targeting indices showed that compound Conj2 had an over 2-times higher targeting efficiency in most cell lines compared to the A2058 cell line. Interestingly, WM983A showed the lowest TI among the high-MC1R-expressing cell lines compared to A2058, and WM983B exhibited high TI regardless of the relatively low MC1R expression on the mRNA level. In the case of Conj4, the treatment resulted in the highest TIs with OCM-1 and WM983B cell lines." REF00294 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.124 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100263 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.126 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100188 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.129 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100297 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.13 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100766 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.13 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100529 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.13 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100495 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.13 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100328 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.136 ug/mL . . . Colon adenocarcinoma DLD-1 cell . REF100323 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.136 ug/mL . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100364 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.14 ug/mL . . . Chronic myeloid leukemia K562 cell . REF100654 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.14 ug/mL . . . Astrocytoma SF268 cell . REF100609 DRG00038 Monomethyl auristatin E Half Maximal Effective Concentration (EC50) = 0.14±0.03 nM 48 h . . Melanoma DX3-puro cell "Both NH2-PDC-1 and [natCu]PDC-1 exhibited integrin αvβ6-dependent cytotoxicity, only reducing cell viability of the αvβ6-positive cells. For [natCu]PDC-1 high cytotoxicity was observed in DX3puroβ6 (+) cells (EC50: 0.058 0.003 nM) with no observable cytotoxic effects in the DX3puro () cells, while free MMAE had almost equal cytotoxicity to both DX3puroβ6 (+) and DX3puro cells () (EC50: 0.140.15 nM). The pancreatic cells also showed αvβ6-dependent cytotoxicity for [natCu]PDC-1 (EC50: BxPC-3 65.1 10.6 nM) and required high concentrations of 250 nM for noticeable cytotoxic effects in the minimally integrin αvβ6-expressing MIA PaCa-2 cells. Again, free, non-targeted MMAE exhibited nondiscriminatory cytotoxicity among the pancreatic cells with an effective concentration range of EC50 = 0.160.5 nM. Peptides NH2-2 and [natCu]2 were not toxic to any cells." REF00272 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.142 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100185 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.144 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100733 DRG00009 Camptothecin Half Maximal Effective Concentration (EC50) = 0.15 nM . . . Colon adenocarcinoma SW620 cell . REF100088 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.15 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101976 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.15 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100435 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 0.15 ug/mL . . . Erythroleukemia HEL cell . REF100037 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.15 uM . . . Prostate carcinoma DU145 cell . REF100574 DRG00038 Monomethyl auristatin E Half Maximal Effective Concentration (EC50) = 0.15±0.02 nM 48 h . . Melanoma DX3-puro/beta6 cell "Both NH2-PDC-1 and [natCu]PDC-1 exhibited integrin αvβ6-dependent cytotoxicity, only reducing cell viability of the αvβ6-positive cells. For [natCu]PDC-1 high cytotoxicity was observed in DX3puroβ6 (+) cells (EC50: 0.058 0.003 nM) with no observable cytotoxic effects in the DX3puro () cells, while free MMAE had almost equal cytotoxicity to both DX3puroβ6 (+) and DX3puro cells () (EC50: 0.140.15 nM). The pancreatic cells also showed αvβ6-dependent cytotoxicity for [natCu]PDC-1 (EC50: BxPC-3 65.1 10.6 nM) and required high concentrations of 250 nM for noticeable cytotoxic effects in the minimally integrin αvβ6-expressing MIA PaCa-2 cells. Again, free, non-targeted MMAE exhibited nondiscriminatory cytotoxicity among the pancreatic cells with an effective concentration range of EC50 = 0.160.5 nM. Peptides NH2-2 and [natCu]2 were not toxic to any cells." REF00272 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.152 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100232 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.153 ng/mL . . . Colon cancer HT29 cell . REF100203 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.16 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100965 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.16 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100365 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.16 ug/mL . . . Gastric adenocarcinoma SNU-16 cell . REF100271 DRG00038 Monomethyl auristatin E Half Maximal Effective Concentration (EC50) = 0.16±0.01 µM 48 h . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell "Both NH2-PDC-1 and [natCu]PDC-1 exhibited integrin αvβ6-dependent cytotoxicity, only reducing cell viability of the αvβ6-positive cells. For [natCu]PDC-1 high cytotoxicity was observed in DX3puroβ6 (+) cells (EC50: 0.058 0.003 nM) with no observable cytotoxic effects in the DX3puro () cells, while free MMAE had almost equal cytotoxicity to both DX3puroβ6 (+) and DX3puro cells () (EC50: 0.140.15 nM). The pancreatic cells also showed αvβ6-dependent cytotoxicity for [natCu]PDC-1 (EC50: BxPC-3 65.1 10.6 nM) and required high concentrations of 250 nM for noticeable cytotoxic effects in the minimally integrin αvβ6-expressing MIA PaCa-2 cells. Again, free, non-targeted MMAE exhibited nondiscriminatory cytotoxicity among the pancreatic cells with an effective concentration range of EC50 = 0.160.5 nM. Peptides NH2-2 and [natCu]2 were not toxic to any cells." REF00272 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.163 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100909 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.17 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100657 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.17 ug/mL . . . Colon carcinoma HCT 116 cell . REF100461 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.17 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100425 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.17 ug/mL . . . Colon adenocarcinoma SW620 cell . REF100328 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.17 ug/mL . . . Colon adenocarcinoma HCC 2998 cell . REF100328 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.17 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100235 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.17±0.01 µM 72 h . . Pancreatic ductal adenocarcinoma PANC-1 cell "To investigate the anticancer activity of the GnRH-III drug conjugates, cell viability studies have been performed on A2780 ovarian cancer and Panc-1 pancreatic cancer cells. The GnRH-R expression of these cell lines was determined by Western blot studies. In the case of the A2780 cells, a distinct band at 38 kDa could be detected which corresponds to the full-length human GnRH-R. In contrast, the signal intensity of the 38 kDa band was much lower for Panc-1 pancreatic cancer cells being in line with our previous results. Thus, the antiproliferative activity of the GnRH-drug conjugates was studied on high-GnRH-R-expressing A2780 cells and low-GnRH-R-expressing Panc-1 cells. Since the release of free Dau and PTX can be assumed, both drugs were used as controls. The cells were treated for either 24 h (Dau conjugates) or six hours (PTX compounds), followed by additional incubation with fresh growth medium until 72 h after treatment initiation. The obtained results reveal, on the one hand, that the non-cleavable linker-containing conjugates possess a reduced anticancer activity in comparison to the cleavable conjugates and, on the other hand, that the activity of the all GnRH-III-drug conjugates was substantially reduced compared to the free drug. Moreover, all compounds displayed a lower biological activity on Panc-1 cells than on A2780. In the case of the cleavable GnRH-III-Dau conjugates, the IC50 values varied between 2.8511.18 M on A2780 cells, whereby the best activity was obtained for compound 13 (2.85 M) which contained the cathepsin B-cleavage site Val-Ala and the GnRH-III-[2δHis-3D-Tic-4Lys(Bu)] peptide carrier. Apart from that, the IC50 values of the cleavable PTX conjugates on A2780 cells are in the same sub-micromolar range and vary between 0.510.77 M, while the activity of these conjugates was approximately 10 times lower on Panc-1 cells (5.038.15 M)." REF00219 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.179 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100265 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.18 ng/mL . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100337 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 0.18 ug/mL . . . Lung squamous cell carcinoma QG-56 cell . REF100008 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.18 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF101055 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.18 ug/mL . . . Lung large cell carcinoma NCI-H460 cell . REF100609 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.18 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100444 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.18 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100473 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.18 uM . . . Lung adenocarcinoma A-549 cell . REF100574 DRG00003 Fluorouracil Half Maximal Infective Dose (ID50) = 0.18 uM/L . . . Lymphoblastic leukemia L1210 cell . REF100028 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.18±0.08 µM 72 h . . Neuroblastoma Kelly-WT cell "The cytotoxic effect of the peptide-drug conjugate on Kelly-WT cells was comparable to that of 9, but not as strong as the one of the native drug. Contrary to the other utilized substances, the antiproliferative action of the bioconjugate in wild-type and drug-resistant cells was nearly the same. In comparison with doxorubicin the cytotoxicity of 10 against Kelly-ADR cells was increased by a factor of 3 according to the obtained IC50 values. Even the unmodified dimer had roughly the same cytotoxic effect on Kelly-ADR cells as doxorubicin." REF00017 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.189 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100244 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.19 nM . . . Gastric adenocarcinoma MKN45 cell . REF100893 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 0.19 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100670 DRG00011 Doxorubicin Half Maximal Lethal dose (LD50) = 0.19 ug/mL . . . Prostate carcinoma PC-3 cell . REF102080 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.19 ug/mL . . . Glioma XF498 cell . REF100718 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.19 ug/mL . . . Breast adenocarcinoma MDA-MB-231 cell . REF100557 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.19 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100440 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.19 ug/mL . . . Lung adenocarcinoma A-549 cell . REF100440 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.19 ug/mL . . . Glioma XF498 cell . REF100403 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.19±0.06 nM 24 h . . Melanoma WM983A cell "The in vitro cytostatic effects of Dauα-MSH conjugates were compared with the PrestoBlue assay, which has a higher specificity and efficacy that of the previously used MTT assay, using the same six human melanoma cell lines used in the real-time qPCR assay. According to our results, free daunomycin exhibited the lowest IC50 values, and therefore the highest cytostatic effect, due to the fact that free daunomycin passively diffuses into cells. Our Dauα-MSH conjugates showed similar trends in the effectiveness of the tested cell lines. Conj2 and Conj4 resulted in IC50 values in the low µM range. A calculation of the targeting indices showed that compound Conj2 had an over 2-times higher targeting efficiency in most cell lines compared to the A2058 cell line. Interestingly, WM983A showed the lowest TI among the high-MC1R-expressing cell lines compared to A2058, and WM983B exhibited high TI regardless of the relatively low MC1R expression on the mRNA level. In the case of Conj4, the treatment resulted in the highest TIs with OCM-1 and WM983B cell lines." REF00294 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.198 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100214 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.2 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101449 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.2 nM . . . Anaplastic thyroid carcinoma ARO cell . REF100598 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 0.2 nM . . . Prostate carcinoma LNCaP cell . REF101637 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.2 ug/mL . . . Breast adenocarcinoma MDA-MB-231 cell . REF100677 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.2 ug/mL . . . Lung adenocarcinoma A-549 cell . REF100515 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.2 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100463 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.2 ug/mL . . . Gliosarcoma SF539 cell . REF100285 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.2 ug/mL . . . Glioma XF498 cell . REF100283 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.2 ug/mL . . . Melanoma SK-MEL-2 cell . REF100283 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.2 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100283 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.2 ug/mL . . . Lymphoma P388 cell . REF100273 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) = 0.2 ug/mL . . . Erythroleukemia HEL cell . REF100003 DRG00081 Cytarabine Half Maximal Effective Dosage (ED50) = 0.2 uM . . . Fibroblast sarcoma CCRF S-180 cell . REF100004 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.208 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100215 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.209 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100234 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.21 ug/mL . . . Colon cancer HT29 cell . REF100328 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.21 ug/mL . . . Skin squamous cell carcinoma A431 cell . REF100328 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 0.21 ug/mL . . . Ileocecal adenocarcinoma HCT-8 cell . REF100109 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.21±0.01 µM 72 h . . Ovarian endometrioid adenocarcinoma A2780 cell "To investigate the anticancer activity of the GnRH-III drug conjugates, cell viability studies have been performed on A2780 ovarian cancer and Panc-1 pancreatic cancer cells. The GnRH-R expression of these cell lines was determined by Western blot studies. In the case of the A2780 cells, a distinct band at 38 kDa could be detected which corresponds to the full-length human GnRH-R. In contrast, the signal intensity of the 38 kDa band was much lower for Panc-1 pancreatic cancer cells being in line with our previous results. Thus, the antiproliferative activity of the GnRH-drug conjugates was studied on high-GnRH-R-expressing A2780 cells and low-GnRH-R-expressing Panc-1 cells. Since the release of free Dau and PTX can be assumed, both drugs were used as controls. The cells were treated for either 24 h (Dau conjugates) or six hours (PTX compounds), followed by additional incubation with fresh growth medium until 72 h after treatment initiation. The obtained results reveal, on the one hand, that the non-cleavable linker-containing conjugates possess a reduced anticancer activity in comparison to the cleavable conjugates and, on the other hand, that the activity of the all GnRH-III-drug conjugates was substantially reduced compared to the free drug. Moreover, all compounds displayed a lower biological activity on Panc-1 cells than on A2780. In the case of the cleavable GnRH-III-Dau conjugates, the IC50 values varied between 2.8511.18 M on A2780 cells, whereby the best activity was obtained for compound 13 (2.85 M) which contained the cathepsin B-cleavage site Val-Ala and the GnRH-III-[2δHis-3D-Tic-4Lys(Bu)] peptide carrier. Apart from that, the IC50 values of the cleavable PTX conjugates on A2780 cells are in the same sub-micromolar range and vary between 0.510.77 M, while the activity of these conjugates was approximately 10 times lower on Panc-1 cells (5.038.15 M)." REF00219 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 0.21±0.03 µM 48 h . . Colon carcinoma HCT 116 cell "MTT assay was preformed to measure the in vitro cytotoxicities of the compounds against cancer cells (HCT-116, SGC-7901, MCF-7, HCT-116/CPT, SGC-7901/CPT and MCF-7/C4) and benign cells (NCM460, GES-1 and LO2). As present in Table 1, all the peptides (Kb-C01, 0207) exhibited certain selective anticancer activities, which are comparable to their parent counterpart KM8-Aib. The target PDCs (Kb-CC01, 0207) were further obtained by coupling the peptides with CPT, displaying markedly improved antiproliferative activities and selectivities against cancer cell lines over CPT. Studies have revealed that cancer cell membranes are negatively charged due to the presence of substantial amounts of acid phospholipids. Therefore, positively charged CAPs are capable of binding to cancer cell surface through electrostatic interactions, making them specific to cancer cells. In this project, since the PDCs were composed of CAP KM8-Aib and CPT, they potentially inherited the antineoplastic activities of KM8-Aib against cancer cells, as well as low toxicities to non-malignant cells." REF00278 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 0.21±0.04 µM 48 h . . Breast adenocarcinoma SK-BR-3 cell "The cytotoxicity of conjugates was evaluated on cell lines with different expression levels of HER2. The results showed that among all conjugates with a single CPT molecule (I-1 to I-3), I-1 was the most cytotoxic against three HER2-positive cell lines (SK-BR-3, NCI-N87, and SK-OV-3 cells), and the calculated IC50 values for the three cells were 1.47 0.54, 3.29 0.67, and 4.29 1.11 µM, respectively. Similarly, among all conjugates with two CPT molecules (I-4 to I-6), I-4 showed the highest cytotoxicity toward HER2-positive cells, and the IC50 values for SK-BR-3, NCI-N87, and SK-OV-3 cells were 0.12 0.07, 1.78 0.47, and 1.27 0.38 µM, respectively. The activity of I-4 against SK-BR-3 cells was also slightly better than that of the positive control CPT (IC50 = 0.21 0.04 µM). The cytotoxicity of I-1 and I-4 against HER2-negative MDA-MB-231 cells was comparatively lower (calculated IC50s were 7.60 1.23 and 7.72 0.92 µM, respectively). In contrast, CPT itself showed higher cytotoxicity against MDA-MB-231 (IC50 = 1.06 0.42 µM), indicating that conjugates showed higher specificity in cell targeting. Furthermore, the cytotoxicity of I-1 and I-4 against normal cells MCF-10A (IC50 = 23.90 1.58 and 17.14 2.42 µM, respectively) was significantly lower than that of CPT alone (2.58 0.77 µM). Based on these results, I-1 and I-4 were selected for subsequent biological evaluation." REF00244 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.22 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF101486 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.22 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100614 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.23 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF101972 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.23 ug/mL . . . Glioblastoma SF-295 cell . REF101910 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.23 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100187 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 0.23 ug/mL . . . Colon cancer HT29 cell . REF100871 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 0.23 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102150 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 0.23 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF102032 DRG00003 Fluorouracil Half Maximal Infective Dose (ID50) = 0.23 uM/L . . . Lymphoblastic leukemia L1210 cell . REF100028 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 0.24 nM . . . Invasive breast carcinoma ZR-75-1 cell . REF100538 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.24 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100965 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.24 ug/mL . . . Prostate carcinoma PC-3 cell . REF100595 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.24 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100425 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.24 ug/mL . . . Breast adenocarcinoma MDA-MB-231 cell . REF100328 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 0.24 ug/mL . . . Melanoma B16 cell . REF102014 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.241 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100357 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.25 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF101378 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.25 ug/mL . . . Glioblastoma SF-295 cell . REF100705 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.25 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100424 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 0.26 ng/mL . . . Anaplastic thyroid carcinoma SW-1736 cell . REF100089 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.26 ug/mL . . . Chronic myeloid leukemia K562 cell . REF101209 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 0.26±0.06 µM 48 h . . Breast adenocarcinoma SK-BR-3 cell "To evaluated the in vitro anti-tumor activity of the conjugates, HER2-positive SK-BR-3, NCI-N87, HER2-negative MDA-MB-231 and normal MCF-10A cells were selected. As shown in Table 2, nearly all conjugates exhibited obvious anti-proliferation activity against SK-BR-3 cells, while most of the conjugates, except for Z6 and Z9, demonstrated different degrees of inhibitory activity on NCI-N87 cells. Taken together, Z8 and Z11 exhibited superior anti-tumor activity. The antiproliferative activity of Z8 against NCI-N87 cells (IC50 = 1.91 0.71 µM) was comparable to that of CPT (IC50 = 2.10 1.34 µM), while the antiproliferative activity of Z11 against SK-BR-3 cells (IC50 = 0.41 0.13 µM) was comparable to that of CPT (IC50 = 0.26 0.06 µM). Additionally, the IC50 values of these two conjugates against MDA-MB-231 and MCF-10A cells were significantly increased, showing their ability to selectively inhibit tumor cells. Based on the above results, Z8 and Z11, which exhibited better activity and apparent selectivity, were selected for subsequent studies." REF00312 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 0.27 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101004 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.27 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100952 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.27 ug/mL . . . Colon cancer HT29 cell . REF101054 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.27 ug/mL . . . Lymphoma P388 cell . REF100142 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.28 ng/ml . . . Cutaneous melanoma SK-MEL-5 cell . REF100192 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.28 ug/mL . . . Prostate carcinoma PC-3 cell . REF100889 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.28 ug/mL . . . Cervical squamous cell carcinoma C-33-A cell . REF100860 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.28 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100469 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.286 ug/mL . . . Colon carcinoma HCT 116 cell . REF100858 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.287 ug/mL . . . Prostate carcinoma PC-3 cell . REF100220 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.29 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100701 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.29 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101131 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.29 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100388 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 0.29 ug/mL . . . Lung adenocarcinoma NCI-H23 cell . REF100572 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 0.3 nM . . . Endocervical adenocarcinoma HeLa cell . REF101700 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.3 ug/mL . . . Renal carcinoma UO-31 cell . REF102000 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.3 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100376 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) = 0.3 ug/mL . . . Erythroleukemia HEL cell . REF100003 DRG00010 Daunorubicin Half Maximal Effective Dosage (ED50) = 0.3 uM . . . Lymphoblastic leukemia L1210 cell . REF100129 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.31 ug/mL . . . Gingival squamous cell carcinoma Ca9-22 cell . REF101055 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 0.31 ug/mL . . . Acute monocytic leukemia U-937 cell . REF102013 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 0.32 nM . . . Glioblastoma LN-229 cell . REF101708 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 0.32 nM . . . Hepatocellular carcinoma Huh-7 cell . REF101708 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.32 nM . . . Thigh metastasis of melanoma WM 266-4 cell . REF101758 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 0.32 ug/mL . . . Lymphoblastic leukemia L1210 cell . REF102028 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.32 ug/mL . . . Lung adenocarcinoma A-549 cell . REF100793 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.32 ug/mL . . . Colon adenocarcinoma DLD-1 cell . REF100328 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 0.32 ug/mL . . . Colon adenocarcinoma Caco-2 cell . REF100871 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 0.32 ug/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102014 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.329 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100184 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.33 ug/mL . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100889 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.33 ug/mL . . . Lung adenocarcinoma A-549 cell . REF100860 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.33±0.05 µM 24 h . . Melanoma WM983B cell "The in vitro cytostatic effects of Dauα-MSH conjugates were compared with the PrestoBlue assay, which has a higher specificity and efficacy that of the previously used MTT assay, using the same six human melanoma cell lines used in the real-time qPCR assay. According to our results, free daunomycin exhibited the lowest IC50 values, and therefore the highest cytostatic effect, due to the fact that free daunomycin passively diffuses into cells. Our Dauα-MSH conjugates showed similar trends in the effectiveness of the tested cell lines. Conj2 and Conj4 resulted in IC50 values in the low µM range. A calculation of the targeting indices showed that compound Conj2 had an over 2-times higher targeting efficiency in most cell lines compared to the A2058 cell line. Interestingly, WM983A showed the lowest TI among the high-MC1R-expressing cell lines compared to A2058, and WM983B exhibited high TI regardless of the relatively low MC1R expression on the mRNA level. In the case of Conj4, the treatment resulted in the highest TIs with OCM-1 and WM983B cell lines." REF00294 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.339 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100300 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 0.34 ug/mL . . . Multiple myeloma IM-9 cell . REF102052 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.34 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100793 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 0.34 ug/mL . . . Colon carcinoma KM-20L2 cell . REF100062 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.35 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100901 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.35 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100479 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.36 pg/mL . . . Lung large cell carcinoma NCI-H460 cell . REF100457 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.366 ng/ml . . . Renal carcinoma A498 cell . REF100224 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.38 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100893 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.38 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100605 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 0.38±0.11 µM 48 h . . Breast adenocarcinoma SK-BR-3 cell "HER2 positive SK-BR-3, NCIN87 and SK-OV-3 cells, and HER2 negative MDA-MB-231 and MCF-10A cells were selected to determine the cell activity of the target conjugates. From Table 3, most conjugates showed certain cytotoxicity to three HER2 positive cell lines. Among the three connection sites (S1S3), compounds 1, 4, and 7 with the first connection mode showed better activity. In the three HER2 positive SK-BR-3, NCIN87 and SK-OV-3 cells, conjugate 4 exhibited superior activity (IC50s of 0.53 0.17 µM, 1.58 0.41 µM, 2.50 0.78 µM, respectively), which almost equal to that of CPT (IC50s of 0.38 0.11 µM, 2.07 0.67 µM, 4.07 1.82 µM, respectively). The activity of conjugate 4 on HER2 positive cells was superior to that of conjugate 1 and 7. In MDA-MB-231 and MCF-10A cells, IC50s of conjugate 4 were 18.44 2.09 µM and 17.76 1.35 µM, respectively, which showed great tumor cell selectivity. Based on the above, conjugate 4 with better in vitro antitumor activity was selected for subsequent biological study." REF00288 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 0.39 nM 72 h . . Cutaneous melanoma SORT1-positive SKMEL28 cell "SORT1-positive SK-MEL-28 and B16-F10 melanoma cells were selected for testing the anti-proliferative effect of docetaxel and TH1902. When TH1902 biological effects were monitored, the half-maximal inhibitory concentration (IC50) of TH1902 was similar to that of docetaxel, averaging 0.38 vs. 0.39 nM, respectively, in human SK-MEL-28 cells, and 2.57 vs. 1.72 nM in murine B16-F10 cells." REF00303 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.39 ug/mL . . . Lymphoma P388 cell . REF102103 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.39 ug/mL . . . Lung adenocarcinoma A-549 cell . REF101916 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.39 ug/mL . . . Breast adenocarcinoma MDA-MB-231 cell . REF100613 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 0.39 ug/mL . . . Pancreatic ductal adenocarcinoma BxPC-3 cell . REF102194 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.4 nM . . . Lymphoblastic leukemia L1210 cell . REF100952 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.4 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF101804 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.4 ug/mL . . . Prostate carcinoma DU145 cell . REF101705 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.4 ug/mL . . . Normal LLC-PK1 cell . REF101363 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.4 ug/mL . . . Laryngeal carcinoma HEp-2 cell . REF100809 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.41 ug/mL . . . Glioblastoma SF-295 cell . REF100916 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.414 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101348 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.42 ug/mL . . . Lung adenocarcinoma A-549 cell . REF100557 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.43 nM . . . Prostate carcinoma PC-3 cell . REF100975 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 0.43 nM . . . Small cell lung carcinoma PC-6 cell . REF102180 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.43 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100757 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.44 nM . . . Hepatoblastoma Hep-G2 cell . REF101094 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.44±0.11 µM . . . Human papillomavirus-related cervical adenocarcinoma L-02 cell "As shown in Fig.4a, free DOX had poor selectivity between tumor and normal cells, so there was not too much difference in its cytotoxicities against HepG2 cell line (IC501.030.13µM) and L-O2 cell line (IC500.440.11µM)." REF00079 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.45 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100860 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.45 ug/mL . . . Chronic myeloid leukemia K562 cell . REF100614 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.45 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100382 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.457 ug/mL . . . Acute myeloid leukemia HL-60 cell . REF100858 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.46 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100557 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.47 ug/mL . . . Amelanotic melanoma MDA-MB-435 cell . REF100595 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.47 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF101214 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.48 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100550 DRG00010 Daunorubicin Half Maximal Effective Dosage (ED50) = 0.48 uM . . . Lymphoblastic leukemia L1210 cell . REF102004 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 0.5 ng/mL . . . Normal MT4 cell . REF102098 DRG00038 Monomethyl auristatin E Half Maximal growth inhibition concentration (GI50) = 0.5 nM 3 days . . Ovarian serous adenocarcinoma OVCAR-3 cell "GI50s are summarised in Table 1. Our cell panel consisted of LHRH receptor-positive (OVCAR-3) and receptor-negative (SK-OV-3) ovarian cancer cell lines used in Zoptarelin doxorubicin's preclinical development studies. Non-cancerous human ovarian (H-6036) and lung fibroblast (MRC-5) cell lines were also included for selectivity comparison. Paclitaxel, a first-line chemotherapeutic drug used for ovarian cancer, was observed to be highly cytotoxic against all cell lines, including non-cancerous ovarian and human fibroblasts (GI50s 15nM). Unsurprisingly, common and serious side-effects experienced by more than 50% patients dosed with this drug included anaemia, neutropenia, peripheral neuropathy, nausea, vomiting, myalgia, arthralgia and alopecia. Similarly, doxorubicin was also shown to be non-specific towards all the cell lines (GI50s 60311nM), below the reported average 631nM GI50 in a study involving 39 cancer cell lines. It is noteworthy that doxorubicin exhibited moderate GI50s of 311 and 218nM against OVCAR-3 and SK-OV-3, respectively, supporting earlier in vitro data. Tubulin binder MMAE was found to be ultra-toxic against all cell lines (GI50s 0.51.1nM), supporting the findings from an earlier report. It is therefore unsurprising that MMAE has never been approved as a drug on its own. The LHRH analog and carrier peptide, D-Cys6-LHRH, was inactive against all cell lines (GI50s >50,000nM)." REF00310 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 0.5 nM 48 h . . Lung adenocarcinoma H1975 cell "DTX-P7 showed comparable effect with DTX in the two cell lines. IC50 values of DTX and DTX-P7 for A549 cells were 1.11 nM and 11.4 nM, respectively, while IC50 values of DTX and DTX-P7 for H1975 cells were 0.50 nM and 0.62 nM, respectively." REF00222 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.5 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101520 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.5 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF101382 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.5 nM . . . Invasive breast carcinoma MCF-7 cell . REF100368 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 0.5 nM . . . Prostate carcinoma PC-3 cell . REF101741 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 0.5 ug/mL . . . Acute monocytic leukemia U-937 cell . REF102052 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 0.5 ug/mL . . . Bladder carcinoma T24 cell . REF102050 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.5 ug/mL . . . Colon cancer HT29 cell . REF100277 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 0.5 ug/mL . . . Bladder carcinoma T24 cell . REF102014 DRG00221 Acyclovir Half Maximal Effective Concentration (EC50) = 0.5 ug/mL . . . Normal Vero cell . REF100070 DRG00221 Acyclovir Half Maximal Effective Dosage (ED50) = 0.5 uM . . . Normal Vero cell . REF102047 DRG00221 Acyclovir Half Maximal Infective Dose (ID50) = 0.5 uM . . . Normal Vero cell . REF102025 DRG00038 Monomethyl auristatin E Half Maximal Effective Concentration (EC50) = 0.50±0.03 nM 48 h . . Pancreatic ductal adenocarcinoma BxPC-3 (+) cells "Both NH2-PDC-1 and [natCu]PDC-1 exhibited integrin αvβ6-dependent cytotoxicity, only reducing cell viability of the αvβ6-positive cells. For [natCu]PDC-1 high cytotoxicity was observed in DX3puroβ6 (+) cells (EC50: 0.058 0.003 nM) with no observable cytotoxic effects in the DX3puro () cells, while free MMAE had almost equal cytotoxicity to both DX3puroβ6 (+) and DX3puro cells () (EC50: 0.140.15 nM). The pancreatic cells also showed αvβ6-dependent cytotoxicity for [natCu]PDC-1 (EC50: BxPC-3 65.1 10.6 nM) and required high concentrations of 250 nM for noticeable cytotoxic effects in the minimally integrin αvβ6-expressing MIA PaCa-2 cells. Again, free, non-targeted MMAE exhibited nondiscriminatory cytotoxicity among the pancreatic cells with an effective concentration range of EC50 = 0.160.5 nM. Peptides NH2-2 and [natCu]2 were not toxic to any cells." REF00272 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.51 ng/mL . . . Colon cancer HT29 cell . REF100240 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.52 nM . . . Normal MRC5 cell . REF101795 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.52 ug/mL . . . Lung adenocarcinoma A-549 cell . REF100657 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.52 ug/mL . . . Colon adenocarcinoma LoVo cell . REF100303 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.53 pg/mL . . . Astrocytoma SF268 cell . REF100457 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.53 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100328 DRG00296 Zidovudine Half Maximal Infective Dose (ID50) = 0.53 ug/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100011 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 0.53±0.21 µM 48 h . . Breast adenocarcinoma MDA-MB-231 cell "HER2 positive SK-BR-3, NCIN87 and SK-OV-3 cells, and HER2 negative MDA-MB-231 and MCF-10A cells were selected to determine the cell activity of the target conjugates. From Table 3, most conjugates showed certain cytotoxicity to three HER2 positive cell lines. Among the three connection sites (S1S3), compounds 1, 4, and 7 with the first connection mode showed better activity. In the three HER2 positive SK-BR-3, NCIN87 and SK-OV-3 cells, conjugate 4 exhibited superior activity (IC50s of 0.53 0.17 µM, 1.58 0.41 µM, 2.50 0.78 µM, respectively), which almost equal to that of CPT (IC50s of 0.38 0.11 µM, 2.07 0.67 µM, 4.07 1.82 µM, respectively). The activity of conjugate 4 on HER2 positive cells was superior to that of conjugate 1 and 7. In MDA-MB-231 and MCF-10A cells, IC50s of conjugate 4 were 18.44 2.09 µM and 17.76 1.35 µM, respectively, which showed great tumor cell selectivity. Based on the above, conjugate 4 with better in vitro antitumor activity was selected for subsequent biological study." REF00288 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.54 ug/mL . . . Chronic myeloid leukemia K562 cell . REF101755 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.54 ug/mL . . . Melanoma B16 cell . REF100271 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 0.54 uM . . . Colon adenocarcinoma HCT 15 cell . REF100344 DRG00023 Tesaglitazar Ketone level = 0.55 mM/L Every day 2.5 μM db/db mice model. . . "Whereas in the vehicle/untreated mice, the HbA1C values increased by approximately 2%, a graduated reduced increase was seen for [F7, P34]-NPY (2), peptide conjugate (3), and tesa (Figure 8A). Body temperature, which decreased to 35 C in the vehicle/untreated db/db controls, was normalized to 36 C in all of the treated mice including the mice treated with [F7, P34]-NPY (2) (Figure 8B). Treatment with tesa and tesa-NPY (3) led to normalization of the plasma concentration of ketone bodies and adiponectin, whereas [F7, P34]-NPY (2) and vehicle/untreated showed no effect (Figure 8C/E). Treatment had no major influence on the insulin and Mcp-1 levels (Figure 8D/G). The serum leptin concentration was reduced in the mice treated with tesa, whereas no reduction was detectable in all of the other treated mice (Figure 8F)." REF00088 DRG00023 Tesaglitazar Triglycerides level = 0.55 mmol/L Every day 2.5 μM db/db mice model. . . "The influence of tesa, tesa-NPY (3), and [F7, P34]-NPY (2) on the plasma lipids was also analyzed (Figure 9). The vehicle/untreated db/db mice showed elevated levels of triglycerides and free fatty acids (FFA) compared to the lean C57BL/6N mice. Treatment with tesa and tesa-NPY (3) led to a normalization of the triglycerides, FFA, whereas [F7, P34]-NPY (2) and vehicle/untreated had no influence on the lipid metabolism (Figure 9A/B). The cholesterol levels were unchanged by any treatment as these levels were also comparable in the untreated db/db mice compared to the lean mice (Figure 9C)." REF00088 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 0.55 nM . . . Colon carcinoma HCT 116 cell . REF102180 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.55 ug/mL . . . Colon adenocarcinoma LoVo cell . REF100790 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.55 ug/mL . . . Lymphoma P388 cell . REF100252 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.56 ng/ml . . . Colon cancer HT29 cell . REF100192 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.56±0.05 µM 24 h . . Cutaneous melanoma OCM-3 cell "The in vitro cytostatic effects of Dauα-MSH conjugates were compared with the PrestoBlue assay, which has a higher specificity and efficacy that of the previously used MTT assay, using the same six human melanoma cell lines used in the real-time qPCR assay. According to our results, free daunomycin exhibited the lowest IC50 values, and therefore the highest cytostatic effect, due to the fact that free daunomycin passively diffuses into cells. Our Dauα-MSH conjugates showed similar trends in the effectiveness of the tested cell lines. Conj2 and Conj4 resulted in IC50 values in the low µM range. A calculation of the targeting indices showed that compound Conj2 had an over 2-times higher targeting efficiency in most cell lines compared to the A2058 cell line. Interestingly, WM983A showed the lowest TI among the high-MC1R-expressing cell lines compared to A2058, and WM983B exhibited high TI regardless of the relatively low MC1R expression on the mRNA level. In the case of Conj4, the treatment resulted in the highest TIs with OCM-1 and WM983B cell lines." REF00294 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.57 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100811 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.57 ug/mL . . . Colon adenocarcinoma DLD-1 cell . REF100424 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.58 nM . . . Lymphoblastic leukemia L1210 cell . REF100368 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.58 ug/mL . . . Colon adenocarcinoma LoVo cell . REF100281 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.58 uM . . . Lymphoblastic leukemia L1210 cell . REF100130 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.59 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100820 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 0.6 ng/mL . . . Lung large cell carcinoma NCI-H460 cell . REF100062 DRG00038 Monomethyl auristatin E Half Maximal growth inhibition concentration (GI50) = 0.6 nM 3 days . . Normal H-6036 cell "GI50s are summarised in Table 1. Our cell panel consisted of LHRH receptor-positive (OVCAR-3) and receptor-negative (SK-OV-3) ovarian cancer cell lines used in Zoptarelin doxorubicin's preclinical development studies. Non-cancerous human ovarian (H-6036) and lung fibroblast (MRC-5) cell lines were also included for selectivity comparison. Paclitaxel, a first-line chemotherapeutic drug used for ovarian cancer, was observed to be highly cytotoxic against all cell lines, including non-cancerous ovarian and human fibroblasts (GI50s 15nM). Unsurprisingly, common and serious side-effects experienced by more than 50% patients dosed with this drug included anaemia, neutropenia, peripheral neuropathy, nausea, vomiting, myalgia, arthralgia and alopecia. Similarly, doxorubicin was also shown to be non-specific towards all the cell lines (GI50s 60311nM), below the reported average 631nM GI50 in a study involving 39 cancer cell lines. It is noteworthy that doxorubicin exhibited moderate GI50s of 311 and 218nM against OVCAR-3 and SK-OV-3, respectively, supporting earlier in vitro data. Tubulin binder MMAE was found to be ultra-toxic against all cell lines (GI50s 0.51.1nM), supporting the findings from an earlier report. It is therefore unsurprising that MMAE has never been approved as a drug on its own. The LHRH analog and carrier peptide, D-Cys6-LHRH, was inactive against all cell lines (GI50s >50,000nM)." REF00310 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.6 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101885 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.6 nM . . . Hepatocellular carcinoma SNU-398 cell . REF101694 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.6 nM . . . Invasive breast carcinoma MCF-7 cell . REF100478 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.61 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101214 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.61 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100782 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.62 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100973 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.62 pg/mL . . . Invasive breast carcinoma MCF-7 cell . REF100457 DRG00221 Acyclovir Half Maximal Infective Dose (ID50) = 0.62 ug/mL . . . Malignant neoplasms of the mouse mammary gland FM3A cell . REF100013 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.63 ug/mL . . . Lung adenocarcinoma A-549 cell . REF100901 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 0.65 ng/mL . . . Hypopharyngeal squamous cell carcinoma FaDu cell . REF100089 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.65 pg/mL . . . Invasive breast carcinoma MCF-7 cell . REF100420 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.65 ug/mL . . . Colon carcinoma HCT 116 cell . REF100820 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.65 ug/mL . . . Normal LLC-PK1 cell . REF100526 DRG00107 Betulinic acid Half Maximal Effective Dosage (ED50) = 0.65 ug/mL . . . T acute lymphoblastic leukemia Jurkat cell . REF102114 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 0.65±0.03 µM 48 h . . Gastric carcinoma SGC-7901 cell "MTT assay was preformed to measure the in vitro cytotoxicities of the compounds against cancer cells (HCT-116, SGC-7901, MCF-7, HCT-116/CPT, SGC-7901/CPT and MCF-7/C4) and benign cells (NCM460, GES-1 and LO2). As present in Table 1, all the peptides (Kb-C01, 0207) exhibited certain selective anticancer activities, which are comparable to their parent counterpart KM8-Aib. The target PDCs (Kb-CC01, 0207) were further obtained by coupling the peptides with CPT, displaying markedly improved antiproliferative activities and selectivities against cancer cell lines over CPT. Studies have revealed that cancer cell membranes are negatively charged due to the presence of substantial amounts of acid phospholipids. Therefore, positively charged CAPs are capable of binding to cancer cell surface through electrostatic interactions, making them specific to cancer cells. In this project, since the PDCs were composed of CAP KM8-Aib and CPT, they potentially inherited the antineoplastic activities of KM8-Aib against cancer cells, as well as low toxicities to non-malignant cells." REF00278 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.65±0.20 µM 48 h . . Glioblastoma U87 cell "DOX showed strong in vitro cytotoxicity against all four kinds of cells without tumor selectivity, with IC50 values of 1.65 0.20 M (U87), 1.58 0.19 M (HepG2), 3.55 0.21 M (A549), and 1.29 0.18 M (LO2), respectively" REF00315 DRG00010 Daunorubicin Half Maximal Effective Dosage (ED50) = 0.66 uM . . . Lymphoblastic leukemia L1210 cell . REF100169 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.67 ug/mL . . . Thymoma EL4 cell . REF102103 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 0.68±0.04 µM 48 h . . Invasive breast carcinoma MCF-7 cell "MTT assay was preformed to measure the in vitro cytotoxicities of the compounds against cancer cells (HCT-116, SGC-7901, MCF-7, HCT-116/CPT, SGC-7901/CPT and MCF-7/C4) and benign cells (NCM460, GES-1 and LO2). As present in Table 1, all the peptides (Kb-C01, 0207) exhibited certain selective anticancer activities, which are comparable to their parent counterpart KM8-Aib. The target PDCs (Kb-CC01, 0207) were further obtained by coupling the peptides with CPT, displaying markedly improved antiproliferative activities and selectivities against cancer cell lines over CPT. Studies have revealed that cancer cell membranes are negatively charged due to the presence of substantial amounts of acid phospholipids. Therefore, positively charged CAPs are capable of binding to cancer cell surface through electrostatic interactions, making them specific to cancer cells. In this project, since the PDCs were composed of CAP KM8-Aib and CPT, they potentially inherited the antineoplastic activities of KM8-Aib against cancer cells, as well as low toxicities to non-malignant cells." REF00278 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.69 ug/mL . . . Amelanotic melanoma MDA-MB-435 cell . REF100916 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.69 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100570 DRG00107 Betulinic acid Half Maximal Effective Dosage (ED50) = 0.69 ug/mL . . . Acute monocytic leukemia U-937 cell . REF102114 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 0.7 ng/mL . . . Normal MT4 cell . REF102058 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 0.7 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102058 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.7 nM . . . Invasive breast carcinoma MCF-7 cell . REF100602 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.7 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100537 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 0.7 nM . . . Normal MT4 cell . REF102068 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 0.7 ug/mL . . . Chronic myeloid leukemia K562 cell . REF101223 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.7 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100308 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 0.7 uM . . . Melanoma B16 cell . REF101996 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.71 nM . . . Chronic myeloid leukemia K562 cell . REF100998 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 0.71 nM . . . Ovarian adenocarcinoma A2780-1A9 cell . REF100568 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.71 ug/mL . . . Normal WI-38 cell . REF100570 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.72 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100820 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.73 ug/mL . . . Breast adenocarcinoma MDA-MB-231 cell . REF100440 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.73 ug/mL . . . Osteosarcoma MG-22A cell . REF100416 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 0.73 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100111 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.73±0.06 µM 24 h . . Amelanotic melanoma OCM-1 cell "The in vitro cytostatic effects of Dauα-MSH conjugates were compared with the PrestoBlue assay, which has a higher specificity and efficacy that of the previously used MTT assay, using the same six human melanoma cell lines used in the real-time qPCR assay. According to our results, free daunomycin exhibited the lowest IC50 values, and therefore the highest cytostatic effect, due to the fact that free daunomycin passively diffuses into cells. Our Dauα-MSH conjugates showed similar trends in the effectiveness of the tested cell lines. Conj2 and Conj4 resulted in IC50 values in the low µM range. A calculation of the targeting indices showed that compound Conj2 had an over 2-times higher targeting efficiency in most cell lines compared to the A2058 cell line. Interestingly, WM983A showed the lowest TI among the high-MC1R-expressing cell lines compared to A2058, and WM983B exhibited high TI regardless of the relatively low MC1R expression on the mRNA level. In the case of Conj4, the treatment resulted in the highest TIs with OCM-1 and WM983B cell lines." REF00294 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 0.75 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101614 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.75 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100607 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.75±0.01 µM 24 h . . Prostate carcinoma PC-3 cell "The cytostatic effect of the conjugates and the free peptides was evaluated on the three mentioned human cancer cell lines expressing GRP-R. The free Dau was used as a positive control for comparison purposes; it displays an IC50 in the high nanomolar range. Overall, the conjugates containing the LRRY spacer have a higher cytostatic effect than the ones with the GFLG spacer. L1, which has the original BBN (7-14) sequence, and L5, bearing a D-Phe in position 6 and the Sta13Leu14 bond at the C-terminus, shows the best activity in all three cell lines, with IC50 values in the low micromolar range. The Gly11/β-Ala11 and Leu13-Met14/Sta13-Nle14 substitutions, which led to a new BBN (6-14) peptide sequence, held by the conjugate L6, affect the activity only slightly. Contrarily, the two free peptides, bearing the sequences of L5 and L6, do not show any activity on any of the cell lines. The lack of toxicity of the conjugates on healthy cells was checked on MRC-5 human fibroblasts, proving that they are non-toxic on non-cancerous cells." REF00251 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.76 ug/mL . . . Normal WI-38 cell . REF100550 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.77 ug/mL . . . Normal MRC5 cell . REF100557 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 0.78 nM . . . Colon carcinoma HCT 116 cell . REF101669 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.79 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100405 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 0.8 ng/mL . . . Prostate carcinoma DU145 cell . REF102169 DRG00038 Monomethyl auristatin E Half Maximal growth inhibition concentration (GI50) = 0.8 nM 3 days . . Ovarian serous cystadenocarcinoma SK-OV-3 cell "GI50s are summarised in Table 1. Our cell panel consisted of LHRH receptor-positive (OVCAR-3) and receptor-negative (SK-OV-3) ovarian cancer cell lines used in Zoptarelin doxorubicin's preclinical development studies. Non-cancerous human ovarian (H-6036) and lung fibroblast (MRC-5) cell lines were also included for selectivity comparison. Paclitaxel, a first-line chemotherapeutic drug used for ovarian cancer, was observed to be highly cytotoxic against all cell lines, including non-cancerous ovarian and human fibroblasts (GI50s 15nM). Unsurprisingly, common and serious side-effects experienced by more than 50% patients dosed with this drug included anaemia, neutropenia, peripheral neuropathy, nausea, vomiting, myalgia, arthralgia and alopecia. Similarly, doxorubicin was also shown to be non-specific towards all the cell lines (GI50s 60311nM), below the reported average 631nM GI50 in a study involving 39 cancer cell lines. It is noteworthy that doxorubicin exhibited moderate GI50s of 311 and 218nM against OVCAR-3 and SK-OV-3, respectively, supporting earlier in vitro data. Tubulin binder MMAE was found to be ultra-toxic against all cell lines (GI50s 0.51.1nM), supporting the findings from an earlier report. It is therefore unsurprising that MMAE has never been approved as a drug on its own. The LHRH analog and carrier peptide, D-Cys6-LHRH, was inactive against all cell lines (GI50s >50,000nM)." REF00310 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.8 nM . . . Colon cancer HT29 cell . REF101782 DRG00122 Vinblastine Half Maximal Growth Inhibition (GI50) = 0.8 nM . . . Lung carcinoma SW1573 cell . REF101744 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 0.8 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF102496 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.8 pM . . . Invasive breast carcinoma MCF-7 cell . REF100406 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 0.8 ug/mL . . . Lung adenocarcinoma A-549 cell . REF101223 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.8 ug/mL . . . Breast ductal carcinoma BT-549 cell . REF100830 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.81±0.07 µM 24 h . . Breast adenocarcinoma MDA-MB-453 cell "The cytostatic effect of the conjugates and the free peptides was evaluated on the three mentioned human cancer cell lines expressing GRP-R. The free Dau was used as a positive control for comparison purposes; it displays an IC50 in the high nanomolar range. Overall, the conjugates containing the LRRY spacer have a higher cytostatic effect than the ones with the GFLG spacer. L1, which has the original BBN (7-14) sequence, and L5, bearing a D-Phe in position 6 and the Sta13Leu14 bond at the C-terminus, shows the best activity in all three cell lines, with IC50 values in the low micromolar range. The Gly11/β-Ala11 and Leu13-Met14/Sta13-Nle14 substitutions, which led to a new BBN (6-14) peptide sequence, held by the conjugate L6, affect the activity only slightly. Contrarily, the two free peptides, bearing the sequences of L5 and L6, do not show any activity on any of the cell lines. The lack of toxicity of the conjugates on healthy cells was checked on MRC-5 human fibroblasts, proving that they are non-toxic on non-cancerous cells." REF00251 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.82 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100927 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.85 pM . . . Astrocytoma SF268 cell . REF100406 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.85 ug/mL . . . Colon cancer HT29 cell . REF101378 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 0.86 pg/mL . . . Astrocytoma SF268 cell . REF100462 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 0.86 ug/mL . . . Astrocytoma SF268 cell . REF102113 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.87 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101183 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.899 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100733 DRG00221 Acyclovir Half Maximal Infective Dose (ID50) = 0.9 ng/mL . . . Acute monocytic leukemia MV4-11 cell . REF100013 DRG00122 Vinblastine Half Maximal Growth Inhibition (GI50) = 0.9 nM . . . Lung carcinoma SW1573 cell . REF101744 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 0.9 nM . . . Colon carcinoma HCT 116 cell . REF100072 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.9 ug/mL . . . Lymphoblastic leukemia L1210 cell . REF100216 DRG00012 Paclitaxel 90% Lethal Concentration (IC50) = 0.9 ug/mL . . . Ovarian mixed germ cell tumor PA-1 cell . REF100483 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 0.9 ug/mL . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF102070 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 0.90±0.06 µM 24 h . . Breast adenocarcinoma MDA-MB-231 cell "The cytostatic effect of the conjugates and the free peptides was evaluated on the three mentioned human cancer cell lines expressing GRP-R. The free Dau was used as a positive control for comparison purposes; it displays an IC50 in the high nanomolar range. Overall, the conjugates containing the LRRY spacer have a higher cytostatic effect than the ones with the GFLG spacer. L1, which has the original BBN (7-14) sequence, and L5, bearing a D-Phe in position 6 and the Sta13Leu14 bond at the C-terminus, shows the best activity in all three cell lines, with IC50 values in the low micromolar range. The Gly11/β-Ala11 and Leu13-Met14/Sta13-Nle14 substitutions, which led to a new BBN (6-14) peptide sequence, held by the conjugate L6, affect the activity only slightly. Contrarily, the two free peptides, bearing the sequences of L5 and L6, do not show any activity on any of the cell lines. The lack of toxicity of the conjugates on healthy cells was checked on MRC-5 human fibroblasts, proving that they are non-toxic on non-cancerous cells." REF00251 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.90±0.12 µM 72 h . . Invasive breast carcinoma MCF-7 cell The obtained IC50 values for 9 (6.73 2.44 µM) and 10 (3.66 0.77 µM) were higher than for doxorubicin (0.90 0.12 µM). REF00017 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 0.91 nM . . . Invasive breast carcinoma MCF-7 cell . REF100990 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 0.94 nM . . . Lung adenocarcinoma Calu-6 cell . REF100974 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 0.953 ug/ml . . . Invasive breast carcinoma MCF-7 cell . REF100455 DRG00107 Betulinic acid Half Maximal Effective Dosage (ED50) = 0.98 ug/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102114 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 0.988 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100300 DRG00081 Cytarabine Half Maximal Effective Dosage (ED50) = 0.99 uM . . . Mouse plasma cell myeloma MPC-11 cell . REF100029 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1 ng/mL . . . Melanoma B16 cell . REF100416 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1 ng/mL . . . Astrocytoma U-251MG cell . REF100363 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100363 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1 ng/mL . . . Melanoma LOX IMVI cell . REF100363 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101921 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 1 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100393 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Lung adenocarcinoma A-549 cell . REF101887 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Small cell lung carcinoma NCI-H69 cell . REF100917 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100751 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Renal adenocarcinoma ACHN cell . REF100506 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Endocervical adenocarcinoma HeLa cell . REF101563 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Stomach adenocarcinoma BGC-823 cell . REF101527 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101513 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101456 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101391 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 1 nM . . . Colon cancer HT29 cell . REF101121 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Colon adenocarcinoma SW48 cell . REF100763 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 1 nM . . . Ovarian adenocarcinoma A2780-1A9 cell . REF100549 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100533 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100472 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Prostate carcinoma PC-3 cell . REF100834 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Colon carcinoma HCT 116 cell . REF102466 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . B acute lymphoblastic leukemia RS4;11 cell . REF102450 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 1 nM . . . Prostate carcinoma PC-3 cell . REF102290 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Glioma A10 cell . REF101012 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1 nM . . . Melanoma B16 cell . REF100072 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1 ug/mL . . . Colon adenocarcinoma Caco-2 cell . REF100809 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1 ug/mL . . . Chronic myeloid leukemia K562 cell . REF100801 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1 ug/mL . . . Breast ductal carcinoma BT-549 cell . REF100426 DRG00003 Fluorouracil Half Maximal Infective Dose (ID50) = 1 uM . . . Lymphoblastic leukemia L1210 cell . REF100030 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.006 uM . . . Normal HEK293 cell . REF101968 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.01 mM . . . Acute monocytic leukemia MV4-11 cell . REF101294 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.01 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100224 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.01 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100784 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.01 uM . . . Endocervical adenocarcinoma HeLa cell . REF101044 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 1.01 uM . . . Normal NIH3T3 cell . REF100113 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 1.01 uM . . . Lung small cell carcinoma NCI-H526 cell . REF102323 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.02 uM . . . Endocervical adenocarcinoma HeLa cell . REF101604 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.02 uM . . . Lung adenocarcinoma A-549 cell . REF101032 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 1.02329 uM . . . Cutaneous melanoma SK-MEL-28 cell . REF102227 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 1.03 uM . . . Cutaneous melanoma SK-MEL-28 cell . REF102520 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.03 uM . . . Melanoma MEXF514 cell . REF100398 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.03±0.13 µM . . . Hepatoblastoma Hep-G2 cell "As shown in Fig. 4a, free DOX had poor selectivity between tumor and normal cells, so there was not too much difference in its cytotoxicities against HepG2 cell line (IC50 1.030.13 µM) and L-O2 cell line (IC50 0.440.11 µM). " REF00079 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.04 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100291 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.04 uM . . . Lung adenocarcinoma A-549 cell . REF101261 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.05 ug/mL . . . Breast adenocarcinoma MDA-MB-231 cell . REF100793 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.05 uM . . . Invasive breast carcinoma MCF-7 cell . REF101799 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.05 uM . . . Hepatoblastoma Hep-G2 cell . REF101298 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 1.05 uM . . . Normal R1 cell . REF100356 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.054 uM . . . Invasive breast carcinoma MCF-7 cell . REF101353 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.06 uM . . . Normal HEK293 cell . REF101207 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 1.06 uM . . . Melanoma SK-MEL-2 cell . REF101165 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.06 uM . . . Colon cancer HT29 cell . REF101024 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.06±0.42 µM 48 h . . Breast adenocarcinoma MDA-MB-231 cell "The cytotoxicity of conjugates was evaluated on cell lines with different expression levels of HER2. The results showed that among all conjugates with a single CPT molecule (I-1 to I-3), I-1 was the most cytotoxic against three HER2-positive cell lines (SK-BR-3, NCI-N87, and SK-OV-3 cells), and the calculated IC50 values for the three cells were 1.47 0.54, 3.29 0.67, and 4.29 1.11 µM, respectively. Similarly, among all conjugates with two CPT molecules (I-4 to I-6), I-4 showed the highest cytotoxicity toward HER2-positive cells, and the IC50 values for SK-BR-3, NCI-N87, and SK-OV-3 cells were 0.12 0.07, 1.78 0.47, and 1.27 0.38 µM, respectively. The activity of I-4 against SK-BR-3 cells was also slightly better than that of the positive control CPT (IC50 = 0.21 0.04 µM). The cytotoxicity of I-1 and I-4 against HER2-negative MDA-MB-231 cells was comparatively lower (calculated IC50s were 7.60 1.23 and 7.72 0.92 µM, respectively). In contrast, CPT itself showed higher cytotoxicity against MDA-MB-231 (IC50 = 1.06 0.42 µM), indicating that conjugates showed higher specificity in cell targeting. Furthermore, the cytotoxicity of I-1 and I-4 against normal cells MCF-10A (IC50 = 23.90 1.58 and 17.14 2.42 µM, respectively) was significantly lower than that of CPT alone (2.58 0.77 µM). Based on these results, I-1 and I-4 were selected for subsequent biological evaluation." REF00244 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.07 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101526 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.07 uM . . . Acute monocytic leukemia U-937 cell . REF101099 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.07 uM . . . Colon cancer HT29 cell . REF100775 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.07 uM . . . Prostate carcinoma PC-3 cell . REF101713 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.07 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101623 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1.07 uM . . . Invasive breast carcinoma MCF-7 cell . REF100997 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.08 uM . . . Hepatocellular carcinoma SMMC-7721 cell . REF101670 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.08 uM . . . Endocervical adenocarcinoma HeLa cell . REF100929 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.08 uM . . . Colon adenocarcinoma HCT 15 cell . REF101362 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.089 uM . . . Endocervical adenocarcinoma HeLa cell . REF101508 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.1 ng/ml . . . Renal carcinoma A498 cell . REF101935 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.1 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100295 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.1 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100201 DRG00038 Monomethyl auristatin E Half Maximal growth inhibition concentration (GI50) = 1.1 nM 3 days . . Normal MRC-5 cell "GI50s are summarised in Table 1. Our cell panel consisted of LHRH receptor-positive (OVCAR-3) and receptor-negative (SK-OV-3) ovarian cancer cell lines used in Zoptarelin doxorubicin's preclinical development studies. Non-cancerous human ovarian (H-6036) and lung fibroblast (MRC-5) cell lines were also included for selectivity comparison. Paclitaxel, a first-line chemotherapeutic drug used for ovarian cancer, was observed to be highly cytotoxic against all cell lines, including non-cancerous ovarian and human fibroblasts (GI50s 15nM). Unsurprisingly, common and serious side-effects experienced by more than 50% patients dosed with this drug included anaemia, neutropenia, peripheral neuropathy, nausea, vomiting, myalgia, arthralgia and alopecia. Similarly, doxorubicin was also shown to be non-specific towards all the cell lines (GI50s 60311nM), below the reported average 631nM GI50 in a study involving 39 cancer cell lines. It is noteworthy that doxorubicin exhibited moderate GI50s of 311 and 218nM against OVCAR-3 and SK-OV-3, respectively, supporting earlier in vitro data. Tubulin binder MMAE was found to be ultra-toxic against all cell lines (GI50s 0.51.1nM), supporting the findings from an earlier report. It is therefore unsurprising that MMAE has never been approved as a drug on its own. The LHRH analog and carrier peptide, D-Cys6-LHRH, was inactive against all cell lines (GI50s >50,000nM)." REF00310 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.1 nM . . . Endocervical adenocarcinoma HeLa cell . REF101526 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.1 nM . . . Bladder carcinoma SW780 cell . REF101115 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.1 nM . . . Colon carcinoma HCT 116 cell . REF100744 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.1 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100668 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1.1 nM . . . Invasive breast carcinoma MCF-7 cell . REF100289 DRG00221 Acyclovir Half Maximal Infective Dose (ID50) = 1.1 nM . . . Normal Vero cell . REF102024 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 1.1 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF102113 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.1 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102350 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.1 uM . . . Endocervical adenocarcinoma HeLa cell . REF100841 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.1 uM . . . Invasive breast carcinoma MCF-7 cell . REF100760 DRG00011 Doxorubicin Half Maximal Lethal dose (LD50) = 1.1 uM . . . Acute myeloid leukemia HL-60 cell . REF102126 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.1 uM . . . Invasive breast carcinoma MCF-7 cell . REF101814 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 1.1 uM . . . Chronic myeloid leukemia K562 cell . REF101499 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.1 uM . . . Chronic myeloid leukemia K562 cell . REF101361 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.1 uM . . . Colon cancer HT29 cell . REF100946 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.1 uM . . . Neuroblastoma SK-N-SH cell . REF100869 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.1 uM . . . Breast adenocarcinoma SK-BR-3 cell . REF100409 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 1.1 uM . . . Neuroblastoma SK-N-AS cell . REF100967 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 1.1 uM . . . Colon adenocarcinoma Caco-2 cell . REF100850 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 1.1 uM . . . Invasive breast carcinoma MCF-7 cell . REF101450 DRG00221 Acyclovir Half Maximal Effective Concentration (EC50) = 1.1 uM . . . Erythroleukemia HEL cell . REF100069 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 1.11 nM 48 h . . Lung adenocarcinoma A-549 cell "DTX-P7 showed comparable effect with DTX in the two cell lines. IC50 values of DTX and DTX-P7 for A549 cells were 1.11 nM and 11.4 nM, respectively, while IC50 values of DTX and DTX-P7 for H1975 cells were 0.50 nM and 0.62 nM, respectively." REF00222 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.117 uM . . . Invasive breast carcinoma MCF-7 cell . REF101508 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.12 uM . . . Hepatoblastoma Hep-G2 cell . REF101839 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.12 uM . . . Endocervical adenocarcinoma HeLa cell . REF101029 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.12±0.11 µM 48 h . . Normal NCM460 cell "MTT assay was preformed to measure the in vitro cytotoxicities of the compounds against cancer cells (HCT-116, SGC-7901, MCF-7, HCT-116/CPT, SGC-7901/CPT and MCF-7/C4) and benign cells (NCM460, GES-1 and LO2). As present in Table 1, all the peptides (Kb-C01, 0207) exhibited certain selective anticancer activities, which are comparable to their parent counterpart KM8-Aib. The target PDCs (Kb-CC01, 0207) were further obtained by coupling the peptides with CPT, displaying markedly improved antiproliferative activities and selectivities against cancer cell lines over CPT. Studies have revealed that cancer cell membranes are negatively charged due to the presence of substantial amounts of acid phospholipids. Therefore, positively charged CAPs are capable of binding to cancer cell surface through electrostatic interactions, making them specific to cancer cells. In this project, since the PDCs were composed of CAP KM8-Aib and CPT, they potentially inherited the antineoplastic activities of KM8-Aib against cancer cells, as well as low toxicities to non-malignant cells." REF00278 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.13 nM . . . Acute myeloid leukemia HL-60 cell . REF100815 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.15 uM . . . Colon cancer HT29 cell . REF100737 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.16 uM . . . Lung adenocarcinoma A-549 cell . REF102368 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.16 uM . . . Chronic myeloid leukemia K562 cell . REF100722 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.17 uM . . . Endocervical adenocarcinoma HeLa cell . REF101949 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 1.17 uM . . . Lung adenocarcinoma A-549 cell . REF101385 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.17 uM . . . Invasive breast carcinoma MCF-7 cell . REF101724 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.172 uM . . . Invasive breast carcinoma MCF-7 cell . REF101974 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.18 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF101267 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.18 uM . . . Chronic myeloid leukemia K562 cell . REF101044 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.18 uM . . . Lung adenocarcinoma A-549 cell . REF101061 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.19 uM . . . Gastric cancer MGC-803 cell . REF101306 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.2 nM . . . Skin squamous cell carcinoma A431 cell . REF100724 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.2 nM . . . Invasive breast carcinoma MCF-7 cell . REF100367 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.2 nM . . . Lung large cell carcinoma NCI-H460 cell . REF102171 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.2 ug/mL . . . T-lymphoblastic leukemia MOLT-3 cell . REF102052 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.2 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100830 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.2 uM . . . Prostate carcinoma PC-3 cell . REF101554 DRG00011 Doxorubicin Half Maximal Lethal dose (LD50) = 1.2 uM . . . Gastric adenocarcinoma AGS cell . REF102126 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.2 uM . . . Hepatoblastoma Hep-G2 cell . REF101938 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.2 uM . . . Normal Farage cell . REF101925 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.2 uM . . . Normal 184B5 cell . REF101657 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.2 uM . . . Endocervical adenocarcinoma HeLa cell . REF101552 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.2 uM . . . Lung adenocarcinoma A-549 cell . REF101303 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.2 uM . . . Normal MCF-10A cell . REF101173 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.2 uM . . . Gastric adenocarcinoma AGS cell . REF101157 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.2 uM . . . Normal L929 cell . REF100707 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.2 uM . . . Ileocecal adenocarcinoma HCT-8 cell . REF100574 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.2 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100744 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 1.2 uM . . . Lymphoblastic leukemia L1210 cell . REF100145 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 1.2 uM . . . Normal Vero cell . REF100002 DRG00406 Monastrol Half Maximal Effective Concentration (EC50) = 1.2 uM . . . Colon carcinoma HCT 116 cell . REF102172 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.21 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF101245 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.21 uM . . . Hepatoblastoma Hep-G2 cell . REF101714 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.21 uM . . . Lung adenocarcinoma A-549 cell . REF101259 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 1.22 uM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF102305 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.22 uM . . . Endocervical adenocarcinoma HeLa cell . REF100750 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.22 uM . . . Invasive breast carcinoma MCF-7 cell . REF100750 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.22 uM . . . Lymphoma P388 cell . REF100150 DRG00107 Betulinic acid Half Maximal Effective Dosage (ED50) = 1.23 ug/mL . . . T acute lymphoblastic leukemia MOLT-4 cell . REF102114 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.23 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102326 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.23 uM . . . Colon cancer HT29 cell . REF100877 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 1.23027 uM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF100123 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.239 uM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100729 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.246 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101690 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.25 nM . . . Invasive breast carcinoma MCF-7 cell . REF101432 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.25 uM . . . Hepatoma Bel-7402 cell . REF101026 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.258 uM . . . Endocervical adenocarcinoma HeLa cell . REF101353 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 1.25893 uM . . . Colon adenocarcinoma HCC 2998 cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 1.25893 uM . . . Glioblastoma SF-295 cell . REF102222 DRG00224 Pemetrexed Half Maximal Inhibitory Concentration (IC50) = 1.26 uM . . . Lung adenocarcinoma A-549 cell . REF101737 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.27 uM . . . Rhabdomyosarcoma RD cell . REF101684 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.27 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100923 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.274 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100643 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.28 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF101973 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.29±0.18 µM 48 h . . Amelanotic melanoma LO #2 cell "DOX showed strong in vitro cytotoxicity against all four kinds of cells without tumor selectivity, with IC50 values of 1.65 0.20 M (U87), 1.58 0.19 M (HepG2), 3.55 0.21 M (A549), and 1.29 0.18 M (LO2), respectively" REF00315 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.3 mM . . . Hepatoblastoma Hep-G2 cell . REF100575 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.3 nM . . . Stomach adenocarcinoma BGC-823 cell . REF101819 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.3 nM . . . Colon carcinoma HCT 116 cell . REF100908 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.3 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100700 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 1.3 nM . . . Prostate carcinoma DU145 cell . REF100549 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.3 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF101012 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.3 ug/mL . . . Acute myeloid leukemia HL-60 cell . REF102014 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.3 ug/mL . . . Colon carcinoma HCT 116 cell . REF100956 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.3 ug/mL . . . Breast ductal carcinoma BT-549 cell . REF100783 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.3 ug/mL . . . Cervical squamous cell carcinoma SiHa cell . REF100486 DRG00107 Betulinic acid Half Maximal Effective Dosage (ED50) = 1.3 ug/mL . . . Endocervical adenocarcinoma L132 cell . REF102114 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) = 1.3 ug/mL . . . Normal Vero cell . REF100034 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.3 uM . . . Lymphoblastic leukemia L1210 cell . REF102232 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 1.3 uM . . . Endocervical adenocarcinoma HeLa cell . REF100926 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.3 uM . . . Normal WI-38 cell . REF101837 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.3 uM . . . Gingival squamous cell carcinoma Ca9-22 cell . REF100813 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.3 uM . . . Colon cancer HT29 cell . REF100748 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.3 uM . . . Invasive breast carcinoma MCF-7 cell . REF100993 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 1.3 uM . . . Lymphoblastic leukemia L1210 cell . REF100231 DRG00020 Docetaxel Half Maximal Cytotoxicity Concentration (CC50) = 1.3 uM . . . Normal Vero cell . REF101568 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.3 uM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF101448 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.303 uM . . . Lung adenocarcinoma A-549 cell . REF101609 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 1.31 uM . . . Melanoma UACC-62 cell . REF101480 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.32 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100224 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.32 ug/mL . . . Breast adenocarcinoma MDA-MB-231 cell . REF100901 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.32 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101584 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.33 uM . . . Invasive breast carcinoma MCF-7 cell . REF101406 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1.34 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101729 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.34 ug/mL . . . Thymoma EL4 cell . REF102103 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.35 nM . . . Skin squamous cell carcinoma A431 cell . REF101661 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.35 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100830 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.35 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101560 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.35 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100464 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.36 ng/mL . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF101911 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.37 uM . . . Endocervical adenocarcinoma HeLa cell . REF101680 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.375 uM . . . Endocervical adenocarcinoma HeLa cell . REF101124 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.38 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100645 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.38 uM . . . Normal L929 cell . REF102280 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.39 uM . . . Hepatocellular carcinoma SMMC-7721 cell . REF101434 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.39 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100621 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.4 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF100616 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.4 nM . . . Colon cancer HT29 cell . REF100831 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.4 nM . . . Prostate carcinoma PC-3 cell . REF100721 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.4 nM . . . Invasive breast carcinoma MCF-7 cell . REF100415 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.4 nM . . . Chronic myeloid leukemia K562 cell . REF102196 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.4 uM . . . Invasive breast carcinoma MCF-7 cell . REF102378 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.4 uM . . . Colon cancer HT29 cell . REF100384 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.4 uM . . . Prostate carcinoma PC-3 cell . REF101964 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.4 uM . . . Chronic myeloid leukemia K562 cell . REF101820 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.4 uM . . . Lung adenocarcinoma A-549 cell . REF101562 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.4 uM . . . Normal Vero cell . REF101560 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.4 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101367 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 1.4 uM . . . Lung adenocarcinoma A-549 cell . REF102185 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 1.4 uM . . . Colon cancer HT29 cell . REF101063 DRG00024 Thapsigargin Half Maximal Inhibitory Concentration (IC50) = 1.4 uM . . . Thymoma EL4 cell . REF101320 DRG00107 Betulinic acid Half Maximal Effective Concentration (EC50) = 1.4 uM . . . Sezary syndrome H9 cell . REF102069 DRG00221 Acyclovir 90% Lethal Concentration (IC50) = 1.4 uM . . . Normal MRC5 cell . REF100018 DRG00407 Combretastatin A4 Half Maximal Effective Dosage (ED50) = 1.4 uM . . . Cutaneous melanoma SK-MEL-5 cell . REF100140 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.41 ug/mL . . . Chronic myeloid leukemia K562 cell . REF100599 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.41 uM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF101733 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.41 uM . . . Colon cancer HT29 cell . REF101584 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.41 uM . . . Chronic myeloid leukemia K562 cell . REF101081 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 1.41254 uM . . . Renal carcinoma UO-31 cell . REF102227 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.4144 uM . . . Prostate carcinoma PC-3 cell . REF100442 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 1.42 uM . . . Lung large cell carcinoma NCI-H460 cell . REF100822 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.428 uM . . . Invasive breast carcinoma MCF-7 cell . REF101580 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.43 uM . . . Invasive breast carcinoma MCF-7 cell . REF101817 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.43 uM . . . Prostate carcinoma PC-3 cell . REF101761 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.43 uM . . . Skin squamous cell carcinoma A431 cell . REF101761 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.45 mM . . . Acute myeloid leukemia HL-60 cell . REF100612 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.46 uM . . . Prostate carcinoma DU145 cell . REF100788 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.46 uM . . . Colon adenocarcinoma LoVo cell . REF100628 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1.47 nM . . . Prostate carcinoma DU145 cell . REF101729 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.47 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101264 DRG00311 "2,6-Dimethoxyquinone" Half Maximal Effective Dosage (ED50) = 1.5 ng/mL . . . Lymphoma P388 cell . REF102031 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.5 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF101782 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.5 nM . . . Endocervical adenocarcinoma HeLa cell . REF100644 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.5 nM . . . Colon carcinoma HCT 116 cell . REF100499 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.5 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100438 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 1.5 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF102148 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.5 nM . . . Bone marrow neuroblastoma SH-SY5Y cell . REF102121 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.5 ug/mL . . . Normal Vero cell . REF100239 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 1.5 ug/mL . . . Normal MT4 cell . REF102058 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.5 uM . . . Endocervical adenocarcinoma HeLa cell . REF102232 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.5 uM . . . Invasive breast carcinoma MCF-7 cell . REF102168 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 1.5 uM . . . Normal BEAS-2B cell . REF101657 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.5 uM . . . Cervical squamous cell carcinoma SiHa cell . REF100662 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.5 uM . . . Lymphoblastic leukemia L1210 cell . REF100179 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1.5 uM . . . Lung carcinoma SW1573 cell . REF101730 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.5 uM . . . Lung large cell carcinoma NCI-H1299 cell . REF101449 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.5 uM . . . Stomach adenocarcinoma BGC-823 cell . REF100854 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 1.5 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100481 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 1.5 uM . . . Pancreatic ductal adenocarcinoma Capan-1 cell . REF101576 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 1.5 uM . . . Melanoma UACC-257 cell . REF102093 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 1.508 uM . . . Acute myeloid leukemia HL-60 cell . REF100762 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.51 uM . . . Hepatoblastoma Hep-G2 cell . REF101833 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.51 uM . . . Lung adenocarcinoma A549/TR cell . REF101482 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.52 nM . . . Colon adenocarcinoma SW620 cell . REF102270 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 1.53 nM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100482 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.53 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100426 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.54 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100960 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.54 uM . . . Normal MCF-10A cell . REF101660 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.54 uM . . . Invasive breast carcinoma MCF-7 cell . REF101043 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.54 uM . . . Hepatoblastoma Hep-G2 cell . REF100877 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.546 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101295 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 1.557 uM . . . Lung adenocarcinoma A-549 cell . REF101812 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 1.56 uM . . . Invasive breast carcinoma MCF-7 cell . REF101385 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.56 uM . . . Uterine sarcoma MES-SA cell . REF100477 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.57 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100228 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.57 uM . . . Colon cancer HT29 cell . REF101871 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 1.57 uM . . . Lung adenocarcinoma A-549 cell . REF100789 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.57 uM . . . Prostate carcinoma DU145 cell . REF100621 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 1.57 uM . . . Thymoma EL4 cell . REF100255 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.58 uM . . . Lung adenocarcinoma A-549 cell . REF101344 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.58±0.19 µM 48 h . . Hepatoblastoma Hep-G2 cell "DOX showed strong in vitro cytotoxicity against all four kinds of cells without tumor selectivity, with IC50 values of 1.65 0.20 M (U87), 1.58 0.19 M (HepG2), 3.55 0.21 M (A549), and 1.29 0.18 M (LO2), respectively" REF00315 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 1.58489 uM . . . Astrocytoma SF268 cell . REF102227 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 1.58489 uM . . . Colon adenocarcinoma HCC 2998 cell . REF100098 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.59 uM . . . Endocervical adenocarcinoma HeLa cell . REF101358 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.6 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101076 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.6 nM . . . Invasive breast carcinoma MCF-7 cell . REF100928 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.6 nM . . . Endocervical adenocarcinoma HeLa cell . REF101123 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.6 nM . . . Colon carcinoma HCT 116 cell . REF100309 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.6 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100126 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.6 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100965 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 1.6 ug/mL . . . Lung adenocarcinoma PC-9 cell . REF100009 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.6 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101761 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1.6 uM . . . Endocervical adenocarcinoma HeLa cell . REF101761 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.6 uM . . . Lung adenocarcinoma A-549 cell . REF101336 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.6 uM . . . Acute myeloid leukemia HL-60 cell . REF101596 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.6 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101436 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.6 uM . . . Chronic myeloid leukemia K562 cell . REF101377 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.6 uM . . . Normal LLC-PK1 cell . REF101132 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.6 uM . . . Lymphoblastic leukemia L1210 cell . REF100170 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1.6 uM . . . Lung carcinoma SW1573 cell . REF101730 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.61 uM . . . Normal HEK293 cell . REF101684 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 1.62 uM . . . Astrocytoma SF268 cell . REF102305 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.62 uM . . . Invasive breast carcinoma T-47D cell . REF101358 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.63 uM . . . Prostate carcinoma PC-3 cell . REF100877 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 1.64 ug/mL . . . Normal MT4 cell . REF102110 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.64 uM . . . Endocervical adenocarcinoma HeLa cell . REF100945 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1.65 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101759 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.65 uM . . . Prostate carcinoma PC-3 cell . REF101084 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.664 uM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF101690 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.67 uM . . . Chronic myeloid leukemia K562 cell . REF101008 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.67 uM . . . Amelanotic melanoma MDA-MB-435 cell . REF100767 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.67 uM . . . Colon adenocarcinoma HCT 15 cell . REF100594 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.68 uM . . . Endocervical adenocarcinoma HeLa cell . REF101373 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 1.68 uM . . . Endocervical adenocarcinoma L132 cell . REF101392 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.69 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101236 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.69 uM . . . Invasive breast carcinoma MCF-7 cell . REF100904 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.7 nM . . . Invasive breast carcinoma MCF-7 cell . REF101967 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.7 nM . . . Endocervical adenocarcinoma HeLa cell . REF101164 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 1.7 nM . . . Invasive breast carcinoma MCF-7 cell . REF101654 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.7 nM . . . Colon adenocarcinoma HCT 15 cell . REF102090 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.7 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100426 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.7 uM . . . Breast carcinoma MX1 cell . REF101231 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 1.7 uM . . . Colon adenocarcinoma WiDr cell . REF100753 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.7 uM . . . Colon cancer HT29 cell . REF101965 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.7 uM . . . Normal HEL 299 cell . REF101925 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.7 uM . . . Endocervical adenocarcinoma HeLa cell . REF101762 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.7 uM . . . Lymphoblastic leukemia L1210 cell . REF101705 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.7 uM . . . Lung adenocarcinoma A-549 cell . REF101553 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 1.7 uM . . . Lung adenocarcinoma A-549 cell . REF101109 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.7 uM . . . Melanoma B16 cell . REF101042 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.7 uM . . . T acute lymphoblastic leukemia Jurkat cell . REF100411 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.7 uM . . . Lung adenocarcinoma A-549 cell . REF100445 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.718 uM . . . Hepatoma Bel-7402 cell . REF100126 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 1.72 nM 72 h . . Mouse melanoma SORT1-positive B16-F10 cell "SORT1-positive SK-MEL-28 and B16-F10 melanoma cells were selected for testing the anti-proliferative effect of docetaxel and TH1902. When TH1902 biological effects were monitored, the half-maximal inhibitory concentration (IC50) of TH1902 was similar to that of docetaxel, averaging 0.38 vs. 0.39 nM, respectively, in human SK-MEL-28 cells, and 2.57 vs. 1.72 nM in murine B16-F10 cells." REF00303 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.72 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100663 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.73 uM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF101844 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.73 uM . . . Endocervical adenocarcinoma HeLa cell . REF101569 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 1.7378 uM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF102227 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 1.74 uM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF102305 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.75 uM . . . Prostate carcinoma DU145 cell . REF100904 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 1.75 uM . . . Lung adenocarcinoma A-549 cell . REF102424 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1.76 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101729 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1.76 nM . . . Normal COLO205 cell . REF100197 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.76 uM . . . Colon cancer HT29 cell . REF101236 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.76 uM . . . Colon adenocarcinoma HCT 15 cell . REF101089 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.76 uM . . . Prostate carcinoma PC-3 cell . REF100803 DRG00010 Daunorubicin Half Maximal Growth Inhibition (GI50) = 1.77 uM . . . Normal Detroit 551 cell . REF100836 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.78 ng/ml . . . Renal carcinoma A498 cell . REF100235 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.78 uM . . . Laryngeal carcinoma HEp-2 cell . REF101684 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.78 uM . . . Endocervical adenocarcinoma HeLa cell . REF101387 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.79 uM . . . Invasive breast carcinoma ZR-75-1 cell . REF101919 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.79 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101224 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.8 nM . . . Invasive breast carcinoma MCF-7 cell . REF100576 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.8 ug/mL . . . Amelanotic melanoma A-375 cell . REF100381 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.8 uM . . . Invasive breast carcinoma MCF-7 cell . REF101030 DRG00011 Doxorubicin Half Maximal Lethal dose (LD50) = 1.8 uM . . . Colon cancer HT29 cell . REF102126 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 1.8 uM . . . Prostate carcinoma DuPro cell . REF102095 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.8 uM . . . Acute monocytic leukemia THP-1 cell . REF101793 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.8 uM . . . Pancreatic ductal adenocarcinoma Capan-1 cell . REF101705 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 1.8 uM . . . Normal BEAS-2B cell . REF101657 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.8 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100408 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.8 uM . . . Invasive breast carcinoma MCF-7 cell . REF101256 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.8 uM . . . Hepatoma Bel-7402 cell . REF100838 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.8 uM . . . Endocervical adenocarcinoma HeLa cell . REF101448 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.807 uM . . . Prostate carcinoma DU145 cell . REF101609 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.81 uM . . . Prostate carcinoma PC-3 cell . REF101049 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.819 uM . . . Invasive breast carcinoma MCF-7 cell . REF101444 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.82 uM . . . Invasive breast carcinoma T-47D cell . REF101089 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.83 uM . . . Lung adenocarcinoma A-549 cell . REF101284 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.84 uM . . . Invasive breast carcinoma T-47D cell . REF101404 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.86 uM . . . Prostate carcinoma DU145 cell . REF101584 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 1.87 mM . . . Normal MT-2 cell . REF102153 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 1.873 mM . . . Sezary syndrome H9 cell . REF102088 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 1.875 mM . . . Sezary syndrome H9 cell . REF102081 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.88 ug/mL . . . Acute myeloid leukemia HL-60 cell . REF100300 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.88 uM . . . Colon carcinoma HCT 116 cell . REF101684 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.88 uM . . . Invasive breast carcinoma T-47D cell . REF101362 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.89 uM . . . Hepatoma Bel-7402 cell . REF101143 DRG00107 Betulinic acid Half Maximal Effective Concentration (EC50) = 1.9 mM . . . Prostate carcinoma PC-3 cell . REF102093 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 1.9 mM . . . Sezary syndrome H9 cell . REF102151 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.9 ng/ml . . . Renal carcinoma A498 cell . REF100288 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.9 ng/mL . . . Lung adenocarcinoma A-549 cell . REF101076 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.9 nM . . . Hepatoblastoma Hep-G2 cell . REF101727 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1.9 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101456 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.9 nM . . . Invasive breast carcinoma MCF-7 cell . REF100505 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.9 nM . . . Endocervical adenocarcinoma HeLa cell . REF102310 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.9 nM . . . Acute myeloid leukemia HL-60 cell . REF102132 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1.9 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100099 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.9 uM . . . Lung adenocarcinoma A-549 cell . REF101828 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 1.9 uM . . . Renal carcinoma A498 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.9 uM . . . Cervical squamous cell carcinoma SiHa cell . REF101495 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.9 uM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF101476 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.9 uM . . . Invasive breast carcinoma T-47D cell . REF101358 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.9 uM . . . Lung adenocarcinoma A-549 cell . REF101335 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.9 uM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101249 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.9 uM . . . Lung adenocarcinoma NCI-H23 cell . REF101169 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1.9 uM . . . Cervical squamous cell carcinoma SiHa cell . REF101019 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.9 uM . . . Prostate carcinoma DU145 cell . REF100961 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.9 uM . . . Lung adenocarcinoma PC-14 cell . REF100301 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 1.9 uM . . . Colon cancer HT29 cell . REF101389 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 1.9 uM . . . Lung adenocarcinoma A-549 cell . REF102193 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 1.9 uM . . . Endocervical adenocarcinoma HeLa cell . REF102041 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.91 uM . . . Endocervical adenocarcinoma HeLa cell . REF101584 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.91 uM . . . Prostate carcinoma DU145 cell . REF101554 DRG00081 Cytarabine Half Maximal Lethal dose (LD50) = 1.91 uM . . . Mouse plasma cell myeloma MPC-11 cell . REF100029 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.92 uM . . . Lung adenocarcinoma A-549 cell . REF100590 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.93 nM . . . Lung adenocarcinoma A-549 cell . REF100793 DRG00003 Fluorouracil Half Maximal Effective Dosage (ED50) = 1.94 ug/mL . . . Lymphoblastic leukemia L1210 cell . REF102029 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.94 uM . . . Prostate carcinoma DU145 cell . REF101357 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 1.94 uM . . . Acute myeloid leukemia HL-60 cell . REF101710 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.945 uM . . . Lung adenocarcinoma A-549 cell . REF101508 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.95 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100184 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.96 uM . . . Colon carcinoma HCT 116 cell . REF101684 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 1.97 ng/ml . . . Renal carcinoma A498 cell . REF100184 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 1.98 nM . . . Colon cancer HT29 cell . REF101149 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1.98 uM . . . Acute monocytic leukemia U-937 cell . REF101045 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.986 uM . . . Lung adenocarcinoma A-549 cell . REF101353 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.99 uM . . . Breast adenocarcinoma MDA-MB-453 cell . REF101554 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1.995 uM . . . Endocervical adenocarcinoma HeLa cell . REF101609 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 1.99526 uM . . . Breast ductal carcinoma BT-549 cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 1.99526 uM . . . Chronic myeloid leukemia K562 cell . REF102222 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 10 µM 1 h . . human coronary artery endothelial cell Human coronary artery endothelial cell "We next determined whether treatment of HCAEC and Molt-3 T cells with peptides, MTX, and MTX-peptide conjugates resulted in inhibition of cell proliferation. Both HCAEC and Molt-3 T cells were affected by test compound in different levels. None of the molecules caused growth stimulation or total culture extinction. A net cell killing of HCAEC was observed upon treatment with MTX at all test concentrations while MTX affected net killing at 1.0 µM in Molt-3 T cells. The MTX-peptide conjugates were less toxic than MTX. In HCAEC, the net cell killing was at lower concentration for MTX at 0.1 µM compared to MTX-peptide conjugates at 500 µM. The net cell killing of Molt-3 T cells was found at 1.0 µM for MTX and 50 µM for MTX-peptide conjugates. For all test concentrations, the conjugates only resulted in HCAEC partial growth inhibition. For Molt-3 T cells, a total growth inhibition emerged at 100 µM for cLABL and cLBEL; however, 500 µM cLABL and cLBEL did not cause total cell killing for T cells." REF00259 DRG00034 Chlorin e6 Half Maximal Inhibitory Concentration (IC50) > 10 µM 24 h . . Human papillomavirus-related cervical adenocarcinoma GPC3-negative HeLa cell "Subsequently, the antiproliferative activities of the PS conjugates, including dark toxicity and phototoxicity (660 nM, light dose: 10 J/cm2), were evaluated. Dark toxicity refers to the toxicity of PS conjugates against cancer cells in the absence of light and can be regarded as a crucial measure of the safety profile, while phototoxicity is the most direct indicator of the PDT efficacy of PS. The results showed that the dark toxicity of all the compounds against the five cell lines was comparatively low, demonstrating that the PS conjugates exhibited a high safety index in the absence of light. Compound 8b exhibited the optimum tumor cell selectivity in terms of phototoxicity, with the IC50 values of 0.82 µM against HepG2 cells and 2.4 µM against Huh-7 cells, respectively, whereas its toxicity against GPC3-negative cell lines was >10 µM. Although compounds 8a and 8cd exhibited excellent phototoxicity against HepG2 and Huh-7 cells, (IC50 range: 0.22.0 µM), these compounds lacked selectivity between GPC3-overexpressed and GPC3-negative cells because they also showed considerable phototoxicity against the cell lines with minimal GPC3 expression. Notably, compound 1 showed low phototoxicity and selectivity against all the tested cell lines (IC50 > 10 µM)." REF00289 DRG00034 Chlorin e6 Half Maximal Inhibitory Concentration (IC50) > 10 µM 24 h . . Invasive breast carcinoma GPC3 negative MCF7 cell "Subsequently, the antiproliferative activities of the PS conjugates, including dark toxicity and phototoxicity (660 nM, light dose: 10 J/cm2), were evaluated. Dark toxicity refers to the toxicity of PS conjugates against cancer cells in the absence of light and can be regarded as a crucial measure of the safety profile, while phototoxicity is the most direct indicator of the PDT efficacy of PS. The results showed that the dark toxicity of all the compounds against the five cell lines was comparatively low, demonstrating that the PS conjugates exhibited a high safety index in the absence of light. Compound 8b exhibited the optimum tumor cell selectivity in terms of phototoxicity, with the IC50 values of 0.82 µM against HepG2 cells and 2.4 µM against Huh-7 cells, respectively, whereas its toxicity against GPC3-negative cell lines was >10 µM. Although compounds 8a and 8cd exhibited excellent phototoxicity against HepG2 and Huh-7 cells, (IC50 range: 0.22.0 µM), these compounds lacked selectivity between GPC3-overexpressed and GPC3-negative cells because they also showed considerable phototoxicity against the cell lines with minimal GPC3 expression. Notably, compound 1 showed low phototoxicity and selectivity against all the tested cell lines (IC50 > 10 µM)." REF00289 DRG00034 Chlorin e6 Half Maximal Inhibitory Concentration (IC50) > 10 µM 24 h . . Normal Human umbilical vein endothelial cell "Subsequently, the antiproliferative activities of the PS conjugates, including dark toxicity and phototoxicity (660 nM, light dose: 10 J/cm2), were evaluated. Dark toxicity refers to the toxicity of PS conjugates against cancer cells in the absence of light and can be regarded as a crucial measure of the safety profile, while phototoxicity is the most direct indicator of the PDT efficacy of PS. The results showed that the dark toxicity of all the compounds against the five cell lines was comparatively low, demonstrating that the PS conjugates exhibited a high safety index in the absence of light. Compound 8b exhibited the optimum tumor cell selectivity in terms of phototoxicity, with the IC50 values of 0.82 µM against HepG2 cells and 2.4 µM against Huh-7 cells, respectively, whereas its toxicity against GPC3-negative cell lines was >10 µM. Although compounds 8a and 8cd exhibited excellent phototoxicity against HepG2 and Huh-7 cells, (IC50 range: 0.22.0 µM), these compounds lacked selectivity between GPC3-overexpressed and GPC3-negative cells because they also showed considerable phototoxicity against the cell lines with minimal GPC3 expression. Notably, compound 1 showed low phototoxicity and selectivity against all the tested cell lines (IC50 > 10 µM)." REF00289 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 µM 36 h . . Invasive breast carcinoma MCF-7 cell "Doxorubicin (DOX) is one of the most effective anticancer drugs and has been successfully used in clinical practice. However, DOX cannot differentiate between cancer cells and normal cells, which may induce unwanted side effects and severe toxicity. Compared with traditional small-molecule anticancer drugs, the peptide-drug conjugates (PDCs) have enhanced targeting specificity and water solubility. Based on these advantages, to further explore the function of 10a, we designed and prepared a anticancer PDC drug compound RGD-GFLG-DOX containing the tetrapeptide linker Gly-Phe-Leu-Gly, which can be cleaved in presence of cathepsin B, a highly upregulated enzyme in malignant tumors, to release the drug. RGD-GFLG was synthesized as a control. The inhibitory effects of RGD-GFLG-DOX on cancer cell lines were assessed using cytotoxicity assay. Specifically, the effects of RGD-GFLG-DOX were evaluated on integrin αvβ3-positive cancer cell lines, including A549 and U87MG cells, integrin αvβ3-negative cancer cell lines such as HeLa and MCF-7 cells, as well as normal cell lines, namely LO2 and MIHA cells. RGD-GFLG-DOX exhibited a lower cytotoxicity on HeLa, MCF-7, LO2 and MIHA cells, but a stronger cytotoxicity than DOX on A549 and U87MG cells. For comparison, RGD-GFLG demonstrated minimal cytotoxicity. In addition, the cytotoxicity of RGD-GFLG-DOX with various concentrations (040µM) on A549 and U87MG cells was studied. The results showed that the cytotoxicity of RGD-GFLG-DOX on A549 and U87MG cells was dose-dependent. These indicate that RGD-GFLG-DOX has a good specificity and inhibitory activity toward integrin αvβ3-overexpressed A549 and U87MG cells." REF00270 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 10 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101947 DRG00009 Camptothecin Half Maximal Effective Concentration (EC50) = 10 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100353 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 10 ng/mL . . . Lung adenocarcinoma A-549 cell . REF102176 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 10 ng/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF102176 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101921 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100960 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 ng/mL . . . Hepatoma Bel-7402 cell . REF100656 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100592 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 ng/mL . . . Lung large cell carcinoma NCI-H460 cell . REF100578 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 10 ng/mL . . . Glioma XF498 cell . REF100539 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 10 ng/mL . . . Melanoma SK-MEL-2 cell . REF100539 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 10 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100466 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 10 ng/ml . . . Colon cancer HT29 cell . REF100288 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 10 ng/ml . . . Renal carcinoma A498 cell . REF100232 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 10 ng/ml . . . Prostate carcinoma PC-3 cell . REF100192 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 ng/mL . . . Colon cancer HT29 cell . REF102103 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 ng/mL . . . Lymphoma P388 cell . REF101921 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 10 ng/mL . . . Chronic myeloid leukemia K562 cell . REF100565 DRG00012 Paclitaxel 90% Lethal Concentration (IC50) = 10 ng/mL . . . Colon adenocarcinoma COLO 320DM cell . REF100483 DRG00012 Paclitaxel Half Maximal Cytotoxicity Concentration (CC50) = 10 ng/mL . . . Endocervical adenocarcinoma HeLa cell . REF100441 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 ng/mL . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF100311 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 10 ng/mL . . . Colon cancer HT29 cell . REF100299 DRG00221 Acyclovir Half Maximal Infective Dose (ID50) = 10 ng/mL . . . Normal Vero cell . REF102019 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 10 ng/mL . . . Normal MT4 cell . REF102110 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 10 ng/mL . . . Sezary syndrome H9 cell . REF100073 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Testicular embryonal carcinoma 833K cell . REF101914 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 10 nM . . . Melanoma UACC-62 cell . REF101533 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 10 nM . . . Prostate carcinoma DU145 cell . REF101533 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 10 nM . . . Gliosarcoma SF539 cell . REF101047 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 10 nM . . . Non-small cell lung carcinoma HOP-62 cell . REF100986 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 10 nM . . . Invasive breast carcinoma MCF-7 cell . REF100844 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Lung adenocarcinoma A-549 cell . REF100650 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Lung squamous cell carcinoma SK-MES-1 cell . REF100540 DRG00009 Camptothecin Half Maximal Cytotoxicity Concentration (CC50) = 10 nM . . . Normal MT4 cell . REF100269 DRG00011 Doxorubicin Half Maximal Infective Dose (ID50) = 10 nM . . . EBV-related Burkitt lymphoma Raji cell . REF102009 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Colon carcinoma HCT 116 cell . REF101908 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 10 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101330 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Endocervical adenocarcinoma HeLa cell . REF101247 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Prostate carcinoma DU145 cell . REF101247 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Melanoma SK-MEL-2 cell . REF101160 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Lung adenocarcinoma A-549 cell . REF100856 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100808 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Amelanotic melanoma A-375 cell . REF100630 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100627 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Normal MT4 cell . REF100506 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 10 nM . . . Colon adenocarcinoma LoVo cell . REF100409 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 10 nM . . . Endocervical adenocarcinoma HeLa cell . REF100409 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Chronic myeloid leukemia K562 cell . REF100394 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Neuroblastoma IMR-32 cell . REF100370 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Astrocytoma U-373MG ATCC cell . REF100340 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Invasive breast carcinoma MCF-7 cell . REF100305 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Mouse colon adenocarcinoma MC-38 cell . REF100205 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Lung adenocarcinoma A-549 cell . REF101662 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF101615 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Amelanotic melanoma A-375 cell . REF101481 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101481 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 10 nM . . . Colon carcinoma HCT 116 cell . REF101147 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Acute myeloid leukemia HL-60 cell . REF100944 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 10 nM . . . Melanoma B16 cell . REF100828 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Astrocytoma SF268 cell . REF100827 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 10 nM . . . Hepatocellular carcinoma SNU-398 cell . REF100712 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Lymphoma P388 cell . REF100633 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Colon carcinoma RKO cell . REF100606 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100606 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100598 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 10 nM . . . Lung adenocarcinoma A-549 cell . REF100448 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100394 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 10 nM . . . Melanoma M14 cell . REF100274 DRG00013 Gemcitabine Half Maximal Growth Inhibition (GI50) = 10 nM . . . Invasive breast carcinoma MCF-7 cell . REF100108 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101413 DRG00019 Methotrexate Half Maximal Growth Inhibition (GI50) = 10 nM . . . Colon carcinoma HCT 116 cell . REF100434 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Reuber hepatoma H35 cell . REF100177 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Lymphoblastic leukemia L1210 cell . REF100173 DRG00019 Methotrexate Half Maximal Infective Dose (ID50) = 10 nM . . . Lymphoblastic leukemia L1210 cell . REF100022 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101849 DRG00024 Thapsigargin Half Maximal Lethal dose (LD50) = 10 nM . . . Prostate carcinoma LNCaP cell . REF101858 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF100023 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 10 nM . . . Normal MT4 cell . REF102051 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF100035 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100035 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Lung adenocarcinoma A-549 cell . REF102376 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 10 nM . . . Breast ductal carcinoma BT-549 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 10 nM . . . Cutaneous melanoma SK-MEL-5 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 10 nM . . . Melanoma UACC-62 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 10 nM . . . Prostate carcinoma DU145 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 10 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102164 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Hepatoma Bel-7402 cell . REF102131 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 10 nM . . . Endocervical adenocarcinoma HeLa cell . REF101811 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 10 pg/ml . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100158 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 10 ug/mL . . . Lung adenocarcinoma PC-14 cell . REF102014 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) = 10 ug/mL . . . Erythroleukemia HEL cell . REF100003 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 10 uM . . . Colon adenocarcinoma Caco-2 cell . REF101738 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 10 uM . . . Endocervical adenocarcinoma HeLa cell . REF101738 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 10 uM . . . Prostate carcinoma DU145 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 10 uM . . . Renal carcinoma A498 cell . REF100098 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 10 uM . . . Invasive breast carcinoma MCF-7 cell . REF100675 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 uM . . . Hepatoblastoma Hep-G2 cell . REF102516 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100410 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 10 uM . . . Prostate carcinoma PC-3 cell . REF100987 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 10 uM . . . Melanoma M14 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 10 uM . . . Renal cell carcinoma SN12C cell . REF100756 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 10 uM . . . Mouse melanoma B16-F10 cell . REF102217 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 10 uM . . . Normal MT-2 cell . REF102010 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10.02 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101515 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 10.1 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100188 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 10.1 uM . . . Endocervical adenocarcinoma HeLa cell . REF101504 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 10.1 uM . . . Hepatoblastoma Hep-G2 cell . REF102367 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 10.12 uM . . . Lung carcinoid tumor NCI-H727 cell . REF102400 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10.15 uM . . . Hepatoblastoma Hep-G2 cell . REF101397 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 10.17 uM . . . Hepatoblastoma Hep-G2 cell . REF102371 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 10.2 uM . . . Invasive breast carcinoma MCF-7 cell . REF102401 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 10.2 uM . . . Colon cancer HT29 cell . REF102236 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 10.21 uM . . . Hepatoblastoma Hep-G2 cell . REF102447 DRG00019 Methotrexate Half Maximal Growth Inhibition (GI50) = 10.25 uM . . . Pleural epithelioid mesothelioma NCI-H226 cell . REF100983 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 10.3 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100224 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 10.3 nM . . . Astrocytoma SF268 cell . REF102166 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 10.3 nM . . . Invasive breast carcinoma MCF-7 cell . REF101688 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10.3 uM . . . Hepatoblastoma Hep-G2 cell . REF101698 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 10.3 uM . . . Lung adenocarcinoma A-549 cell . REF100120 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10.32 uM . . . Hepatoblastoma Hep-G2 cell . REF101096 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10.4 uM . . . Cervical carcinoma L02 cell . REF101542 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 10.4±1.6 nM 24 h . . Ovarian endometrioid adenocarcinoma A2780 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10.44 uM . . . Cervical carcinoma L02 cell . REF101728 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 10.5 uM . . . Breast ductal carcinoma BT-549 cell . REF101978 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 10.56 uM . . . Invasive breast carcinoma T-47D cell . REF102322 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10.6 pg/ml . . . Hepatoblastoma Hep-G2 cell . REF101400 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 10.6 uM . . . Invasive breast carcinoma MCF-7 cell . REF102401 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10.6 uM . . . Invasive breast carcinoma MCF-7 cell . REF101573 DRG00038 Monomethyl auristatin E Half Maximal Inhibitory Concentration (IC50) = 10.7 nM 72 h . . Gastric adenocarcinoma MKN45 cell "We next evaluated the in vitro cytotoxicity of 1131-MMAE. NUGC-4, MKN45 and HGC27 cells were drug-treated for 72 h and their viability was assessed. 1131-MMAE killed KK-LC-1 positive gastric cancer cells with high potency. The IC50 values of 1131-MMAE were 3.87 nM for NUGC-4 cells and 5.26 nM for MKN45 cells. However, although a very high concentration was used, 1131-MMAE could only moderately inhibit the viability of KK-LC-1 negative HGC27 cells. The IC50 value of 1131-MMAE for HGC27 cells was 100200 times higher than that in NUGC-4 and MNK45 cells. Free MMAE exerted cytotoxicity irrespective of the KK-LC-1 expression status. The IC50 values of free MMAE were 10.97 nM for NUGC-4 cells, 10.70 nM for MKN45 cells and 7.18 nM for HGC27 cells. Naked 1131 peptide showed no cytotoxicity to all three cell lines. These results were consistent with the KK-LC-1-dependent endocytosis and confirmed the target-selective killing of 1131-MMAE." REF00226 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 10.7 uM . . . Lung adenocarcinoma A-549 cell . REF102502 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 10.7 uM . . . Hepatoblastoma Hep-G2 cell . REF101587 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 10.7 uM . . . Endocervical adenocarcinoma HeLa cell . REF101498 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 10.71519 uM . . . Breast ductal carcinoma BT-549 cell . REF102227 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 10.8 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100136 DRG00101 Vidarabine Half Maximal Infective Dose (ID50) = 10.8 uM . . . Lymphoma P388 cell . REF102027 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 10.82 uM . . . Lung adenocarcinoma A-549 cell . REF100804 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 10.86 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100731 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10.86 uM . . . Prostate carcinoma DU145 cell . REF101088 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 10.9 uM . . . Ovarian serous adenocarcinoma OVCAR-5 cell . REF102305 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 10.9 uM . . . Invasive breast carcinoma MCF-7 cell . REF101202 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 10.9 uM . . . Endocervical adenocarcinoma HeLa cell . REF101203 DRG00038 Monomethyl auristatin E Half Maximal Inhibitory Concentration (IC50) = 10.97 nM 72 h . . Gastric signet ring cell adenocarcinoma NUGC-4 cell "We next evaluated the in vitro cytotoxicity of 1131-MMAE. NUGC-4, MKN45 and HGC27 cells were drug-treated for 72 h and their viability was assessed. 1131-MMAE killed KK-LC-1 positive gastric cancer cells with high potency. The IC50 values of 1131-MMAE were 3.87 nM for NUGC-4 cells and 5.26 nM for MKN45 cells. However, although a very high concentration was used, 1131-MMAE could only moderately inhibit the viability of KK-LC-1 negative HGC27 cells. The IC50 value of 1131-MMAE for HGC27 cells was 100200 times higher than that in NUGC-4 and MNK45 cells. Free MMAE exerted cytotoxicity irrespective of the KK-LC-1 expression status. The IC50 values of free MMAE were 10.97 nM for NUGC-4 cells, 10.70 nM for MKN45 cells and 7.18 nM for HGC27 cells. Naked 1131 peptide showed no cytotoxicity to all three cell lines. These results were consistent with the KK-LC-1-dependent endocytosis and confirmed the target-selective killing of 1131-MMAE." REF00226 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 10.97 uM . . . Lung adenocarcinoma PC-9 cell . REF102275 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 10.99 uM . . . Invasive breast carcinoma MCF-7 cell . REF102223 DRG00034 Chlorin e6 Half Maximal Inhibitory Concentration (IC50) > 100 µM 24 h . . Hepatoblastoma L-O2 cell line "Subsequently, the antiproliferative activities of the PS conjugates, including dark toxicity and phototoxicity (660 nM, light dose: 10 J/cm2), were evaluated. Dark toxicity refers to the toxicity of PS conjugates against cancer cells in the absence of light and can be regarded as a crucial measure of the safety profile, while phototoxicity is the most direct indicator of the PDT efficacy of PS. The results showed that the dark toxicity of all the compounds against the five cell lines was comparatively low, demonstrating that the PS conjugates exhibited a high safety index in the absence of light. Compound 8b exhibited the optimum tumor cell selectivity in terms of phototoxicity, with the IC50 values of 0.82 µM against HepG2 cells and 2.4 µM against Huh-7 cells, respectively, whereas its toxicity against GPC3-negative cell lines was >10 µM. Although compounds 8a and 8cd exhibited excellent phototoxicity against HepG2 and Huh-7 cells, (IC50 range: 0.22.0 µM), these compounds lacked selectivity between GPC3-overexpressed and GPC3-negative cells because they also showed considerable phototoxicity against the cell lines with minimal GPC3 expression. Notably, compound 1 showed low phototoxicity and selectivity against all the tested cell lines (IC50 > 10 µM)." REF00289 DRG00034 Chlorin e6 Half Maximal Inhibitory Concentration (IC50) > 100 µM 24 h . . Human papillomavirus-related cervical adenocarcinoma GPC3-negative HeLa cell "Subsequently, the antiproliferative activities of the PS conjugates, including dark toxicity and phototoxicity (660 nM, light dose: 10 J/cm2), were evaluated. Dark toxicity refers to the toxicity of PS conjugates against cancer cells in the absence of light and can be regarded as a crucial measure of the safety profile, while phototoxicity is the most direct indicator of the PDT efficacy of PS. The results showed that the dark toxicity of all the compounds against the five cell lines was comparatively low, demonstrating that the PS conjugates exhibited a high safety index in the absence of light. Compound 8b exhibited the optimum tumor cell selectivity in terms of phototoxicity, with the IC50 values of 0.82 µM against HepG2 cells and 2.4 µM against Huh-7 cells, respectively, whereas its toxicity against GPC3-negative cell lines was >10 µM. Although compounds 8a and 8cd exhibited excellent phototoxicity against HepG2 and Huh-7 cells, (IC50 range: 0.22.0 µM), these compounds lacked selectivity between GPC3-overexpressed and GPC3-negative cells because they also showed considerable phototoxicity against the cell lines with minimal GPC3 expression. Notably, compound 1 showed low phototoxicity and selectivity against all the tested cell lines (IC50 > 10 µM)." REF00289 DRG00034 Chlorin e6 Half Maximal Inhibitory Concentration (IC50) > 100 µM 24 h . . Invasive breast carcinoma GPC3 negative MCF7 cell "Subsequently, the antiproliferative activities of the PS conjugates, including dark toxicity and phototoxicity (660 nM, light dose: 10 J/cm2), were evaluated. Dark toxicity refers to the toxicity of PS conjugates against cancer cells in the absence of light and can be regarded as a crucial measure of the safety profile, while phototoxicity is the most direct indicator of the PDT efficacy of PS. The results showed that the dark toxicity of all the compounds against the five cell lines was comparatively low, demonstrating that the PS conjugates exhibited a high safety index in the absence of light. Compound 8b exhibited the optimum tumor cell selectivity in terms of phototoxicity, with the IC50 values of 0.82 µM against HepG2 cells and 2.4 µM against Huh-7 cells, respectively, whereas its toxicity against GPC3-negative cell lines was >10 µM. Although compounds 8a and 8cd exhibited excellent phototoxicity against HepG2 and Huh-7 cells, (IC50 range: 0.22.0 µM), these compounds lacked selectivity between GPC3-overexpressed and GPC3-negative cells because they also showed considerable phototoxicity against the cell lines with minimal GPC3 expression. Notably, compound 1 showed low phototoxicity and selectivity against all the tested cell lines (IC50 > 10 µM)." REF00289 DRG00034 Chlorin e6 Half Maximal Inhibitory Concentration (IC50) > 100 µM 24 h . . Adult hepatocellular carcinoma GPC3-positive Huh-7 cell "Subsequently, the antiproliferative activities of the PS conjugates, including dark toxicity and phototoxicity (660 nM, light dose: 10 J/cm2), were evaluated. Dark toxicity refers to the toxicity of PS conjugates against cancer cells in the absence of light and can be regarded as a crucial measure of the safety profile, while phototoxicity is the most direct indicator of the PDT efficacy of PS. The results showed that the dark toxicity of all the compounds against the five cell lines was comparatively low, demonstrating that the PS conjugates exhibited a high safety index in the absence of light. Compound 8b exhibited the optimum tumor cell selectivity in terms of phototoxicity, with the IC50 values of 0.82 µM against HepG2 cells and 2.4 µM against Huh-7 cells, respectively, whereas its toxicity against GPC3-negative cell lines was >10 µM. Although compounds 8a and 8cd exhibited excellent phototoxicity against HepG2 and Huh-7 cells, (IC50 range: 0.22.0 µM), these compounds lacked selectivity between GPC3-overexpressed and GPC3-negative cells because they also showed considerable phototoxicity against the cell lines with minimal GPC3 expression. Notably, compound 1 showed low phototoxicity and selectivity against all the tested cell lines (IC50 > 10 µM)." REF00289 DRG00003 Fluorouracil Half Maximal Lethal Concentration (IC50) = 100 nM . . . Colon adenocarcinoma HCT 15 cell . REF102292 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 nM . . . Hepatoma SK-HEP1 cell . REF102292 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 nM . . . Invasive breast carcinoma MCF-7 cell . REF102292 DRG00003 Fluorouracil Half Maximal Lethal Concentration (IC50) = 100 nM . . . Pancreatic ductal adenocarcinoma BxPC-3 cell . REF102292 DRG00003 Fluorouracil Half Maximal Lethal Concentration (IC50) = 100 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF102292 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 nM . . . Prostate carcinoma PC-3 cell . REF102292 DRG00003 Fluorouracil Half Maximal Lethal Concentration (IC50) = 100 nM . . . Prostate carcinoma DU145 cell . REF102292 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Prostate carcinoma PC-3 cell . REF101305 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Prostate carcinoma DU145 cell . REF101305 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 100 nM . . . Ovarian adenocarcinoma A2780-1A9 cell . REF102139 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Chronic myeloid leukemia K562 cell . REF101891 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Normal HMEC-1 cell . REF101889 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Normal MRC5 cell . REF101831 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 100 nM . . . Glioblastoma SF-295 cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 100 nM . . . Renal carcinoma RXF 393 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Endocervical adenocarcinoma HeLa cell . REF101492 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Hepatoblastoma Hep-G2 cell . REF101492 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Lung adenocarcinoma A-549 cell . REF101492 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 100 nM . . . Astrocytoma SF268 cell . REF101480 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Colon cancer HT29 cell . REF101373 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Endometrial adenocarcinoma Ishikawa cell . REF101327 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Invasive breast carcinoma T-47D cell . REF101137 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Lung small cell carcinoma NCI-H187 cell . REF101064 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 100 nM . . . Chronic myeloid leukemia K562 cell . REF100902 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 100 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100680 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 100 nM . . . Colon cancer HT29 cell . REF100680 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 100 nM . . . Lung adenocarcinoma A-549 cell . REF100680 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Acute myeloid leukemia HL-60 cell . REF100638 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100582 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Colon adenocarcinoma DLD-1 cell . REF100582 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Renal carcinoma UO-31 cell . REF100582 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Melanoma B16 cell . REF100541 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100471 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Invasive breast carcinoma MCF-7 cell . REF100471 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Colon carcinoma HCT 116 cell . REF100447 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101731 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Invasive breast carcinoma MCF-7 cell . REF101442 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Promyelocytic leukemia NB-4 cell . REF100691 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Hepatoma Bel-7402 cell . REF100611 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Chronic myeloid leukemia K562 cell . REF102440 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Endocervical adenocarcinoma HeLa cell . REF100651 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 100 nM . . . Lung adenocarcinoma A-549 cell . REF100519 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 100 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100104 DRG00003 Fluorouracil Half Maximal Lethal Concentration (IC50) = 100 uM . . . Colon carcinoma HCT 116 cell . REF102277 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 uM . . . Glioblastoma SF-295 cell . REF102277 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 uM . . . Hepatoma SK-HEP1 cell . REF102277 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 uM . . . Invasive breast carcinoma MCF-7 cell . REF102277 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 uM . . . Lung large cell carcinoma NCI-H460 cell . REF102277 DRG00003 Fluorouracil Half Maximal Lethal Concentration (IC50) = 100 uM . . . Lung small cell carcinoma DMS 114 cell . REF102277 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 100 uM . . . Lung small cell carcinoma DMS 114 cell . REF102277 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 uM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF102277 DRG00003 Fluorouracil Half Maximal Lethal Concentration (IC50) = 100 uM . . . Pancreatic ductal adenocarcinoma BxPC-3 cell . REF102277 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 uM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF102277 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 uM . . . Prostate carcinoma PC-3 cell . REF102277 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 100 uM . . . Small cell lung carcinoma NCI-H69 cell . REF102277 DRG00003 Fluorouracil Half Maximal Lethal Concentration (IC50) = 100 uM . . . Small cell lung carcinoma NCI-H69 cell . REF102277 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 100 uM . . . Melanoma UACC-257 cell . REF100098 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 100 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101605 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 100 uM . . . Chronic myeloid leukemia K562 cell . REF101566 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 100 uM . . . Clear cell renal cell carcinoma Caki-1 cell . REF101566 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 100 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF101566 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 100 uM . . . Leukemia SR cell . REF101566 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 100 uM . . . Lung adenocarcinoma A-549 cell . REF101566 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 100 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101566 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 100 uM . . . Plasma cell myeloma RPMI-8226 cell . REF101566 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 100 uM . . . Prostate carcinoma DU145 cell . REF101566 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 100 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101566 DRG00013 Gemcitabine Tumor Growth Inhibition value (TGI) = 100 uM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF102277 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 100 uM . . . T acute lymphoblastic leukemia CCRF-CEM/ara-C cell . REF100023 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 100 uM . . . Normal MT4 cell . REF100057 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 100 uM . . . Renal carcinoma UO-31 cell . REF102249 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 100 uM . . . Invasive breast carcinoma T-47D cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 100 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 100 uM . . . Prostate carcinoma PC-3 cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 100 uM . . . Prostate carcinoma DU145 cell . REF102222 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Endocervical adenocarcinoma HeLa cell . REF102232 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Acute myeloid leukemia HL-60 cell . REF102089 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Acute monocytic leukemia THP-1 cell . REF101130 DRG00004 Gemfibrozil Half Maximal Effective Concentration (EC50) > 1000 nM . 1000 nM . . . "Moreover, we did not observe any activation potency of GFZ on GLP-1 receptor at the highest concentration tested (1000 nM), indicating that the GLP-1 receptor activation potency of 1ai was attributed to the peptide sequence of 1ai instead of GFZ." REF00109 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . EBV-related Burkitt lymphoma Raji cell . REF100812 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Prostate carcinoma DU145 cell . REF100775 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Colon carcinoma HCT 116 cell . REF100621 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Invasive breast carcinoma MCF-7 cell . REF101979 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Hepatoblastoma Hep-G2 cell . REF101823 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Amelanotic melanoma A-375 cell . REF101345 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101300 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Prostate carcinoma PC-3 cell . REF101177 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Normal HEK293 cell . REF101089 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1000 nM . . . Gastric carcinoma NUGC-3 cell . REF101084 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Prostate carcinoma DU145 cell . REF100951 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Melanoma M14 cell . REF100891 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Endocervical adenocarcinoma HeLa cell . REF100748 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 1000 nM . . . Chronic myeloid leukemia K562 cell . REF100707 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Chronic myeloid leukemia K562 cell . REF100610 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Non-small cell lung carcinoma HOP-62 cell . REF100593 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Colon adenocarcinoma LoVo cell . REF100290 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 1000 nM . . . Renal carcinoma UO-31 cell . REF100274 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102148 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Lymphoblastic leukemia L1210 cell . REF100172 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Lung adenocarcinoma NCI-H23 cell . REF100061 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Chronic myeloid leukemia K562 cell . REF102375 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 1000 nM . . . Renal carcinoma RXF 393 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 1000 nM . . . Colon cancer HT29 cell . REF101159 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 101 uM . . . Chronic myeloid leukemia K562 cell . REF100634 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 104.5 uM . . . Lung adenocarcinoma A-549 cell . REF102462 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 105 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100521 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 107.15 nM . . . Non-small cell lung carcinoma HOP-62 cell . REF100848 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 108 ug/mL . . . Melanoma M21 cell . REF100157 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 109 nM . . . Colon adenocarcinoma HCT 15 cell . REF101326 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 109 ug/mL . . . Melanoma M21 cell . REF100157 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 109.5 nmol/L 72 h . . Breast adenocarcinoma MDA-MB-231 cell "Besides, the combination of DTX and CTCE showed a substantially greater cytotoxicity, with an approximate 2 folds reduction (67.9 nmol/L) in half-maximal inhibitory concentration (IC50) compared to DTX alone. What's more, CTCEDTX NPs retained a greater cytotoxicity (IC50 = 88.5 nmol/L) than ScDTX NPs (IC50 = 169.5 nmol/L), which meant CXCR4 antagonist peptide could work as a sensitizer to DTX. The slightly higher IC50 value of CTCEDTX NPs than that of DTX + CTCE group may attribute to the incomplete disassembly of nanostructures. Meanwhile, consistent with previous reports14, the CXCR4 antagonist peptide and scramble peptide didn't not show any cytotoxicity to 4T1 cell at low concentration. We also tested the cytotoxicity of the formulations to another CXCR4 high expression (MDA-MB-231) and CXCR4 low expression (HepG2) cell lines and calculated the IC50. In MDA-MB-231 cell line, the IC50 of CTCEDTX NPs (99.2 nmol/L) was significantly lower than that of DTX (135.8 nmol/L) and ScDTX NPs (250.1 nmol/L), which was consist with the tendency of formulations to 4T1 cell line. In comparison, in HepG2 cell line, the IC50 of CTCEDTX NPs (166.8 nmol/L) was higher than that of DTX (109.5 nmol/L). The results further proved that the recognition of CTCEDTX NPs with CXCR4 could enhance the cytotoxicity to tumor cells. These results demonstrated that CTCE peptide enhanced the chemosensitivity of cancer cell toward DTX but possessed with no direct toxicity." REF00279 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 109.65 nM . . . Colon adenocarcinoma HCT 15 cell . REF100123 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 109.65 nM . . . Prostate carcinoma DU145 cell . REF100589 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 11 µM 36 h . . Endocervical adenocarcinoma HeLa cell "Doxorubicin (DOX) is one of the most effective anticancer drugs and has been successfully used in clinical practice. However, DOX cannot differentiate between cancer cells and normal cells, which may induce unwanted side effects and severe toxicity. Compared with traditional small-molecule anticancer drugs, the peptide-drug conjugates (PDCs) have enhanced targeting specificity and water solubility. Based on these advantages, to further explore the function of 10a, we designed and prepared a anticancer PDC drug compound RGD-GFLG-DOX containing the tetrapeptide linker Gly-Phe-Leu-Gly, which can be cleaved in presence of cathepsin B, a highly upregulated enzyme in malignant tumors, to release the drug. RGD-GFLG was synthesized as a control. The inhibitory effects of RGD-GFLG-DOX on cancer cell lines were assessed using cytotoxicity assay. Specifically, the effects of RGD-GFLG-DOX were evaluated on integrin αvβ3-positive cancer cell lines, including A549 and U87MG cells, integrin αvβ3-negative cancer cell lines such as HeLa and MCF-7 cells, as well as normal cell lines, namely LO2 and MIHA cells. RGD-GFLG-DOX exhibited a lower cytotoxicity on HeLa, MCF-7, LO2 and MIHA cells, but a stronger cytotoxicity than DOX on A549 and U87MG cells. For comparison, RGD-GFLG demonstrated minimal cytotoxicity. In addition, the cytotoxicity of RGD-GFLG-DOX with various concentrations (040µM) on A549 and U87MG cells was studied. The results showed that the cytotoxicity of RGD-GFLG-DOX on A549 and U87MG cells was dose-dependent. These indicate that RGD-GFLG-DOX has a good specificity and inhibitory activity toward integrin αvβ3-overexpressed A549 and U87MG cells." REF00270 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 11 ng/mL . . . Chronic myeloid leukemia K562 cell . REF100656 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 11 ng/mL . . . Prostate carcinoma PC-3 cell . REF100266 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 11 ng/mL . . . Ileocecal adenocarcinoma HCT-8 cell . REF100401 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 11 nM . . . Colon cancer HT29 cell . REF101625 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 11 nM . . . Colon adenocarcinoma SW480 cell . REF100948 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 11 nM . . . Colon adenocarcinoma HCT 15 cell . REF100724 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 11 nM . . . Lung adenocarcinoma A-549 cell . REF101812 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 11 nM . . . Invasive breast carcinoma MCF-7 cell . REF102124 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 11 nM . . . Hepatoma Bel-7402 cell . REF101877 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 11 uM . . . Lung large cell carcinoma NCI-H460 cell . REF101042 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 11 uM . . . Normal HEK293 cell . REF102504 DRG00043 JH-VII-139-1 Half Maximal growth inhibition concentration (GI50) = 11±0.3 µM . . . Breast adenocarcinoma MDA-MB-231 cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 11.1 ug/mL . . . Cutaneous melanoma SK-MEL-28 cell . REF102014 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 11.1 uM . . . Lung adenocarcinoma A-549 cell . REF102218 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 11.17 uM . . . Invasive breast carcinoma T-47D cell . REF101401 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 11.2 nM . . . Invasive breast carcinoma MCF-7 cell . REF101648 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 11.2 uM . . . Endocervical adenocarcinoma HeLa cell . REF101105 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 11.3 nM . . . Hypopharyngeal squamous cell carcinoma FaDu cell . REF100312 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 11.3 uM . . . Lung adenocarcinoma A-549 cell . REF102231 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 11.3 uM . . . Invasive breast carcinoma MCF-7 cell . REF101541 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 11.32 uM . . . Invasive breast carcinoma MCF-7 cell . REF101546 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 11.4 nM . . . Invasive breast carcinoma MCF-7 cell . REF101571 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 11.4 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102152 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 11.4 uM . . . Lung adenocarcinoma A-549 cell . REF102401 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 11.46 nM . . . Invasive breast carcinoma MCF-7 cell . REF101501 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 11.5 nM . . . Colon carcinoma HCT 116 cell . REF101500 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 11.54 uM . . . Colon carcinoma HCT 116 cell . REF102304 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 11.58 uM . . . Amelanotic melanoma A-375 cell . REF102275 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 11.6 ng/ml . . . Colon cancer HT29 cell . REF100184 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 11.62 uM . . . Lung adenocarcinoma A-549 cell . REF101458 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 11.67 uM . . . Invasive breast carcinoma MCF-7 cell . REF101023 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 11.83 uM . . . Bladder carcinoma T24 cell . REF102424 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 11.86 uM . . . Lung adenocarcinoma A-549 cell . REF102467 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 11.87 uM . . . Colon adenocarcinoma HCT 15 cell . REF102441 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 11.9 uM . . . Bone marrow neuroblastoma SH-SY5Y cell . REF102399 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 11.9 uM . . . Prostate carcinoma DU145 cell . REF100465 DRG00101 Vidarabine Half Maximal Inhibitory Concentration (IC50) = 11.9 uM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF100055 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF101240 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . Colon adenocarcinoma SW620 cell . REF101787 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF101645 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 110 nM . . . Prostate carcinoma DU145 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . Breast ductal carcinoma BT-549 cell . REF101137 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101074 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 110 nM . . . Invasive breast carcinoma ZR-75-1 cell . REF100971 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 110 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100849 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 110 nM . . . Melanoma SK-MEL-2 cell . REF100653 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . Laryngeal carcinoma HEp-2 cell . REF101927 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . Breast adenocarcinoma SK-BR-3 cell . REF101083 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Growth Inhibition (GI50) = 110 nM . . . Gastric epithelial carcinoma MKN-28 cell . REF102448 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . Stomach adenocarcinoma BGC-823 cell . REF100651 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . Colon adenocarcinoma HCC 2998 cell . REF100270 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . Endocervical adenocarcinoma HeLa cell . REF100068 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 110 nM . . . Lung adenocarcinoma A-549 cell . REF100742 DRG00011 Doxorubicin Tumor volume = 1100 mm3 24 days 6 mg/kg BALB/c male nude mice inoculated with high metastatic HCCLM3-LUC cells model. Adult hepatocellular carcinoma HCCLM3-Luc cell "The antitumor activity of CSNs was assessed in BALB/c male nude mice inoculated with high metastatic HCCLM3-LUC cells. As can be seen from Figure 3A,B, DOX caused severe systemic toxicity and a significant weight loss (up to 24.38%) during treatment. In contrast, there was little change in body weight for PDC- and CSNs-treated mice. Tumor progression was greatly suppressed in the CSNs group, as observed by bioluminescence. Tumor tissue images collected on day 27 confirmed that nude mice treated with CSNs bore the smallest tumors." REF00112 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 111 uM . . . Normal Vero cell . REF100053 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 112 nM . . . Melanoma UACC-375 cell . REF100237 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 112.23 uM . . . Lung adenocarcinoma A549/TR cell . REF101706 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 114 nM . . . Prostate carcinoma PC-3 cell . REF101228 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 115 ug/mL . . . Melanoma M21 cell . REF100157 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 116.54 uM . . . Normal CCD-18Co cell . REF101803 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 117 nM . . . Melanoma SK-MEL-2 cell . REF100732 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 117 ug/mL . . . Melanoma M21 cell . REF100157 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 117.5±8.6 nM 24 h . . Normal C-26 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 118.8±25.0 nM 24 h . . Amelanotic melanoma M24 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 119 ug/mL . . . Melanoma M21 cell . REF100157 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 119.84 uM . . . Normal MT-2 cell . REF100049 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 12 ng/ml . . . Skin squamous cell carcinoma A431 cell . REF100192 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 12 ng/mL . . . Sezary syndrome H9 cell . REF102076 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Prostate carcinoma PC-3 cell . REF100917 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Invasive breast carcinoma MCF-7 cell . REF100751 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Breast adenocarcinoma MDA-MB-361 cell . REF100287 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Glioblastoma T98G cell . REF101859 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Lung adenocarcinoma A-549 cell . REF101830 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101140 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 12 nM . . . Invasive breast carcinoma MCF-7 cell . REF100941 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Acute myeloid leukemia HL-60 cell . REF101915 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 12 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100369 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Astrocytoma U-373MG ATCC cell . REF100222 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Lymphoblastic leukemia L1210 cell . REF100172 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 12 nM . . . Normal MT4 cell . REF100076 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF102390 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Invasive breast carcinoma MCF-7 cell . REF102131 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 12 nM . . . Endocervical adenocarcinoma HeLa cell . REF101423 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 12 uM . . . Bone marrow neuroblastoma SH-SY5Y cell . REF102388 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 12 uM . . . Prostate carcinoma PC-3 cell . REF100465 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 12 uM . . . Uterine sarcoma MES-SA cell . REF100372 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 12 uM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF102411 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 12 uM . . . Erythroleukemia HEL cell . REF100059 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 12 uM . . . Normal MT4 cell . REF100078 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 12.06 nM . . . Invasive breast carcinoma MCF-7 cell . REF101760 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 12.1 ng/mL . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100323 DRG00011 Doxorubicin Maximal Effective Concentration (EC50) = 12.1 nM . . . Normal WI-38 cell . REF101770 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 12.1 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101662 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 12.1 nM . . . Colon adenocarcinoma SW480 cell . REF101124 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 12.1 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102014 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 12.1 uM . . . Prostate carcinoma LNCaP cell . REF101360 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 12.11 uM . . . Endocervical adenocarcinoma HeLa cell . REF102341 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 12.2 ng/ml . . . Renal carcinoma A498 cell . REF100249 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 12.2 uM . . . Colon adenocarcinoma LoVo cell . REF100962 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 12.21 uM . . . Chronic myeloid leukemia K562 cell . REF101706 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 12.23 uM . . . Cervical carcinoma L02 cell . REF101446 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 12.25±0.13 nM 24 h . . Glioblastoma U-87MG cell "Furthermore, it was also observed that PDC shows time-dependent cytotoxicity against U87MG cells, as at 12 h drug treatment. PDC shows a slightly lower inhibitory effect on cell survival (EC50 = 25.82 0.31 nM) than PTX alone (EC50 = 12.25 0.13 nM), and CPPSA alone shows higher EC50 = 54.37 0.24 in U87MG cells. Besides this, it was previously observed that CPP-treated healthy VERO cells showed 88.05 0.86% viable cells even using 10 µM concentration, indicating the specificity of CPP for glioblastoma cells. However, at 24 h incubation period, our PDC shows a significantly enhanced cell survival inhibitory effect with EC50 = 8.32 0.09 nM, suggesting the delayed effect of PDC because of the time required for the intracellular pH to cause maximal cleavage of PTX from the PDC. Moreover, it also shows that CPPSA has a lower cytotoxicity effect on glioblastoma cells compared with PTX alone and PDC, indicating its specificity as a carrier and selectivity for integrin receptors overexpressed on the cell surface. Additionally, we have also studied the potential of our novel-designed PDC to internalize into PTX-resistant glioblastoma (U87MG-PR) cells to show cytotoxic activity upon intracellular cleavage of PTX from CPP. The data presented in Figure 3b reveal approximately 15% viability increases in U87MG-PR cells compared with parent U87MG cells. It can be seen in the inset in Figure 3b that PTX alone (EC50 = 41.3 1.5 nM) showed significantly 2-fold reduced cytotoxic activity in U87MG-PR cells in comparison with our novel-designed PDC having EC50 = 20.55 1.02 nM. It was also observed in Figure 3b that at lower concentrations (010 nM) the viable cell count was 75%; however, it significantly decreased to 20% viability with an increase in concentration (40 nM) of the test samples, highlighting the dose-dependent cytotoxicity behavior of PDC in a 24 h incubation period." REF00266 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 12.27 uM . . . Invasive breast carcinoma MCF-7 cell . REF102218 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 12.3 nM . . . Ovarian endometrioid adenocarcinoma A2780S cell . REF101544 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 12.3 uM . . . Colon adenocarcinoma SW480 cell . REF101379 DRG00010 Daunorubicin Half Maximal Infective Dose (ID50) = 12.5 ng/ml . . . Endocervical adenocarcinoma HeLa cell . REF100020 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 12.5 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 12.5 nM . . . Invasive breast carcinoma T-47D cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 12.5 nM . . . Minimally invasive lung adenocarcinoma NCI-H322M cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 12.5 nM . . . Breast adenocarcinoma MDA-MB-468 cell . REF101624 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 12.5 uM . . . Hepatoma Bel-7402 cell . REF100620 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 12.5 uM . . . Hepatoblastoma Hep-G2 cell . REF101239 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 12.58925 uM . . . Cutaneous melanoma SK-MEL-5 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 12.58925 uM . . . Lung adenocarcinoma NCI-H23 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 12.58925 uM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 12.58925 uM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF100098 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 12.58925 uM . . . Melanoma LOX IMVI cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 12.58925 uM . . . Melanoma UACC-62 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 12.58925 uM . . . Pleural epithelioid mesothelioma NCI-H226 cell . REF100756 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 12.58925 uM . . . Astrocytoma U-251MG cell . REF102222 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 12.59 uM . . . Prostate carcinoma PC-3 cell . REF100902 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 12.59 uM . . . Renal adenocarcinoma ACHN cell . REF100587 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 12.6 nM . . . Ehrlich ascites carcinoma Ehrlich cell . REF100175 DRG00101 Vidarabine Half Maximal Infective Dose (ID50) = 12.7 uM . . . Lymphoma P388 cell . REF102027 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 12.8 uM . . . Bone marrow neuroblastoma SH-SY5Y cell . REF102225 DRG00023 Tesaglitazar Adiponectin level = 120 µg/mL Every day 2.5 μM db/db mice model. . . "Whereas in the vehicle/untreated mice, the HbA1C values increased by approximately 2%, a graduated reduced increase was seen for [F7, P34]-NPY (2), peptide conjugate (3), and tesa (Figure 8A). Body temperature, which decreased to 35 C in the vehicle/untreated db/db controls, was normalized to 36 C in all of the treated mice including the mice treated with [F7, P34]-NPY (2) (Figure 8B). Treatment with tesa and tesa-NPY (3) led to normalization of the plasma concentration of ketone bodies and adiponectin, whereas [F7, P34]-NPY (2) and vehicle/untreated showed no effect (Figure 8C/E). Treatment had no major influence on the insulin and Mcp-1 levels (Figure 8D/G). The serum leptin concentration was reduced in the mice treated with tesa, whereas no reduction was detectable in all of the other treated mice (Figure 8F)." REF00088 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Colon carcinoma HCT 116 cell . REF101484 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Colon cancer HT29 cell . REF100742 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Lung carcinoma LX-1 cell . REF100353 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Colon cancer HT29 cell . REF101951 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Lung adenocarcinoma A-549 cell . REF101926 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Endocervical adenocarcinoma HeLa S3 cell . REF101725 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Normal MRC5 cell . REF101667 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 120 nM . . . Gliosarcoma SF539 cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 120 nM . . . Melanoma UACC-257 cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 120 nM . . . Colon cancer HT29 cell . REF101480 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Prostate carcinoma DU145 cell . REF101305 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Invasive breast carcinoma MCF-7 cell . REF101297 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 120 nM . . . Colon adenocarcinoma LoVo cell . REF101269 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Colon adenocarcinoma SW620 cell . REF101217 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Colon adenocarcinoma LoVo cell . REF101011 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 120 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100653 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Hepatoblastoma Hep-G2 cell . REF100370 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Chronic myeloid leukemia K562 cell . REF100301 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Prostate carcinoma PC-3 cell . REF101927 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Lymphoblastic leukemia L1210 cell . REF101016 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF101607 DRG00081 Cytarabine Half Maximal Growth Inhibition (GI50) = 120 nM . . . Colon carcinoma HCT 116 cell . REF102266 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 120 nM . . . Invasive breast carcinoma MCF-7 cell . REF102393 DRG00005 Primaquine Half Maximal Cytotoxicity Concentration (CC50) = 120.03 uM . . . Hepatoblastoma Hep-G2 cell . REF102437 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 120.5 nM . . . Normal R2 cell . REF101187 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 121 nM . . . Normal R2 cell . REF100994 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 121 ug/mL . . . Melanoma M21 cell . REF100157 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 123 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101729 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 123 nM . . . Lymphoma P388/ADR cell . REF100521 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 123 uM . . . Normal MT-2 cell . REF102034 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 123.03 nM . . . Renal carcinoma A498 cell . REF101977 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 124 nM . . . Lung adenocarcinoma A-549 cell . REF101460 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 124 nM . . . Small cell lung carcinoma DMS-79 cell . REF102131 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 125 nM . . . Lymphoblastic leukemia L1210 cell . REF102085 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 125 nM . . . Renal carcinoma UO-31 cell . REF101860 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 125.89 nM . . . Small cell lung carcinoma SHP-77 cell . REF100517 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 125.89 nM . . . Astrocytoma SF268 cell . REF102222 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 125.89254 uM . . . Astrocytoma SNB-19 cell . REF100098 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 126 nM . . . Colon adenocarcinoma HCC 2998 cell . REF100987 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 126 nM . . . Glioblastoma SNB-75 cell . REF100987 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 126 uM . . . Chronic myeloid leukemia K562 cell . REF102320 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) = 126 uM . . . Normal Vero cell . REF102154 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 126 uM . . . Normal Vero cell . REF100107 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 126.4±53.7 nM 24 h . . Glioblastoma U-87MG cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 128 nM . . . Astrocytoma U-251MG cell . REF101233 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 128.7 uM . . . Laryngeal carcinoma HEp-2 cell . REF102141 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 128.82 uM . . . Bladder carcinoma 5637 cell . REF102431 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 129 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100521 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 13 nM . . . Invasive breast carcinoma MCF-7 cell . REF101533 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 13 nM . . . Amelanotic melanoma A-375 cell . REF101421 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 13 nM . . . Acute myeloid leukemia HL-60 cell . REF100621 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 13 nM . . . Lymphoma P388 cell . REF100331 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 13 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101633 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 13 nM . . . Minimally invasive lung adenocarcinoma NCI-H322M cell . REF100987 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 13 nM . . . Lung adenocarcinoma A-549 cell . REF101292 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 13 nM . . . Endocervical adenocarcinoma HeLa cell . REF102062 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 13 nM . . . Acute myeloid leukemia HL-60 cell . REF102506 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 13 nM . . . Uterine sarcoma MES-SA cell . REF102115 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 13 nM . . . Invasive breast carcinoma MCF-7 cell . REF101333 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 13 uM . . . Colon carcinoma HCT 116 cell . REF102483 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 13 uM . . . Endocervical adenocarcinoma HeLa cell . REF101448 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 13 uM . . . Sezary syndrome H9 cell . REF102212 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 13 uM . . . Colon carcinoma HCT 116 cell . REF102411 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 13 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102064 DRG00043 JH-VII-139-1 Half Maximal Inhibitory Concentration (IC50) = 13±0.3 µM 48 h . . Chronic myeloid leukemia K562 cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 13.01 uM . . . Lung adenocarcinoma A-549 cell . REF101019 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 13.05 uM . . . Lung adenocarcinoma A-549 cell . REF100667 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 13.09 uM . . . Anaplastic thyroid carcinoma SW-1736 cell . REF102218 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 13.1 nM . . . Colon adenocarcinoma SW620 cell . REF101737 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 13.1 uM . . . Colon adenocarcinoma LoVo cell . REF101011 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 13.15 uM . . . Lung adenocarcinoma NCI-H23 cell . REF101566 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 13.18 uM . . . Osteosarcoma U2OS cell . REF102166 DRG00224 Pemetrexed Half Maximal Inhibitory Concentration (IC50) = 13.2 nM . . . Normal R2 cell . REF101179 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 13.2 uM . . . Colon cancer HT29 cell . REF102304 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 13.23 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101711 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 13.24 uM . . . Prostate carcinoma DU145 cell . REF101082 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 13.24 uM . . . Hepatoblastoma Hep-G2 cell . REF102275 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 13.3 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100258 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 13.3 uM . . . Ileocecal adenocarcinoma HCT-8 cell . REF101128 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 13.4 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101593 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 13.46 uM . . . Colon carcinoma HCT 116 cell . REF100756 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 13.5 nM . . . Lung adenocarcinoma A-549 cell . REF101462 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 13.5 uM . . . Invasive breast carcinoma MCF-7 cell . REF102360 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 13.5 uM . . . Colon adenocarcinoma HCC 2998 cell . REF102272 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 13.6 nM . . . Colon adenocarcinoma SW480 cell . REF102166 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 13.6 uM . . . Chronic myeloid leukemia K562 cell . REF101025 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 13.62 uM . . . Invasive breast carcinoma MCF-7 cell . REF101555 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 13.64 uM . . . Lung adenocarcinoma A-549 cell . REF101504 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 13.7 nM . . . Lung adenocarcinoma A-549 cell . REF101727 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 13.7 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101530 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 13.77 uM . . . Prostate carcinoma PC-3 cell . REF102166 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 13.8 ng/mL . . . Invasive breast carcinoma MCF-7 cell . REF101945 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 13.8 uM . . . Colon carcinoma HCT 116 cell . REF101834 DRG00011 Doxorubicin Half Maximal Cytotoxicity Concentration (CC50) = 13.9 uM . . . Normal MCF-10A cell . REF101882 DRG00407 Combretastatin A4 Half Maximal Cytotoxicity Concentration (CC50) = 13.9 uM . . . Normal HT22 cell . REF102502 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 13.93 uM . . . Colon cancer HT29 cell . REF102218 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Endocervical adenocarcinoma HeLa cell . REF101613 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Chronic myeloid leukemia K562 cell . REF101285 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Colon carcinoma HCT 116 cell . REF100756 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Hepatoblastoma Hep-G2 cell . REF100650 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101873 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101709 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Gastric carcinoma SGC-7901 cell . REF101678 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Lung adenocarcinoma A-549 cell . REF101662 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Invasive breast carcinoma MCF-7 cell . REF101420 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Endocervical adenocarcinoma HeLa cell . REF100939 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 130 nM . . . Colon carcinoma HCT 116 cell . REF100795 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Prostate carcinoma DU145 cell . REF100573 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 130 nM . . . Normal Vero cell . REF101568 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 130 uM . . . Acute myeloid leukemia HL-60 cell . REF100470 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 130.7 uM . . . Normal Vero cell . REF100053 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 131.83 nM . . . Invasive breast carcinoma MCF-7 cell . REF100848 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 133 nM . . . Colon cancer HT29 cell . REF100156 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 134 nM . . . Prostate carcinoma DU145 cell . REF101729 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 135 uM . . . Invasive breast carcinoma MCF-7 cell . REF100280 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 135.8 nmol/L 72 h . . Breast adenocarcinoma MDA-MB-231 cell "Besides, the combination of DTX and CTCE showed a substantially greater cytotoxicity, with an approximate 2 folds reduction (67.9 nmol/L) in half-maximal inhibitory concentration (IC50) compared to DTX alone. What's more, CTCEDTX NPs retained a greater cytotoxicity (IC50 = 88.5 nmol/L) than ScDTX NPs (IC50 = 169.5 nmol/L), which meant CXCR4 antagonist peptide could work as a sensitizer to DTX. The slightly higher IC50 value of CTCEDTX NPs than that of DTX + CTCE group may attribute to the incomplete disassembly of nanostructures. Meanwhile, consistent with previous reports14, the CXCR4 antagonist peptide and scramble peptide didn't not show any cytotoxicity to 4T1 cell at low concentration. We also tested the cytotoxicity of the formulations to another CXCR4 high expression (MDA-MB-231) and CXCR4 low expression (HepG2) cell lines and calculated the IC50. In MDA-MB-231 cell line, the IC50 of CTCEDTX NPs (99.2 nmol/L) was significantly lower than that of DTX (135.8 nmol/L) and ScDTX NPs (250.1 nmol/L), which was consist with the tendency of formulations to 4T1 cell line. In comparison, in HepG2 cell line, the IC50 of CTCEDTX NPs (166.8 nmol/L) was higher than that of DTX (109.5 nmol/L). The results further proved that the recognition of CTCEDTX NPs with CXCR4 could enhance the cytotoxicity to tumor cells. These results demonstrated that CTCE peptide enhanced the chemosensitivity of cancer cell toward DTX but possessed with no direct toxicity." REF00279 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 137 nM . . . Small cell lung carcinoma NCI-H69 cell . REF100351 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 14 mM . . . Colon adenocarcinoma DLD-1 cell . REF100298 DRG00011 Doxorubicin Median Toxic Dose (TD50) = 14 ng/ml . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF101705 DRG00012 Paclitaxel Half Maximal Lethal dose (LD50) = 14 ng/mL . . . Lymphoblastic leukemia L1210 cell . REF102080 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 14 nM . . . Lymphoma P388 cell . REF100681 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 14 nM . . . Lung adenocarcinoma A-549 cell . REF100327 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 14 nM . . . Uterine sarcoma MES-SA/Dx5 cell . REF100302 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 14 nM . . . Chronic myeloid leukemia K562 cell . REF101090 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 14 nM . . . Invasive breast carcinoma MCF-7 cell . REF101299 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 14 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100984 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 14 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100186 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 14 nM . . . Breast adenocarcinoma MDA-MB-468 cell . REF101549 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 14 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100071 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 14 nM . . . Normal MT-2 cell . REF100049 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 14 nM . . . Invasive breast carcinoma MCF-7 cell . REF102390 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 14 uM . . . Endocervical adenocarcinoma HeLa cell . REF101336 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 14 uM . . . Lung adenocarcinoma A-549 cell . REF101279 DRG00043 JH-VII-139-1 Half Maximal Inhibitory Concentration (IC50) = 14±0.8 µM 48 h . . Endocervical adenocarcinoma HeLa cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 14.04 uM . . . Mammary carcinoma 4T1 cell . REF101307 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 14.2 nM . . . Endocervical adenocarcinoma HeLa cell . REF102427 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 14.2 uM . . . Cervical carcinoma QGY-7703 cell . REF102416 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 14.2 uM . . . Invasive breast carcinoma MCF-7 cell . REF100841 DRG00011 Doxorubicin Half Maximal Infective Dose (ID50) = 14.2 uM . . . Breast carcinoma MCF7-VP cell . REF102057 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 14.2 uM . . . Renal adenocarcinoma ACHN cell . REF100560 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 14.2 uM . . . Normal NIH3T3 cell . REF102225 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 14.3 mM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102063 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 14.3 uM . . . Hepatoblastoma Hep-G2 cell . REF100716 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 14.3 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100077 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 14.4 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100312 DRG00107 Betulinic acid Half Maximal Effective Concentration (EC50) = 14.4 uM . . . Colon cancer HT29 cell . REF102361 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 14.5 nM . . . Invasive breast carcinoma MCF-7 cell . REF102292 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 14.5 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100481 DRG00019 Methotrexate Half Maximal Effective Dosage (ED50) = 14.5 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100225 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 14.66 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101458 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 14.7 uM . . . Normal COLO205 cell . REF101019 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 14.76 uM . . . Breast adenocarcinoma MDA-MB-468 cell . REF101380 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 14.76 uM . . . Normal MRC5 cell . REF101649 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 14.8 uM . . . Colon adenocarcinoma KM12 cell . REF102352 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 14.84 uM . . . Normal MRC5 cell . REF101982 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 14.9 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100721 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 140 nM . . . Glioblastoma A-172 cell . REF101975 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 140 nM . . . Invasive breast carcinoma MCF-7 cell . REF101684 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 140 nM . . . Chronic myeloid leukemia K562 cell . REF101645 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 140 nM . . . Cutaneous melanoma SK-MEL-5 cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 140 nM . . . Melanoma UACC-62 cell . REF101480 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 140 nM . . . Non-small cell lung carcinoma HOP-62 cell . REF101162 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 140 nM . . . Normal COLO205 cell . REF101162 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 140 nM . . . Cervical squamous cell carcinoma SiHa cell . REF101049 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 140 nM . . . Prostate carcinoma PC-3 cell . REF101128 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 140 nM . . . Normal CHO-VV 3-2 cell . REF100998 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 140 nM . . . Lymphoma P388 cell . REF100068 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 140 nM . . . Hepatocellular carcinoma SMMC-7721 cell . REF102197 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 141.25 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100848 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 142 nM . . . Invasive breast carcinoma MCF-7 cell . REF101561 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 142.6 uM . . . Endocervical adenocarcinoma HeLa cell . REF101124 DRG00012 Paclitaxel Half Maximal Lethal Concentration (IC50) = 145 nM . . . Normal COLO205 cell . REF100197 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 146.2 uM . . . Colon cancer HT29 cell . REF102462 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 148 nM . . . Colon carcinoma HCT 116 cell . REF102120 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 148.4 uM . . . Normal HEK293 cell . REF101583 DRG00009 Camptothecin Half Maximal Cytotoxicity Concentration (CC50) = 15 nM . . . Prostate carcinoma DU145 cell . REF102257 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Acute monocytic leukemia U-937 cell . REF100522 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Lymphoblastic leukemia L1210 cell . REF100211 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Invasive breast carcinoma MCF-7 cell . REF101761 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Lymphoma P388 cell . REF100383 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100243 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 15 nM . . . Colon cancer HT29 cell . REF100659 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Lung large cell carcinoma NCI-H1299 cell . REF100559 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100542 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 15 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100344 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Ovarian carcinoma OV-1063 cell . REF100256 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 15 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100330 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Colon adenocarcinoma SW480 cell . REF100176 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100917 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 15 nM . . . Sezary syndrome H9 cell . REF102069 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 15 nM . . . Normal MT4 cell . REF100066 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 15 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF102442 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 15 nM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF102315 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 15 pM . . . Prostate carcinoma PC-3 cell . REF100391 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 15 uM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF102483 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 15 uM . . . Invasive breast carcinoma MCF-7 cell . REF102271 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 15 uM . . . Colon adenocarcinoma DLD-1 cell . REF100120 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 15 uM . . . Colon adenocarcinoma Caco-2 cell . REF102225 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 15 uM . . . Prostate carcinoma PC-3 cell . REF100119 DRG00043 JH-VII-139-1 Tumor Growth Inhibition value (TGI) = 15±0.5 µM . . . Chronic myeloid leukemia K562 cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 15.07 uM . . . Lung adenocarcinoma A-549 cell . REF101052 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 15.2 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101857 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 15.29 uM . . . Colon adenocarcinoma SW620 cell . REF102495 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 15.3 nM . . . Astrocytoma SF268 cell . REF100658 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 15.47 uM . . . Breast carcinoma Bcap37 cell . REF102360 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 15.5 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100316 DRG00019 Methotrexate Half Maximal Effective Dosage (ED50) = 15.5 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100218 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 15.6 nM . . . Chronic myeloid leukemia K562 cell . REF100293 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 15.65 uM . . . Prostate carcinoma DU145 cell . REF101023 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 15.73 nM . . . Ovarian endometrioid adenocarcinoma A2780S cell . REF101634 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 15.8 nM . . . Lung adenocarcinoma A-549 cell . REF101104 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 15.8 nM . . . Prostate carcinoma TRAMP-C2H cell . REF100525 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 15.8 nM . . . Renal carcinoma RXF 393 cell . REF101860 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 15.8±0.7 µM 48 h . . Invasive breast carcinoma of no special type MCF7/C4 cell "MTT assay was preformed to measure the in vitro cytotoxicities of the compounds against cancer cells (HCT-116, SGC-7901, MCF-7, HCT-116/CPT, SGC-7901/CPT and MCF-7/C4) and benign cells (NCM460, GES-1 and LO2). As present in Table 1, all the peptides (Kb-C01, 0207) exhibited certain selective anticancer activities, which are comparable to their parent counterpart KM8-Aib. The target PDCs (Kb-CC01, 0207) were further obtained by coupling the peptides with CPT, displaying markedly improved antiproliferative activities and selectivities against cancer cell lines over CPT. Studies have revealed that cancer cell membranes are negatively charged due to the presence of substantial amounts of acid phospholipids. Therefore, positively charged CAPs are capable of binding to cancer cell surface through electrostatic interactions, making them specific to cancer cells. In this project, since the PDCs were composed of CAP KM8-Aib and CPT, they potentially inherited the antineoplastic activities of KM8-Aib against cancer cells, as well as low toxicities to non-malignant cells." REF00278 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 15.84893 uM . . . Cutaneous melanoma SK-MEL-28 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 15.84893 uM . . . Renal carcinoma TK-10 cell . REF100756 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 15.85 uM . . . Hepatocellular carcinoma Huh-7 cell . REF102294 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 15.85 uM . . . Chronic myeloid leukemia K562 cell . REF100902 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 15.85 uM . . . Colon adenocarcinoma KM12 cell . REF100587 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 15.88 uM . . . Invasive breast carcinoma MCF-7 cell . REF101154 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 15.92 uM . . . Cutaneous melanoma SK-MEL-28 cell . REF101480 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 150 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101872 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 150 nM . . . Colon cancer HT29 cell . REF101862 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 150 nM . . . Lung adenocarcinoma NCI-H23 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 150 nM . . . Invasive breast carcinoma MCF-7 cell . REF101545 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 150 nM . . . Colon adenocarcinoma LoVo cell . REF101383 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 150 nM . . . Lung adenocarcinoma A-549 cell . REF100849 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 150 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100723 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 150 nM . . . Normal COLO205 cell . REF100624 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 150 nM . . . Lung adenocarcinoma A-549 cell . REF100531 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 150 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100410 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 150 nM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF102490 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 150 nM . . . Squamous carcinoma SCC-25 cell . REF100165 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 150 uM . . . Sezary syndrome H9 cell . REF102021 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 153.95 nM . . . Colon adenocarcinoma HCT 15 cell . REF100915 DRG00045 Duocarmycin Sa Half Maximal Inhibitory Concentration (IC50) = 154 nM 72 h . . Fibrosarcoma HT-1080 cell "All cell lines demonstrated sensitivity toward the DSA-PABA payload 5 in the nanomolar range. The cleaved peptide 6, and the benzyl protected control peptide 4, had no appreciable effect on cell proliferation (>100 µM), suggesting that any observed cytotoxic activity is due to the DSA warhead. Interestingly, PDC 7, without the cathepsin B cleavable sequence, also had no appreciable effect on cell proliferation (>100 µM), despite possessing the active DSA DNA alkylating moiety. Perhaps this PDC is either not being taken up into cells or not being broken down by proteases and peptidases in the cell. In both cases, the warhead may not be reaching the nucleus, the site of action of the duocarmycins. Cell lines that demonstrated appreciable levels of TFα were sensitive to PDC 3. Interestingly, HCT116, which had relatively high TFα expression and cathepsin B activity, demonstrated the greatest sensitivity to PDC 3, approaching similar potency to the payload 5. Excitingly, A549, H292, and 16HBE14o, which showed no detectable TFα expression, appeared unaffected by PDC 3 up to 100 µM, suggesting that TFα expression is required for the efficacy of PDC 3." REF00117 DRG00002 Chlorambucil Half Maximal Inhibitory Concentration (IC50) = 154.4 µM 48 h . . Hepatoblastoma Hep-G2 cell "As presented in Figure 5D, the corresponding IC50 values of CRBFFEYSV nanofibers against HepG2, MCF-7, and BEL-7402 cells were 28.9, 47.5, and 25.7 µm, respectively, which were much lower than that of free YSV (842.9, 999.5, and 719.2 µm), free CRB (154.4, 214.6, and 192.5 µm), and the mixed drugs (150.0, 190.3, and 180.6 µm). " REF00319 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 157 nM . . . Ovarian adenocarcinoma 1A9/ptx-10 cell . REF100542 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 158 nM . . . Clear cell renal cell carcinoma Caki-1 cell . REF101860 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 158.2 uM . . . Colon adenocarcinoma SW480 cell . REF101124 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 158.48932 uM . . . Non-small cell lung carcinoma HOP-92 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 158.48932 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 158.49 nM . . . Normal COLO205 cell . REF102227 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 158.49 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 158.49 nM . . . Plasma cell myeloma RPMI-8226 cell . REF100104 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 16 nM . . . Prostate carcinoma PC-3 cell . REF102188 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 16 nM . . . Lung adenocarcinoma A-549 cell . REF101408 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 16 nM . . . Uterine sarcoma MES-SA cell . REF100477 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 16 nM . . . Lung adenocarcinoma A-549 cell . REF101075 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 16 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100975 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 16 nM . . . Lymphoma P388 cell . REF100307 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 16 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF102455 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 16 nM . . . Lung carcinoma SW1573 cell . REF102148 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 16 nM . . . Lung adenocarcinoma A-549 cell . REF100327 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 16 nM . . . Chronic myeloid leukemia K562 cell . REF101726 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 16 nM . . . Normal MT4 cell . REF102022 DRG00303 Prednisolone Half Maximal Effective Concentration (EC50) = 16 nM . . . Endocervical adenocarcinoma HeLa cell . REF100527 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 16 nM . . . Lung adenocarcinoma A-549 cell . REF102357 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 16 uM . . . Laryngeal carcinoma HEp-2 cell . REF102300 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 16 uM . . . Colon adenocarcinoma LoVo cell . REF102411 DRG00162 Curcumin Half Maximal Cytotoxicity Concentration (CC50) = 16 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100269 DRG00034 Chlorin e6 Half Maximal Inhibitory Concentration (IC50) = 16±4.2 µM 24 h . . Hepatoblastoma L-O2 cell line "Subsequently, the antiproliferative activities of the PS conjugates, including dark toxicity and phototoxicity (660 nM, light dose: 10 J/cm2), were evaluated. Dark toxicity refers to the toxicity of PS conjugates against cancer cells in the absence of light and can be regarded as a crucial measure of the safety profile, while phototoxicity is the most direct indicator of the PDT efficacy of PS. The results showed that the dark toxicity of all the compounds against the five cell lines was comparatively low, demonstrating that the PS conjugates exhibited a high safety index in the absence of light. Compound 8b exhibited the optimum tumor cell selectivity in terms of phototoxicity, with the IC50 values of 0.82 µM against HepG2 cells and 2.4 µM against Huh-7 cells, respectively, whereas its toxicity against GPC3-negative cell lines was >10 µM. Although compounds 8a and 8cd exhibited excellent phototoxicity against HepG2 and Huh-7 cells, (IC50 range: 0.22.0 µM), these compounds lacked selectivity between GPC3-overexpressed and GPC3-negative cells because they also showed considerable phototoxicity against the cell lines with minimal GPC3 expression. Notably, compound 1 showed low phototoxicity and selectivity against all the tested cell lines (IC50 > 10 µM)." REF00289 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 16.1 uM . . . Endocervical adenocarcinoma HeLa cell . REF102238 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 16.2 uM . . . Uterine sarcoma MES-SA/Dx5 cell . REF101644 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 16.3±4.6 nM 24 h . . Prostate carcinoma DU145 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 16.31 uM . . . Chronic myeloid leukemia K562 cell . REF101791 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 16.32 uM . . . Endocervical adenocarcinoma HeLa cell . REF101029 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 16.32 uM . . . Colon cancer HT29 cell . REF101850 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 16.4 uM . . . Colon cancer HT29 cell . REF102223 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 16.53 uM . . . Lung adenocarcinoma A-549 cell . REF101786 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 16.7 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100348 DRG00101 Vidarabine Half Maximal Infective Dose (ID50) = 16.8 uM . . . Lymphoma P388 cell . REF102017 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 16.96 uM . . . Lung adenocarcinoma A-549 cell . REF102363 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Acute myeloid leukemia HL-60 cell . REF102135 DRG00009 Camptothecin Tumor Growth Inhibition value (TGI) = 160 nM . . . Invasive breast carcinoma MCF-7 cell . REF101161 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Colon adenocarcinoma SW948 cell . REF100756 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Uterine sarcoma MES-SA cell . REF101644 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Invasive breast carcinoma MCF-7 cell . REF101365 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 160 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101162 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Colon carcinoma HCT 116 cell . REF100935 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Histiocytic lymphoma U-937/GTB cell . REF100933 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Lung adenocarcinoma A-549 cell . REF100804 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Glioma XF498 cell . REF100687 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Endocervical adenocarcinoma HeLa cell . REF100665 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 160 nM . . . Lung adenocarcinoma A-549 cell . REF100653 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Lung adenocarcinoma A-549 cell . REF102449 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Lymphoma P388 cell . REF102087 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 160 nM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF101650 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 161 nM . . . Normal L929 cell . REF101126 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 163 nM . . . Lung large cell carcinoma NCI-H1299 cell . REF102118 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 163.01 uM . . . Colon adenocarcinoma DLD-1 cell . REF101755 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 164 nM . . . Colon adenocarcinoma HCT 15 cell . REF100732 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 166 nM . . . Colon adenocarcinoma HCT 15 cell . REF100991 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 166 nM . . . Normal BALB/3T3 cell . REF101869 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 167.5 uM . . . Prostate carcinoma AT3B-1 cell . REF100476 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 168 nM . . . Gastric adenocarcinoma MKN45 cell . REF101079 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 17 ng/mL . . . Lymphoma P388 cell . REF100151 DRG00008 Dexamethasone Half Maximal Effective Concentration (EC50) = 17 nM . . . Endocervical adenocarcinoma HeLa cell . REF100527 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 17 nM . . . Gastric adenocarcinoma MKN45 cell . REF100327 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 17 nM . . . Breast adenocarcinoma MDA-MB-361 cell . REF100287 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 17 nM . . . Acute myeloid leukemia HL-60 cell . REF101516 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 17 nM . . . Acute monocytic leukemia MV4-11 cell . REF101676 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 17 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101656 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 17 nM . . . Renal carcinoma A498 cell . REF100505 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 17 nM . . . Hypopharyngeal squamous cell carcinoma FaDu cell . REF100186 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 17 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100071 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 17 pM . . . Normal HBL-100 cell . REF101004 DRG00221 Acyclovir Half Maximal Effective Concentration (EC50) = 17 uM . . . Erythroleukemia HEL cell . REF100087 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 17.02 uM . . . Lung adenocarcinoma A-549 cell . REF102402 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 17.23 uM . . . Chronic myeloid leukemia K562 cell . REF100953 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 17.3 nM . . . Melanoma LOX IMVI cell . REF100439 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 17.32 uM . . . Colon cancer HT29 cell . REF101307 DRG00003 Fluorouracil Half Maximal Effective Concentration (EC50) = 17.37 ug/mL . . . Stomach adenocarcinoma BGC-823 cell . REF102251 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 17.4 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF101544 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 17.403 uM . . . Invasive breast carcinoma MCF-7 cell . REF100625 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 17.44 uM . . . Hepatoblastoma Hep-G2 cell . REF102382 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 17.44 uM . . . Melanoma SK-MEL-2 cell . REF100804 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 17.5 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100449 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 17.5 uM . . . Endocervical adenocarcinoma HeLa cell . REF100119 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 17.54 uM . . . Hepatoblastoma Hep-G2 cell . REF100953 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 17.6 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100530 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 17.62 µM . . . Hepatocellular carcinoma SMMC-7721 cell "An MTT colorimetric assay was used to evaluate the in vitro cytotoxicity of materials on SMMC-7721 cells. Within the concentration range of 1.25100 µM, DOX, DOX-SH, and PDC had a certain killing effect on liver cancer cells. The IC50 values of DOX, DOX-SH, and PDC were 17.62, 14.75, and 20.22 µM, respectively." REF00112 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 17.67 uM . . . Melanoma B16 cell . REF101337 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 17.68 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF101706 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 17.7 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100144 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 17.85 uM . . . Melanoma B16 cell . REF102330 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 17.9 nM . . . Invasive breast carcinoma MCF-7 cell . REF100911 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Breast adenocarcinoma MDA-MB-361 cell . REF101108 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 170 nM . . . Lung adenocarcinoma A-549 cell . REF101092 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 170 nM . . . Cervical squamous cell carcinoma SiHa cell . REF101919 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101820 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Astrocytoma U-251MG cell . REF101775 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 170 nM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Colon adenocarcinoma LoVo cell . REF101211 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 170 nM . . . Melanoma SK-MEL-2 cell . REF101165 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 170 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101162 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 170 nM . . . Invasive breast carcinoma MCF-7 cell . REF101162 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Chronic myeloid leukemia K562 cell . REF100897 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100882 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 170 nM . . . Prostate carcinoma PC-3 cell . REF100849 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Lung adenocarcinoma A-549 cell . REF100837 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Hepatoblastoma Hep-G2 cell . REF100485 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF101716 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Normal CHO cell . REF100952 DRG00024 Thapsigargin Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Chronic myeloid leukemia K562 cell . REF101074 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Cervical carcinoma L02 cell . REF102422 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Lymphoblastic leukemia L1210 cell . REF100068 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 170 nM . . . Renal adenocarcinoma ACHN cell . REF102278 DRG00280 Erythromycin Half Maximal Inhibitory Concentration (IC50) = 170 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100093 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 177.83 nM . . . Colon cancer HT29 cell . REF100123 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 178 nM . . . Lung adenocarcinoma NCI-H23 cell . REF101221 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 178 nM . . . Colon adenocarcinoma SW620 cell . REF100552 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 179 nM . . . Lymphoblastic leukemia L1210 cell . REF100379 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 18 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100251 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 18 nM . . . Acute myeloid leukemia HL-60 cell . REF100564 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 18 nM . . . Colon adenocarcinoma HCT 15 cell . REF100496 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 18 nM . . . Normal HEK293 cell . REF101757 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 18 nM . . . Acute myeloid leukemia HL-60 cell . REF100702 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 18 nM . . . Acute myeloid leukemia HL-60 cell . REF100637 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 18 nM . . . Breast adenocarcinoma MDA-MB-361 cell . REF100287 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 18 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101396 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 18 nM . . . Colon carcinoma HCT 116 cell . REF100792 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 18 nM . . . Lung adenocarcinoma A-549 cell . REF102498 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 18 nM . . . Lymphoblastic leukemia R30dm-CCRF-CEM cell . REF100206 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 18 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100186 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 18 nM . . . Colon cancer HT29 cell . REF100176 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 18 nM . . . Lymphoblastic leukemia L1210 cell . REF100145 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 18 nM . . . Invasive breast carcinoma MCF-7 cell . REF102357 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 18 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102366 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 18 uM . . . Breast carcinoma ZR-75-30 cell . REF101484 DRG00043 JH-VII-139-1 Half Maximal Inhibitory Concentration (IC50) = 18±0.5 µM 48 h . . Breast adenocarcinoma MDA-MB-231 cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00034 Chlorin e6 Half Maximal Inhibitory Concentration (IC50) = 18±3.9 µM 24 h . . Adult hepatocellular carcinoma GPC3-positive Huh-7 cell "Subsequently, the antiproliferative activities of the PS conjugates, including dark toxicity and phototoxicity (660 nM, light dose: 10 J/cm2), were evaluated. Dark toxicity refers to the toxicity of PS conjugates against cancer cells in the absence of light and can be regarded as a crucial measure of the safety profile, while phototoxicity is the most direct indicator of the PDT efficacy of PS. The results showed that the dark toxicity of all the compounds against the five cell lines was comparatively low, demonstrating that the PS conjugates exhibited a high safety index in the absence of light. Compound 8b exhibited the optimum tumor cell selectivity in terms of phototoxicity, with the IC50 values of 0.82 µM against HepG2 cells and 2.4 µM against Huh-7 cells, respectively, whereas its toxicity against GPC3-negative cell lines was >10 µM. Although compounds 8a and 8cd exhibited excellent phototoxicity against HepG2 and Huh-7 cells, (IC50 range: 0.22.0 µM), these compounds lacked selectivity between GPC3-overexpressed and GPC3-negative cells because they also showed considerable phototoxicity against the cell lines with minimal GPC3 expression. Notably, compound 1 showed low phototoxicity and selectivity against all the tested cell lines (IC50 > 10 µM)." REF00289 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 18.1±1.1 µM 48 h . . Human papillomavirus-related cervical adenocarcinoma SGC-7901/CPT cell "MTT assay was preformed to measure the in vitro cytotoxicities of the compounds against cancer cells (HCT-116, SGC-7901, MCF-7, HCT-116/CPT, SGC-7901/CPT and MCF-7/C4) and benign cells (NCM460, GES-1 and LO2). As present in Table 1, all the peptides (Kb-C01, 0207) exhibited certain selective anticancer activities, which are comparable to their parent counterpart KM8-Aib. The target PDCs (Kb-CC01, 0207) were further obtained by coupling the peptides with CPT, displaying markedly improved antiproliferative activities and selectivities against cancer cell lines over CPT. Studies have revealed that cancer cell membranes are negatively charged due to the presence of substantial amounts of acid phospholipids. Therefore, positively charged CAPs are capable of binding to cancer cell surface through electrostatic interactions, making them specific to cancer cells. In this project, since the PDCs were composed of CAP KM8-Aib and CPT, they potentially inherited the antineoplastic activities of KM8-Aib against cancer cells, as well as low toxicities to non-malignant cells." REF00278 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 18.2 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100325 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 18.23 uM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF101023 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 18.24 uM . . . Colon adenocarcinoma HCT 15 cell . REF102166 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 18.24 uM . . . Prostate carcinoma PC-3 cell . REF101668 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 18.35 uM . . . Hepatoblastoma Hep-G2 cell . REF102402 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 18.35 uM . . . Colon carcinoma HCT 116 cell . REF102275 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 18.4 uM . . . Prostate carcinoma PC-3 cell . REF101834 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 18.42 uM . . . Prostate carcinoma PC-3 cell . REF102478 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 18.47 uM . . . Acute myeloid leukemia HL-60 cell . REF102385 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 18.5 uM . . . Gastric cancer MGC-803 cell . REF102283 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 18.5 uM . . . Invasive breast carcinoma MCF-7 cell . REF101583 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 18.56 uM . . . Lung adenocarcinoma A-549 cell . REF101473 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 18.6 uM . . . Normal BEAS-2B cell . REF101607 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 18.65 uM . . . Hepatoma Bel-7402 cell . REF102456 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 18.7 uM . . . Normal CCD-841CoN cell . REF102484 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 18.73 nM . . . Lung adenocarcinoma A-549 cell . REF101197 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 18.81 uM . . . Lung squamous cell carcinoma NCI-H2170 cell . REF101905 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 18.9 ng/ml . . . Prostate carcinoma PC-3 cell . REF100235 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 18.9 nM . . . Stomach adenocarcinoma BGC-823 cell . REF100695 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 18.9 uM . . . Hepatoblastoma Hep-G2 cell . REF102512 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Lymphoblastic leukemia L1210 cell . REF101975 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF101650 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF101534 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Endocervical adenocarcinoma HeLa cell . REF101317 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100106 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Colon carcinoma HCT 116 cell . REF102487 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Mantle cell lymphoma JeKo-1 cell . REF101582 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 180 nM . . . Melanoma M14 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Melanoma B16 cell . REF101281 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 180 nM . . . Normal COLO205 cell . REF101165 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 180 nM . . . Renal carcinoma TK-10 cell . REF101165 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 180 nM . . . Skin squamous cell carcinoma A431 cell . REF100795 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Colon cancer HT29 cell . REF100208 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Pancreatic adenocarcinoma SW1990 cell . REF101861 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Hepatoblastoma Hep-G2 cell . REF101739 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 180 nM . . . Hepatoblastoma Hep-G2 cell . REF101114 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Osteosarcoma U2OS cell . REF102440 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 180 nM . . . Normal MT-2 cell . REF100010 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Lung adenocarcinoma A-549 cell . REF102510 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 180 nM . . . Invasive breast carcinoma MCF-7 cell . REF102278 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 182 nM . . . Renal adenocarcinoma ACHN cell . REF100833 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 182 nM . . . Lymphoblastic leukemia L1210 cell . REF100646 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 185.6±99.8 nM 24 h . . High grade ovarian serous adenocarcinoma OVCAR-8 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 186 uM . . . Lymphoblastic leukemia L1210 cell . REF100155 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 188 nM . . . Prostate carcinoma PC-3 cell . REF100975 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 189.8 uM . . . Normal Vero cell . REF100053 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 19 nM . . . Prostate carcinoma DU145 cell . REF101631 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 19 nM . . . Chronic myeloid leukemia K562 cell . REF101855 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 19 nM . . . Hepatoblastoma Hep-G2 cell . REF100911 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 19 nM . . . Leukemia P388/S cell . REF100217 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 19 nM . . . Lung adenocarcinoma A-549 cell . REF100611 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 19 nM . . . Invasive breast carcinoma MCF-7 cell . REF100487 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 19 nM . . . Pancreatic ductal adenocarcinoma Capan-1 cell . REF102412 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 19 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100210 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 19 nM . . . Hypopharyngeal squamous cell carcinoma FaDu cell . REF100206 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 19 nM . . . Melanoma Malme-3M cell . REF102290 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 19 nM . . . Renal carcinoma UO-31 cell . REF102290 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 19 uM . . . Chronic myeloid leukemia K562 cell . REF102388 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 19 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101436 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 19 uM . . . Endocervical adenocarcinoma HeLa cell . REF100753 DRG00043 JH-VII-139-1 Tumor Growth Inhibition value (TGI) = 19±0.2 µM . . . Endocervical adenocarcinoma HeLa cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00043 JH-VII-139-1 Tumor Growth Inhibition value (TGI) = 19±0.3 µM . . . Invasive breast carcinoma MCF-7 cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 19.01 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101088 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 19.14 uM . . . Mouse melanoma B16-F10 cell . REF101000 DRG00403 Fluconazole Half Maximal Inhibitory Concentration (IC50) = 19.21 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102523 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 19.3 uM . . . Colon cancer HT29 cell . REF101080 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 19.31 uM . . . Endocervical adenocarcinoma HeLa cell . REF101959 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 19.51 uM . . . Prostate carcinoma PC-3 cell . REF101038 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 19.52 uM . . . Lung adenocarcinoma A-549 cell . REF101608 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 19.6 ng/ml . . . Prostate carcinoma PC-3 cell . REF100224 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 19.64 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100703 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 19.7 nM . . . Invasive breast carcinoma MCF-7 cell . REF102525 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 19.76 uM . . . Lung adenocarcinoma A-549 cell . REF102500 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 19.8 nM . . . Gliosarcoma SF539 cell . REF102166 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 19.84 uM . . . Gastric carcinoma SGC-7901 cell . REF102417 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 19.95 uM . . . Chronic myeloid leukemia K562 cell . REF100902 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 19.95 uM . . . Invasive breast carcinoma MCF-7 cell . REF100902 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 19.95 uM . . . Prostate carcinoma PC-3 cell . REF100902 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 19.95262 uM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF100098 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Invasive breast carcinoma MCF-7 cell . REF101971 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Lung adenocarcinoma A-549 cell . REF101892 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Acute myeloid leukemia HL-60 cell . REF101589 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Lung mucoepidermoid carcinoma NCI-H292 cell . REF101589 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Prostate carcinoma PC-3 cell . REF101236 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Hepatoblastoma Hep-G2 cell . REF100855 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Endocervical adenocarcinoma HeLa cell . REF100749 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 190 nM . . . Colon adenocarcinoma HCT 15 cell . REF100724 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Endocervical adenocarcinoma HeLa cell . REF100805 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Endocervical adenocarcinoma HeLa cell . REF100068 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Hepatoblastoma Hep-G2 cell . REF102413 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 190 nM . . . Normal HaCaT cell . REF102407 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 190 uM . . . Colon adenocarcinoma HCT 15 cell . REF101647 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 190.55 nM . . . Lung adenocarcinoma A-549 cell . REF100123 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 191 nM . . . Renal carcinoma UO-31 cell . REF100246 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 191 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100048 DRG00002 Chlorambucil Half Maximal Inhibitory Concentration (IC50) = 192.5 µM 48 h . . Hepatoma Bel-7402 cell "As presented in Figure 5D, the corresponding IC50 values of CRBFFEYSV nanofibers against HepG2, MCF-7, and BEL-7402 cells were 28.9, 47.5, and 25.7 µm, respectively, which were much lower than that of free YSV (842.9, 999.5, and 719.2 µm), free CRB (154.4, 214.6, and 192.5 µm), and the mixed drugs (150.0, 190.3, and 180.6 µm). " REF00319 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 194 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100833 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 197 uM . . . Mouse leukemia L1210 ( R81) cell . REF100159 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 199.53 nM . . . Invasive breast carcinoma MCF-7 cell . REF101977 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 199.53 nM . . . Hepatoblastoma Hep-G2 cell . REF100517 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 199.53 nM . . . Colon adenocarcinoma HCT 15 cell . REF100274 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 199.53 nM . . . Colon carcinoma HCT 116 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 199.53 nM . . . Renal carcinoma UO-31 cell . REF102222 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100578 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2 ng/mL . . . Melanoma SK-MEL-2 cell . REF100363 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100233 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100810 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 ng/mL . . . Prostate carcinoma DU145 cell . REF100810 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 2 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100580 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 2 ng/mL . . . Ovarian adenocarcinoma A2780-1A9 cell . REF100401 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 ng/mL . . . Colon cancer HT29 cell . REF100273 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 2 ng/mL . . . Lymphoma P388 cell . REF100299 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 2 ng/mL . . . Normal MT4 cell . REF102005 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101696 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Chronic myeloid leukemia K562 cell . REF100835 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Colon carcinoma HCT 116 cell . REF100751 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 2 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100558 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Lung adenocarcinoma A-549 cell . REF101278 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Melanoma SK-MEL-2 cell . REF101066 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF100748 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Colon cancer HT29 cell . REF100687 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Colon carcinoma HCT 116 cell . REF101866 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Colon cancer HT29 cell . REF101731 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101585 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Cervical carcinoma L02 cell . REF101490 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF101012 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 2 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100938 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Invasive breast carcinoma MCF-7 cell . REF100934 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Colon adenocarcinoma SW480 cell . REF100763 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 2 nM . . . Plasma cell myeloma RPMI-8226 cell . REF100587 DRG00013 Gemcitabine Half Maximal Growth Inhibition (GI50) = 2 nM . . . Lung adenocarcinoma NCI-H23 cell . REF102202 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Prostate carcinoma PC-3 cell . REF100246 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 2 nM . . . Normal MT4 cell . REF102053 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2 nM . . . Non-small cell lung carcinoma NCI-H522 cell . REF102357 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2 nM . . . Melanoma M14 cell . REF102290 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2 nM . . . Non-small cell lung carcinoma HOP-62 cell . REF102290 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2 nM . . . Renal carcinoma RXF 393 cell . REF102290 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102290 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Melanoma B16 cell . REF102240 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Endocervical adenocarcinoma HeLa cell . REF102214 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Invasive breast carcinoma MCF-7 cell . REF102128 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101014 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2 nM . . . Acute myeloid leukemia HL-60 cell . REF100749 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2 nM . . . Colon carcinoma HCT 116 cell . REF100127 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2 ug/mL . . . Lung adenocarcinoma A-549 cell . REF100758 DRG00011 Doxorubicin Half Maximal Cytotoxicity Concentration (CC50) = 2 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF101270 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2 ug/mL . . . Normal CCD 19Lu cell . REF101921 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 2 ug/mL . . . Acute myeloid leukemia HL-60 cell . REF100657 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2 ug/mL . . . Cutaneous melanoma SK-MEL-5 cell . REF100058 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2 uM . . . Colon cancer HT29 cell . REF100675 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 2 uM . . . Uterine sarcoma MES-SA/Dx5 cell . REF100302 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 uM . . . Breast carcinoma Bcap37 cell . REF101964 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 uM . . . Chronic myeloid leukemia K562 cell . REF101673 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 uM . . . Rhabdomyosarcoma RD cell . REF101349 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 uM . . . Prostate carcinoma PC-3 cell . REF101347 DRG00011 Doxorubicin Half Maximal Cytotoxicity Concentration (CC50) = 2 uM . . . Endocervical adenocarcinoma HeLa cell . REF100707 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 uM . . . Normal COLO205 cell . REF100662 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2 uM . . . EBV-related Burkitt lymphoma Raji cell . REF100610 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 2 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100678 DRG00059 Sunitinib Half Maximal Growth Inhibition (GI50) = 2 uM . . . Gastrointestinal stromal tumor GIST430 cell . REF102482 DRG00059 Sunitinib Half Maximal Growth Inhibition (GI50) = 2 uM . . . Gastrointestinal stromal tumor GIST48 cell . REF102458 DRG00221 Acyclovir Half Maximal Effective Concentration (EC50) = 2 uM . . . Normal BHK-21 cell . REF102056 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 2.01 ug/mL . . . Normal MT4 cell . REF102177 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2.02 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100214 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.02 uM . . . Endocervical adenocarcinoma HeLa cell . REF101734 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.03 uM . . . Hepatoblastoma Hep-G2 cell . REF100878 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 2.03 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100316 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.04 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100777 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.04±0.20 µM 48 h . . Normal GES1 cell "MTT assay was preformed to measure the in vitro cytotoxicities of the compounds against cancer cells (HCT-116, SGC-7901, MCF-7, HCT-116/CPT, SGC-7901/CPT and MCF-7/C4) and benign cells (NCM460, GES-1 and LO2). As present in Table 1, all the peptides (Kb-C01, 0207) exhibited certain selective anticancer activities, which are comparable to their parent counterpart KM8-Aib. The target PDCs (Kb-CC01, 0207) were further obtained by coupling the peptides with CPT, displaying markedly improved antiproliferative activities and selectivities against cancer cell lines over CPT. Studies have revealed that cancer cell membranes are negatively charged due to the presence of substantial amounts of acid phospholipids. Therefore, positively charged CAPs are capable of binding to cancer cell surface through electrostatic interactions, making them specific to cancer cells. In this project, since the PDCs were composed of CAP KM8-Aib and CPT, they potentially inherited the antineoplastic activities of KM8-Aib against cancer cells, as well as low toxicities to non-malignant cells." REF00278 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.05 ug/mL . . . Plasma cell myeloma RPMI-8226 cell . REF101311 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.05 uM . . . Lung adenocarcinoma A-549 cell . REF102456 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.05 uM . . . Normal COS-7 cell . REF101755 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.05 uM . . . Colon cancer HT29 cell . REF100821 DRG00122 Vinblastine Half Maximal Growth Inhibition (GI50) = 2.051 mM . . . Lung carcinoma SW1573 cell . REF101730 DRG00005 Primaquine Half Maximal Inhibitory Concentration (IC50) = 2.07 µM 18-24 h . . Plasmodium falciparum infection Plasmodium falciparum strain 3D7 "The six PDIP-PQ conjugates were analyzed for their ability to inhibit the in vitro growth of P. falciparum asexual blood stage parasites (strain 3D7) in RBCs and were compared to the activity of the parent drug and peptide. We were encouraged to discover that most of the PDIP-PQ PDCs retained antiplasmodial activity similar to PDIP, with IC50 values in the low micromolar range. Notably, the various design elements probed provided valuable information regarding which PDC characteristics can be modified to improve activity." REF00265 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.07±0.67 µM 48 h . . Gastric tubular adenocarcinoma NCI-N87 cell "HER2 positive SK-BR-3, NCIN87 and SK-OV-3 cells, and HER2 negative MDA-MB-231 and MCF-10A cells were selected to determine the cell activity of the target conjugates. From Table 3, most conjugates showed certain cytotoxicity to three HER2 positive cell lines. Among the three connection sites (S1S3), compounds 1, 4, and 7 with the first connection mode showed better activity. In the three HER2 positive SK-BR-3, NCIN87 and SK-OV-3 cells, conjugate 4 exhibited superior activity (IC50s of 0.53 0.17 µM, 1.58 0.41 µM, 2.50 0.78 µM, respectively), which almost equal to that of CPT (IC50s of 0.38 0.11 µM, 2.07 0.67 µM, 4.07 1.82 µM, respectively). The activity of conjugate 4 on HER2 positive cells was superior to that of conjugate 1 and 7. In MDA-MB-231 and MCF-10A cells, IC50s of conjugate 4 were 18.44 2.09 µM and 17.76 1.35 µM, respectively, which showed great tumor cell selectivity. Based on the above, conjugate 4 with better in vitro antitumor activity was selected for subsequent biological study." REF00288 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.08 uM . . . Invasive breast carcinoma MCF-7 cell . REF101503 DRG00013 Gemcitabine Half Maximal Growth Inhibition (GI50) = 2.085 nM . . . Lung large cell carcinoma NCI-H460 cell . REF102408 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.089 uM . . . Endocervical adenocarcinoma HeLa cell . REF101505 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 2.0893 uM . . . Non-small cell lung carcinoma HOP-62 cell . REF101977 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 2.0893 uM . . . Prostate carcinoma PC-3 cell . REF100848 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2.1 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100238 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.1 nM . . . Lung adenocarcinoma A-549 cell . REF100499 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 2.1 nM . . . Lymphoblastic leukemia L1210 cell . REF100162 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.1 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102112 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.1 uM . . . Prostate carcinoma PC-3 cell . REF102273 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.1 uM . . . Colon adenocarcinoma SW480 cell . REF100763 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.1 uM . . . Lung adenocarcinoma A-549 cell . REF101980 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.1 uM . . . Endocervical adenocarcinoma HeLa cell . REF101902 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.1 uM . . . Amelanotic melanoma A-375 cell . REF101843 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.1 uM . . . Normal HEK293 cell . REF101555 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 2.1 uM . . . Cervical squamous cell carcinoma SiHa cell . REF100849 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.1 uM . . . Lung adenocarcinoma A-549 cell . REF101355 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 2.1 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101849 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 2.1 uM . . . Normal Vero cell . REF100090 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.10±1.34 µM 48 h . . Gastric tubular adenocarcinoma NCI-N87 cell "To evaluated the in vitro anti-tumor activity of the conjugates, HER2-positive SK-BR-3, NCI-N87, HER2-negative MDA-MB-231 and normal MCF-10A cells were selected. As shown in Table 2, nearly all conjugates exhibited obvious anti-proliferation activity against SK-BR-3 cells, while most of the conjugates, except for Z6 and Z9, demonstrated different degrees of inhibitory activity on NCI-N87 cells. Taken together, Z8 and Z11 exhibited superior anti-tumor activity. The antiproliferative activity of Z8 against NCI-N87 cells (IC50 = 1.91 0.71 µM) was comparable to that of CPT (IC50 = 2.10 1.34 µM), while the antiproliferative activity of Z11 against SK-BR-3 cells (IC50 = 0.41 0.13 µM) was comparable to that of CPT (IC50 = 0.26 0.06 µM). Additionally, the IC50 values of these two conjugates against MDA-MB-231 and MCF-10A cells were significantly increased, showing their ability to selectively inhibit tumor cells. Based on the above results, Z8 and Z11, which exhibited better activity and apparent selectivity, were selected for subsequent studies." REF00312 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.11 uM . . . Invasive breast carcinoma MCF-7 cell . REF100894 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 2.12 nM . . . Acute monocytic leukemia U-937 cell . REF101429 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.12 nM . . . Lung adenocarcinoma A-549 cell . REF101386 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.12 uM . . . Lung adenocarcinoma A-549 cell . REF101273 DRG00011 Doxorubicin 30% Inhibitory Concentration (IC30) = 2.13 ug/mL . . . T acute lymphoblastic leukemia Jurkat cell . REF102186 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 2.177 uM . . . Colon adenocarcinoma HCT 15 cell . REF100833 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.18 uM . . . Invasive breast carcinoma MCF-7 cell . REF101569 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.19 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF102128 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 2.19 uM . . . Neuroblastoma SK-N-SH cell . REF100997 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.2 nM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF101308 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.2 nM . . . Colon carcinoma HCT 116 cell . REF102446 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.2 ug/mL . . . Chronic myeloid leukemia K562 cell . REF100008 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.2 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100766 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.2 uM . . . Prostate carcinoma PC-3 cell . REF101338 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.2 uM . . . Endocervical adenocarcinoma HeLa cell . REF101118 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.2 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100930 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.21 uM . . . Lung adenocarcinoma A-549 cell . REF101668 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.21 uM . . . Normal V79 cell . REF101771 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.21 uM . . . Hepatoblastoma Hep-G2 cell . REF100497 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.23 uM . . . Lung adenocarcinoma A-549 cell . REF100803 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.24 uM . . . Colon cancer HT29 cell . REF101738 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.24 uM . . . Squamous carcinoma SCC-25 cell . REF101715 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2.26 ng/ml . . . Renal carcinoma A498 cell . REF100325 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.29 uM . . . Invasive breast carcinoma MCF-7 cell . REF101009 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.29087 uM . . . Invasive breast carcinoma MCF-7 cell . REF101606 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 2.3 nM . . . Lung adenocarcinoma A-549 cell . REF100549 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.3 nM . . . Colon carcinoma HCT 116 cell . REF102189 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.3 ug/mL . . . Prostate carcinoma PC-3 cell . REF100965 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.3 uM . . . Colon carcinoma HCT 116 cell . REF100841 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.3 uM . . . Bone marrow neuroblastoma SH-SY5Y cell . REF101867 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.3 uM . . . Lung adenocarcinoma A-549 cell . REF101638 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.3 uM . . . Invasive breast carcinoma MCF-7 cell . REF101553 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.3 uM . . . Neuroblastoma IMR-32 cell . REF101548 DRG00003 Fluorouracil Half Maximal Infective Dose (ID50) = 2.3 uM/L . . . Chronic myeloid leukemia K562 cell . REF100028 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.31 uM . . . Invasive breast carcinoma T-47D cell . REF101528 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.32±0.24 µM 48 h . . Gastric tubular adenocarcinoma NCI-N87 cell "The cytotoxicity of conjugates was evaluated on cell lines with different expression levels of HER2. The results showed that among all conjugates with a single CPT molecule (I-1 to I-3), I-1 was the most cytotoxic against three HER2-positive cell lines (SK-BR-3, NCI-N87, and SK-OV-3 cells), and the calculated IC50 values for the three cells were 1.47 0.54, 3.29 0.67, and 4.29 1.11 µM, respectively. Similarly, among all conjugates with two CPT molecules (I-4 to I-6), I-4 showed the highest cytotoxicity toward HER2-positive cells, and the IC50 values for SK-BR-3, NCI-N87, and SK-OV-3 cells were 0.12 0.07, 1.78 0.47, and 1.27 0.38 µM, respectively. The activity of I-4 against SK-BR-3 cells was also slightly better than that of the positive control CPT (IC50 = 0.21 0.04 µM). The cytotoxicity of I-1 and I-4 against HER2-negative MDA-MB-231 cells was comparatively lower (calculated IC50s were 7.60 1.23 and 7.72 0.92 µM, respectively). In contrast, CPT itself showed higher cytotoxicity against MDA-MB-231 (IC50 = 1.06 0.42 µM), indicating that conjugates showed higher specificity in cell targeting. Furthermore, the cytotoxicity of I-1 and I-4 against normal cells MCF-10A (IC50 = 23.90 1.58 and 17.14 2.42 µM, respectively) was significantly lower than that of CPT alone (2.58 0.77 µM). Based on these results, I-1 and I-4 were selected for subsequent biological evaluation." REF00244 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.33 uM . . . Lung adenocarcinoma A-549 cell . REF102464 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.33 uM . . . Normal BJ cell . REF100877 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 2.34423 uM . . . Prostate carcinoma PC-3 cell . REF102227 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 2.34423 uM . . . Renal carcinoma A498 cell . REF101977 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.35 uM . . . Invasive breast carcinoma MCF-7 cell . REF102405 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 2.355 nM . . . Skin squamous cell carcinoma A431 cell . REF101197 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 2.36 mM . . . Acute myeloid leukemia HL-60 cell . REF100612 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.36 uM . . . Lung adenocarcinoma A-549 cell . REF101895 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.36 uM . . . Invasive breast carcinoma MCF-7 cell . REF101745 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.37 uM . . . Acute myeloid leukemia HL-60 cell . REF102415 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 2.37 uM . . . Lung large cell carcinoma NCI-H460 cell . REF102223 DRG00121 Naproxen Half Maximal Inhibitory Concentration (IC50) = 2.385 mM . . . Invasive breast carcinoma MCF-7 cell . REF102312 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.4 ng/mL . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100266 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.4 ng/mL . . . Colon cancer HT29 cell . REF101918 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.4 ng/mL . . . Prostate carcinoma DU145 cell . REF101076 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.4 nM . . . Colon carcinoma HCT 116 cell . REF100505 DRG00019 Methotrexate Half Maximal Effective Dosage (ED50) = 2.4 nM . . . Laryngeal carcinoma HEp-2 cell . REF100181 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2.4 ug/mL . . . Colon adenocarcinoma HCT 15 cell . REF100257 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.4 uM . . . Chronic myeloid leukemia K562 cell . REF102272 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.4 uM . . . Normal BEAS-2B cell . REF101607 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 2.4 uM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF100409 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.4 uM . . . Chronic myeloid leukemia K562 cell . REF101260 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 2.4 uM . . . Normal Vero cell . REF100090 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 2.4 uM . . . Invasive breast carcinoma MCF-7 cell . REF102367 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.41 uM . . . Hepatoblastoma Hep-G2 cell . REF102397 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.42 uM . . . Prostate carcinoma PC-3 cell . REF101761 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.42 uM . . . Neuroblastoma SK-N-SH cell . REF101600 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2.43 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100235 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.43 uM . . . Colon adenocarcinoma SW480 cell . REF101198 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.43 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100666 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 2.43±0.58 µM 72 h . . Pancreatic ductal adenocarcinoma PANC-1 cell "To investigate the anticancer activity of the GnRH-III drug conjugates, cell viability studies have been performed on A2780 ovarian cancer and Panc-1 pancreatic cancer cells. The GnRH-R expression of these cell lines was determined by Western blot studies. In the case of the A2780 cells, a distinct band at 38 kDa could be detected which corresponds to the full-length human GnRH-R. In contrast, the signal intensity of the 38 kDa band was much lower for Panc-1 pancreatic cancer cells being in line with our previous results. Thus, the antiproliferative activity of the GnRH-drug conjugates was studied on high-GnRH-R-expressing A2780 cells and low-GnRH-R-expressing Panc-1 cells. Since the release of free Dau and PTX can be assumed, both drugs were used as controls. The cells were treated for either 24 h (Dau conjugates) or six hours (PTX compounds), followed by additional incubation with fresh growth medium until 72 h after treatment initiation. The obtained results reveal, on the one hand, that the non-cleavable linker-containing conjugates possess a reduced anticancer activity in comparison to the cleavable conjugates and, on the other hand, that the activity of the all GnRH-III-drug conjugates was substantially reduced compared to the free drug. Moreover, all compounds displayed a lower biological activity on Panc-1 cells than on A2780. In the case of the cleavable GnRH-III-Dau conjugates, the IC50 values varied between 2.8511.18 M on A2780 cells, whereby the best activity was obtained for compound 13 (2.85 M) which contained the cathepsin B-cleavage site Val-Ala and the GnRH-III-[2δHis-3D-Tic-4Lys(Bu)] peptide carrier. Apart from that, the IC50 values of the cleavable PTX conjugates on A2780 cells are in the same sub-micromolar range and vary between 0.510.77 M, while the activity of these conjugates was approximately 10 times lower on Panc-1 cells (5.038.15 M)." REF00219 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.44 uM . . . Invasive breast carcinoma MCF-7 cell . REF102519 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.45 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100556 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.45 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101234 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 2.45 uM . . . Rhabdomyosarcoma RD cell . REF101555 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.45 uM . . . Prostate carcinoma DU145 cell . REF101980 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.46 uM . . . Lung adenocarcinoma A-549 cell . REF100722 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 2.47 uM . . . Hepatoma Bel-7402 cell . REF102120 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.5 mM . . . Hepatoblastoma Hep-G2 cell . REF101058 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.5 nM . . . Lung adenocarcinoma NCI-H1975 cell . REF101333 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.5 nM . . . Invasive breast carcinoma MCF-7 cell . REF100959 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.5 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100686 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.5 nM . . . Lung small cell carcinoma H69AR cell . REF100544 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.5 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101213 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.5 nM . . . Invasive breast carcinoma MCF-7 cell . REF100747 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.5 nM . . . Lung small cell carcinoma H69AR cell . REF100544 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.5 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF102291 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.5 ug/mL . . . Oral cavity squamous cell carcinoma HSC-2 cell . REF100381 DRG00012 Paclitaxel 90% Lethal Concentration (IC50) = 2.5 ug/mL . . . Embryonic hepatoma WRL68 cell . REF100483 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.5 uM . . . Prostate carcinoma PC-3 cell . REF101339 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.5 uM . . . Hepatocellular carcinoma SMMC-7721 cell . REF101705 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.5 uM . . . Lymph node metastasis of prostate carcinoma LNCaP C4-2 cell . REF101470 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.5 uM . . . Chronic myeloid leukemia K562 cell . REF100745 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 2.5 uM . . . Acute monocytic leukemia THP-1 cell . REF100608 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.5 uM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF101923 DRG00059 Sunitinib Half Maximal Effective Concentration (EC50) = 2.5 uM . . . Pancreatic ductal adenocarcinoma BxPC-3 cell . REF102459 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 2.5 uM . . . Renal adenocarcinoma ACHN cell . REF102296 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 2.5 uM . . . Normal Vero cell . REF100018 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.5 uM . . . Endocervical adenocarcinoma HeLa cell . REF101448 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 2.51189 uM . . . Lung adenocarcinoma NCI-H23 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 2.51189 uM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100756 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 2.51189 uM . . . Non-small cell lung carcinoma HOP-62 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2.51189 uM . . . Normal COLO205 cell . REF102222 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 2.512 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100274 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 2.512 nM . . . Colon cancer HT29 cell . REF100274 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 2.512 nM . . . Leukemia SR cell . REF100274 DRG00019 Methotrexate Half Maximal Growth Inhibition (GI50) = 2.512 nM . . . Ovarian adenocarcinoma OVCAR-4 cell . REF100567 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.52±0.22 µM 48 h . . Amelanotic melanoma LO #2 cell "MTT assay was preformed to measure the in vitro cytotoxicities of the compounds against cancer cells (HCT-116, SGC-7901, MCF-7, HCT-116/CPT, SGC-7901/CPT and MCF-7/C4) and benign cells (NCM460, GES-1 and LO2). As present in Table 1, all the peptides (Kb-C01, 0207) exhibited certain selective anticancer activities, which are comparable to their parent counterpart KM8-Aib. The target PDCs (Kb-CC01, 0207) were further obtained by coupling the peptides with CPT, displaying markedly improved antiproliferative activities and selectivities against cancer cell lines over CPT. Studies have revealed that cancer cell membranes are negatively charged due to the presence of substantial amounts of acid phospholipids. Therefore, positively charged CAPs are capable of binding to cancer cell surface through electrostatic interactions, making them specific to cancer cells. In this project, since the PDCs were composed of CAP KM8-Aib and CPT, they potentially inherited the antineoplastic activities of KM8-Aib against cancer cells, as well as low toxicities to non-malignant cells." REF00278 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.53 uM . . . Lung adenocarcinoma A-549 cell . REF100384 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.544 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100991 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 2.55 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100204 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.56 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101896 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.56 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101380 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.57 uM . . . Invasive breast carcinoma MCF-7 cell . REF100875 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.58 uM . . . Lung adenocarcinoma A-549 cell . REF101779 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.58±0.77 µM 48 h . . Normal MCF-10A cell "The cytotoxicity of conjugates was evaluated on cell lines with different expression levels of HER2. The results showed that among all conjugates with a single CPT molecule (I-1 to I-3), I-1 was the most cytotoxic against three HER2-positive cell lines (SK-BR-3, NCI-N87, and SK-OV-3 cells), and the calculated IC50 values for the three cells were 1.47 0.54, 3.29 0.67, and 4.29 1.11 µM, respectively. Similarly, among all conjugates with two CPT molecules (I-4 to I-6), I-4 showed the highest cytotoxicity toward HER2-positive cells, and the IC50 values for SK-BR-3, NCI-N87, and SK-OV-3 cells were 0.12 0.07, 1.78 0.47, and 1.27 0.38 µM, respectively. The activity of I-4 against SK-BR-3 cells was also slightly better than that of the positive control CPT (IC50 = 0.21 0.04 µM). The cytotoxicity of I-1 and I-4 against HER2-negative MDA-MB-231 cells was comparatively lower (calculated IC50s were 7.60 1.23 and 7.72 0.92 µM, respectively). In contrast, CPT itself showed higher cytotoxicity against MDA-MB-231 (IC50 = 1.06 0.42 µM), indicating that conjugates showed higher specificity in cell targeting. Furthermore, the cytotoxicity of I-1 and I-4 against normal cells MCF-10A (IC50 = 23.90 1.58 and 17.14 2.42 µM, respectively) was significantly lower than that of CPT alone (2.58 0.77 µM). Based on these results, I-1 and I-4 were selected for subsequent biological evaluation." REF00244 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 2.581 ug/mL . . . Normal MT4 cell . REF102078 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.6 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101469 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.6 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100998 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.6 nM . . . Endocervical adenocarcinoma HeLa cell . REF100936 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 2.6 nM . . . Prostate carcinoma LNCaP cell . REF100549 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 2.6 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF102166 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 2.6 ug/mL . . . Osteosarcoma HOS-TE85 cell . REF100009 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2.6 ug/mL . . . Neuroblastoma SK-N-SH cell . REF100058 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.6 uM . . . Colon carcinoma HCT 116 cell . REF100763 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.6 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101328 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.6 uM . . . Prostate carcinoma PC-3 cell . REF101898 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.62 uM . . . Invasive breast carcinoma MCF-7 cell . REF100796 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.63 uM . . . Endocervical adenocarcinoma HeLa cell . REF101344 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 2.63 uM . . . Lymphoblastic leukemia R2-CCRF-CEM cell . REF100378 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2.65 nM . . . Non-small cell lung carcinoma HOP-62 cell . REF102316 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.655 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101226 DRG00037 TGX-D1 Half Maximal Inhibitory Concentration (IC50) = 2.67 µM . . . Prostate carcinoma LNCaP cell "Among the four TGX-221 derivatives, TGX-D1 showed the best activity (IC50=2.67 µM) in LNCaP cells. " REF00318 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.67 uM . . . Invasive breast carcinoma MCF-7 cell . REF101991 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2.7 ng/ml . . . Colon cancer HT29 cell . REF100191 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.7 nM . . . Lung adenocarcinoma A-549 cell . REF100367 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.7 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100230 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 2.7 nM . . . Lymphoblastic leukemia L1210 cell . REF100178 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.7 nM . . . Endocervical adenocarcinoma HeLa cell . REF100544 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.7 nM . . . Invasive breast carcinoma MCF-7 cell . REF100072 DRG00407 Combretastatin A4 Half Maximal Effective Dosage (ED50) = 2.7 ug/mL . . . Lymphoma P388 cell . REF100058 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.7 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101030 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.7 uM . . . Colon adenocarcinoma Caco-2 cell . REF101097 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.7 uM . . . Hepatoblastoma Hep-G2 cell . REF101097 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.7 uM . . . Normal NIH3T3 cell . REF100969 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.7 uM . . . Lung adenocarcinoma A-549 cell . REF101993 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.7 uM . . . Ovarian carcinoma HEY cell . REF101614 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.7 uM . . . Chronic myeloid leukemia K562 cell . REF101445 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.7 uM . . . Uterine sarcoma MES-SA/Dx5 cell . REF100302 DRG00024 Thapsigargin Half Maximal Inhibitory Concentration (IC50) = 2.7 uM . . . Invasive breast carcinoma MCF-7 cell . REF101320 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 2.7 uM . . . Colon carcinoma HCT 116 cell . REF102093 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 2.7 uM . . . Melanoma M14 cell . REF102093 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.71 uM . . . Invasive breast carcinoma MCF-7 cell . REF101514 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 2.72 ug/mL . . . Hepatoma Bel-7402 cell . REF100431 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.76 uM . . . Prostate carcinoma LNCaP cell . REF101088 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 2.76 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100206 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 2.78 nM . . . Melanoma M14 cell . REF102316 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.78 uM . . . Endocervical adenocarcinoma HeLa cell . REF101234 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.78 uM . . . Colon adenocarcinoma DLD-1 cell . REF101463 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.78 uM . . . Invasive breast carcinoma MCF-7 cell . REF101398 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.8 nM . . . Endocervical adenocarcinoma HeLa cell . REF101682 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.8 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100776 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 2.8 nM . . . Lung squamous cell carcinoma QG-56 cell . REF102180 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 2.8 nM . . . Normal MT4 cell . REF102038 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.8 nM . . . Prostate carcinoma PC-3 cell . REF102131 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.8 uM . . . Acute myeloid leukemia HL-60 cell . REF101570 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 2.8 uM . . . Lung adenocarcinoma A-549 cell . REF100847 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.8 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101638 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 2.8 uM . . . Non-small cell lung carcinoma NCI-H522 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.8 uM . . . Lung adenocarcinoma A-549 cell . REF101078 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 2.8 uM . . . Normal Vero cell . REF100090 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.81 uM . . . Breast adenocarcinoma MDA-MB-468 cell . REF101618 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.81 uM . . . Lung adenocarcinoma A-549 cell . REF101410 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.82 uM . . . Invasive breast carcinoma MCF-7 cell . REF101072 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 2.82 uM . . . Endocervical adenocarcinoma HeLa cell . REF100997 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.84 uM . . . Chronic myeloid leukemia K562 cell . REF100704 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.85 uM . . . Neuroblastoma SK-N-SH cell . REF101826 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.85 uM . . . Chronic myeloid leukemia K562 cell . REF101044 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.85 uM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101724 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2.86 ng/mL . . . Renal carcinoma A498 cell . REF100318 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.86 uM . . . Invasive breast carcinoma MCF-7 cell . REF102322 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 2.86 uM . . . Hepatoblastoma Hep-G2 cell . REF102365 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.87 uM . . . Breast carcinoma Bcap37 cell . REF101323 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2.88 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF101935 DRG00023 Tesaglitazar Cholesterol level = 2.9 mmol/L Every day 2.5 μM db/db mice model. . . "The influence of tesa, tesa-NPY (3), and [F7, P34]-NPY (2) on the plasma lipids was also analyzed (Figure 9). The vehicle/untreated db/db mice showed elevated levels of triglycerides and free fatty acids (FFA) compared to the lean C57BL/6N mice. Treatment with tesa and tesa-NPY (3) led to a normalization of the triglycerides, FFA, whereas [F7, P34]-NPY (2) and vehicle/untreated had no influence on the lipid metabolism (Figure 9A/B). The cholesterol levels were unchanged by any treatment as these levels were also comparable in the untreated db/db mice compared to the lean mice (Figure 9C)." REF00088 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 2.9 nM . . . Colon adenocarcinoma LoVo cell . REF100974 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.9 uM . . . Colon carcinoma RKO cell . REF102493 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.9 uM . . . Normal COLO205 cell . REF101987 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2.9 uM . . . Lung adenocarcinoma A-549 cell . REF100140 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.9 uM . . . Cervical squamous cell carcinoma Ca-Ski cell . REF101598 DRG00221 Acyclovir Half Maximal Effective Concentration (EC50) = 2.9 uM . . . EBV-related Burkitt lymphoma Raji cell . REF102049 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.92 nM . . . Cervical epithelial carcinoma KB 3-1 cell . REF100320 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 2.93 ng/mL . . . Lymphoma P388 cell . REF100375 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 2.94 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100263 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.947 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100949 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.95 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100978 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.96 uM . . . Invasive breast carcinoma MCF-7 cell . REF101962 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.97 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100863 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.97 ug/mL . . . Acute myeloid leukemia HL-60 cell . REF100300 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 2.98 mM . . . Hepatocellular carcinoma Huh-7 cell . REF102372 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 2.98 uM . . . EBV-related Burkitt lymphoma Raji cell . REF101712 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 2.98 uM . . . Invasive breast carcinoma MCF-7 cell . REF100666 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 20 ng/mL . . . Lymphoma P388 cell . REF100299 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 20 ng/mL . . . Normal Vero cell . REF100202 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 20 ng/mL . . . Leukemia MOLT-4F cell . REF102000 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 ng/mL . . . Acute myeloid leukemia HL-60 cell . REF100826 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100718 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 20 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100539 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100463 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 20 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100458 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 20 ng/mL . . . Glioma XF498 cell . REF100405 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 20 ng/mL . . . Melanoma SK-MEL-2 cell . REF100365 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 20 ng/mL . . . Melanoma SK-MEL3 cell . REF100326 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 20 ng/ml . . . Prostate carcinoma PC-3 cell . REF100288 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 20 ng/ml . . . Colon cancer HT29 cell . REF100251 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 ng/mL . . . Colon cancer HT29 cell . REF100216 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 20 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100192 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 20 ng/mL . . . Normal WI-38 cell . REF100550 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 20 ng/mL . . . Normal MT4 cell . REF102032 DRG00009 Camptothecin Half Maximal Cytotoxicity Concentration (CC50) = 20 nM . . . Hepatoblastoma Hep-G2 cell . REF102257 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Colon adenocarcinoma HCT 15 cell . REF101613 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Acute myeloid leukemia HL-60 cell . REF101579 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 20 nM . . . Renal cell carcinoma SN12C cell . REF101533 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Prostate carcinoma DU145 cell . REF101317 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101184 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Gastric adenocarcinoma AGS cell . REF100760 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100327 DRG00011 Doxorubicin Half Maximal Cytotoxicity Concentration (CC50) = 20 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102345 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101999 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Acute myeloid leukemia HL-60 cell . REF101992 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Colon cancer HT29 cell . REF101940 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Cutaneous melanoma SK-MEL-28 cell . REF101940 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Colon carcinoma HCT 116 cell . REF101939 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101772 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Normal HEK293 cell . REF101684 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF101626 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 20 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101480 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Prostate carcinoma PC-3 cell . REF101334 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF101318 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Lung adenocarcinoma A-549 cell . REF101141 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF101008 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 20 nM . . . Invasive breast carcinoma MCF-7 cell . REF100851 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Colon adenocarcinoma SW620 cell . REF100808 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100696 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF100513 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Hereditary spherocytosis WIL2-NS cell . REF100506 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Leukemia C8166 cell . REF100506 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Lymphoblastic leukemia CCRF-SB cell . REF100506 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 20 nM . . . Prostate carcinoma LNCaP cell . REF100409 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Bladder carcinoma 5637 cell . REF100370 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Bladder carcinoma T24 cell . REF100340 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Breast adenocarcinoma SK-BR-3 cell . REF100305 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Lymphoma P388 cell . REF100301 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100278 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 20 nM . . . Melanoma B16-F1 cell . REF101801 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 20 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF101147 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 20 nM . . . Gastric carcinoma NUGC-3 cell . REF101114 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Endocervical adenocarcinoma HeLa cell . REF100905 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Stomach adenocarcinoma BGC-823 cell . REF100890 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 20 nM . . . Endocervical adenocarcinoma HeLa cell . REF100828 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Colon carcinoma RKO cell . REF100708 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100360 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Invasive breast carcinoma MCF-7 cell . REF100360 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Lymphoma P388 cell . REF100360 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Lung adenocarcinoma A-549 cell . REF102287 DRG00019 Methotrexate Half Maximal Infective Dose (ID50) = 20 nM . . . EBV-related Burkitt lymphoma Raji cell . REF102009 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101262 DRG00019 Methotrexate Half Maximal Effective Dosage (ED50) = 20 nM . . . Adenocarcinoma of the rat mammary gland W256 cell . REF100024 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Colon adenocarcinoma SW620 cell . REF101803 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100023 DRG00081 Cytarabine Half Maximal Effective Dosage (ED50) = 20 nM . . . Lymphoma P388 cell . REF100004 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 20 nM . . . Leukemia C8166 cell . REF102033 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100071 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Burkitt lymphoma CA46 cell . REF102327 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 20 nM . . . Chronic myeloid leukemia K562 cell . REF100394 DRG00101 Vidarabine Minimum Inhibitory Concentration (MIC) = 20 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100015 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 20 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF102032 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 20 uM . . . Ovarian serous adenocarcinoma OVCAR-5 cell . REF102277 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20 uM . . . Normal Vero cell . REF100778 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 20 uM . . . Pleural epithelioid mesothelioma NCI-H226 cell . REF100448 DRG00221 Acyclovir Half Maximal Effective Concentration (EC50) = 20 uM . . . Erythroleukemia HEL cell . REF100087 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 20 uM . . . T acute lymphoblastic leukemia CEM cl13 cell . REF102048 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 20 uM . . . Normal MT4 cell . REF102022 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20.1 nM . . . Lung carcinoma COR-L23 cell . REF100350 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20.2 uM . . . Invasive breast carcinoma MCF-7 cell . REF101641 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 20.4 nM . . . Prostate carcinoma TRAMP-C1A cell . REF102488 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 20.4 uM . . . Cervical carcinoma L02 cell . REF102383 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 20.5 nM . . . Invasive breast carcinoma MCF-7 cell . REF100911 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 20.6 uM . . . Prostate carcinoma DU145 cell . REF102123 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 20.7 uM . . . Chronic myeloid leukemia K562 cell . REF102451 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 20.8 uM . . . Lung adenocarcinoma A-549 cell . REF100728 DRG00009 Camptothecin Half Maximal Effective Dosage (ED50) = 20.9 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100549 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 20.9±2.7 nM 24 h . . Lung adenocarcinoma H1975 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 20.93 uM . . . Endocervical adenocarcinoma HeLa cell . REF101088 DRG00034 Chlorin e6 Half Maximal Inhibitory Concentration (IC50) > 200 µM 24 h . . Normal Human umbilical vein endothelial cell "Subsequently, the antiproliferative activities of the PS conjugates, including dark toxicity and phototoxicity (660 nM, light dose: 10 J/cm2), were evaluated. Dark toxicity refers to the toxicity of PS conjugates against cancer cells in the absence of light and can be regarded as a crucial measure of the safety profile, while phototoxicity is the most direct indicator of the PDT efficacy of PS. The results showed that the dark toxicity of all the compounds against the five cell lines was comparatively low, demonstrating that the PS conjugates exhibited a high safety index in the absence of light. Compound 8b exhibited the optimum tumor cell selectivity in terms of phototoxicity, with the IC50 values of 0.82 µM against HepG2 cells and 2.4 µM against Huh-7 cells, respectively, whereas its toxicity against GPC3-negative cell lines was >10 µM. Although compounds 8a and 8cd exhibited excellent phototoxicity against HepG2 and Huh-7 cells, (IC50 range: 0.22.0 µM), these compounds lacked selectivity between GPC3-overexpressed and GPC3-negative cells because they also showed considerable phototoxicity against the cell lines with minimal GPC3 expression. Notably, compound 1 showed low phototoxicity and selectivity against all the tested cell lines (IC50 > 10 µM)." REF00289 DRG00009 Camptothecin Half Maximal Cytotoxicity Concentration (CC50) = 200 nM . . . Normal MRC5 cell . REF102257 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Hepatoblastoma Hep-G2 cell . REF101912 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Invasive breast carcinoma MCF-7 cell . REF100650 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Colon cancer HT29 cell . REF101063 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Duodenal adenocarcinoma HuTu 80 cell . REF102526 DRG00011 Doxorubicin Half Maximal Cytotoxicity Concentration (CC50) = 200 nM . . . Hepatoblastoma Hep-G2 cell . REF102499 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Acute myeloid leukemia HL-60 cell . REF101891 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Invasive breast carcinoma MCF-7 cell . REF101862 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Melanoma B16 cell . REF101704 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Bone metastasis of prostate carcinoma PC-3M cell . REF101594 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Endocervical adenocarcinoma HeLa cell . REF101574 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 200 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101471 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Colon carcinoma HCT 116 cell . REF101452 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101452 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF101227 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Hepatoblastoma Hep-G2 cell . REF101212 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 200 nM . . . Colon cancer HT29 cell . REF101161 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Prostate carcinoma PC-3 cell . REF101118 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Prostate carcinoma DU145 cell . REF101118 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100725 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 200 nM . . . Lung adenocarcinoma A-549 cell . REF100566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100339 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Lymphoblastic leukemia L1210 cell . REF100150 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Prostate carcinoma PC-3 cell . REF101148 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Bone marrow neuroblastoma SH-SY5Y cell . REF100730 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Barrett adenocarcinoma OE33 cell . REF100598 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Mammary carcinoma 4T1 cell . REF100493 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Lymphoblastic leukemia L1210 cell . REF100153 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Prostate carcinoma DU145 cell . REF100917 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Hepatoblastoma Hep-G2 cell . REF102221 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF101632 DRG00224 Pemetrexed Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF100994 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 200 nM . . . Colon cancer HT29 cell . REF102502 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 200 nM . . . Lung adenocarcinoma A-549 cell . REF102468 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) = 200 ug/mL . . . Erythroleukemia HEL cell . REF102147 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) = 200 ug/mL . . . Erythroleukemia HEL cell . REF100003 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 200 uM . . . Endocervical adenocarcinoma HeLa cell . REF101605 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 200 uM . . . Sezary syndrome H9 cell . REF100035 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 202 nM . . . Breast adenocarcinoma SK-BR-3 cell . REF101516 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 202.9±1.0 nM 24 h . . Colon cancer HT29 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00012 Paclitaxel 90% Lethal Concentration (IC50) = 204 nM . . . Gastric adenocarcinoma MKN45 cell . REF100505 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 206.7 nM . . . Hepatocellular carcinoma Huh-7 cell . REF101197 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 21 nM . . . Uterine sarcoma MES-SA cell . REF100302 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 21 nM . . . Breast adenocarcinoma MDA-MB-361 cell . REF100287 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 21 nM . . . Cervical epithelial carcinoma KB 3-1 cell . REF100372 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 21 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101403 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 21 nM . . . Invasive breast carcinoma MCF-7 cell . REF100887 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 21 nM . . . Endocervical adenocarcinoma HeLa cell . REF101777 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 21 nM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF100994 DRG00101 Vidarabine Half Maximal Infective Dose (ID50) = 21 ug/mL . . . Lymphoblastic leukemia L1210 cell . REF100015 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 21 uM . . . Hepatocellular carcinoma Huh-7 cell . REF102378 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 21 uM . . . Colon adenocarcinoma Caco-2 cell . REF101970 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 21 uM . . . Normal COLO205 cell . REF100785 DRG00043 JH-VII-139-1 Tumor Growth Inhibition value (TGI) = 21±0.4 µM . . . Breast adenocarcinoma MDA-MB-231 cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 21.09 uM . . . Amelanotic melanoma A-375 cell . REF102473 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 21.1 nM . . . Colon adenocarcinoma HCT 15 cell . REF102292 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 21.1 nM . . . Endocervical adenocarcinoma HeLa cell . REF101497 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 21.2 uM . . . Hepatoblastoma Hep-G2 cell . REF101583 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 21.32 uM . . . Normal NIH3T3 cell . REF101619 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 21.33 uM . . . Breast ductal carcinoma BT-549 cell . REF101566 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 21.4 ug/mL . . . Prostate carcinoma PC-3 cell . REF101738 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 21.4 uM . . . Hepatoblastoma Hep-G2 cell . REF101153 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 21.5 uM . . . Melanoma B16 cell . REF100953 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 21.58 uM . . . Lung adenocarcinoma A-549 cell . REF102360 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 21.6 nM . . . Bladder carcinoma RT-112 cell . REF102214 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 21.68 uM . . . Colon adenocarcinoma HCC 2998 cell . REF101165 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 21.7 nM . . . Astrocytoma SF268 cell . REF100407 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 21.87762 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100123 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 21.9 uM . . . Amelanotic melanoma MDA-MB-435 cell . REF101173 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 21.9 uM . . . Chronic myeloid leukemia K562 cell . REF102256 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 21.96 uM . . . Chronic myeloid leukemia K562 cell . REF102385 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 210 nM . . . Colon adenocarcinoma DLD-1 cell . REF101957 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 210 nM . . . Colon adenocarcinoma SW480 cell . REF101802 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 210 nM . . . Prostate carcinoma DU145 cell . REF101736 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 210 nM . . . Stomach adenocarcinoma BGC-823 cell . REF100780 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 210 nM . . . Lung carcinoma SW1573 cell . REF100753 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 210 nM . . . Melanoma SK-MEL-2 cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 210 nM . . . Cutaneous melanoma SK-MEL-28 cell . REF101480 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 210 nM . . . Invasive breast carcinoma MCF-7 cell . REF100851 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 210 nM . . . Amelanotic melanoma A-375 cell . REF102278 DRG00280 Erythromycin 20% Inhibitory Concentration (IC20) = 210 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100093 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 211 nM . . . Invasive breast carcinoma MCF-7 cell . REF101969 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 213.8 nM . . . Colon adenocarcinoma KM12 cell . REF100123 DRG00002 Chlorambucil Half Maximal Inhibitory Concentration (IC50) = 214.6 µM 48 h . . Invasive breast carcinoma MCF-7 cell "As presented in Figure 5D, the corresponding IC50 values of CRBFFEYSV nanofibers against HepG2, MCF-7, and BEL-7402 cells were 28.9, 47.5, and 25.7 µm, respectively, which were much lower than that of free YSV (842.9, 999.5, and 719.2 µm), free CRB (154.4, 214.6, and 192.5 µm), and the mixed drugs (150.0, 190.3, and 180.6 µm). " REF00319 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 216 nM . . . Normal R2 cell . REF100994 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 22 nM . . . Invasive breast carcinoma MCF-7 cell . REF101319 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 22 nM . . . Lung adenocarcinoma A-549 cell . REF100636 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 22 nM . . . Colon adenocarcinoma DLD-1 cell . REF100682 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 22 nM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF100994 DRG00224 Pemetrexed Half Maximal Inhibitory Concentration (IC50) = 22 nM . . . Lymphoblastic leukemia L1210 cell . REF102007 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 22 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101176 DRG00008 Dexamethasone Half Maximal Inhibitory Concentration (IC50) = 22 uM . . . Mouse reticulum cell sarcoma J774.A1 cell . REF101309 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 22 uM . . . Glioblastoma SF-295 cell . REF102300 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 22 uM . . . Normal Vero cell . REF100121 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 22.23 uM . . . Colon cancer HT29 cell . REF102426 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 22.3 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101226 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 22.439 uM . . . Invasive breast carcinoma MCF-7 cell . REF102515 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 22.5 nM . . . Ovarian endometrioid adenocarcinoma A2780S cell . REF101428 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 22.61 uM . . . Invasive breast carcinoma MCF-7 cell . REF101307 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 22.7 ng/ml . . . Prostate carcinoma PC-3 cell . REF100264 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 22.7 nM . . . Acute myeloid leukemia HL-60 cell . REF101462 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 22.8 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100201 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 22.81 uM . . . Hepatocellular carcinoma PLC/PRF/5 cell . REF102402 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 22.9 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101541 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 22.9±1.4 nM 24 h . . Hepatoblastoma Hep-G2 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 220 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF101494 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 220 nM . . . Colon carcinoma HCT 116 cell . REF101776 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 220 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 220 nM . . . Normal L929 cell . REF101547 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 220 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101325 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 220 nM . . . Lung adenocarcinoma A-549 cell . REF101225 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 220 nM . . . Astrocytoma SF268 cell . REF100829 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 220 nM . . . Lung large cell carcinoma NCI-H460 cell . REF102165 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 220 nM . . . Colon cancer HT29 cell . REF100917 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 220 uM . . . Lymphoblastic leukemia L1210 cell . REF100171 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 223 nM . . . Lung adenocarcinoma A-549 cell . REF101600 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 225 nM . . . Colon adenocarcinoma HCT 15 cell . REF100512 DRG00012 Paclitaxel 90% Lethal Concentration (IC50) = 229 nM . . . Renal carcinoma A498 cell . REF100505 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 229.09 nM . . . Colon carcinoma HCT 116 cell . REF102227 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 229.09 nM . . . Glioblastoma SF-295 cell . REF102227 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 23 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100282 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 23 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101166 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 23 nM . . . Colon carcinoma HCT 116 cell . REF100348 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 23 nM . . . Invasive breast carcinoma MCF-7 cell . REF101249 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 23 nM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF101107 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Growth Inhibition (GI50) = 23 nM . . . Colon carcinoma HCT 116 cell . REF102448 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 23 nM . . . Lung adenocarcinoma A-549 cell . REF100246 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 23 nM . . . Prostate carcinoma DU145 cell . REF100246 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 23 nM . . . Lymphoma P388 cell . REF100210 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 23 pM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100762 DRG00012 Paclitaxel 30% Inhibitory Concentration (IC30) = 23 uM . . . Colon adenocarcinoma DLD-1 cell . REF100964 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 23.1 nM . . . Lung adenocarcinoma A-549 cell . REF100658 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 23.11 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101451 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 23.13±2.4% 14 days 5 mg/kg SKBR-3 cells female BALB/c mice xenograft model. Breast adenocarcinoma SK-BR-3 cell "In vivo anti-tumor studies were evaluated by using SKBR-3 xenografted (BALB/c nude) mice treated with the PDC, free DOX, or saline. Figure 5a demonstrates that the PDC had a much more powerful anti-tumor effect than free DOX, reducing tumor growth by 51.1 3.1% on day 14 post treatment, while free DOX only achieved a 23.13 2.4% reduction. Additionally, the PDC had a significantly higher tumor weight inhibition of 57.5 3.4% compared to free DOX." REF00254 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 23.18 nM . . . Lung adenocarcinoma A-549 cell . REF101634 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 23.33 uM . . . Endocervical adenocarcinoma HeLa cell . REF102326 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 23.4 nM . . . Invasive breast carcinoma MCF-7 cell . REF101770 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 23.4 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100684 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 23.43 nM . . . Colon adenocarcinoma T84 cell . REF102270 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 23.47 uM . . . Lung adenocarcinoma PC-9 cell . REF102275 DRG00101 Vidarabine Half Maximal Infective Dose (ID50) = 23.6 uM . . . Lymphoblastic leukemia L1210 cell . REF102027 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 23.76 uM . . . Gastric adenocarcinoma AGS cell . REF101956 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 23.8 nM . . . Leukemia SR cell . REF102268 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 23.94 uM . . . Normal Vero cell . REF100437 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 23.99 nM . . . Leukemia SR cell . REF102227 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 230 nM . . . Normal HBL-100 cell . REF100753 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 230 nM . . . Lung small cell carcinoma NCI-H187 cell . REF101799 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 230 nM . . . Breast ductal carcinoma BT-549 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 230 nM . . . Melanoma B16-F1 cell . REF101516 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 230 nM . . . Lung adenocarcinoma A-549 cell . REF101415 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 230 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100583 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 230 nM . . . Colon adenocarcinoma HCT 15 cell . REF100380 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 230 nM . . . Lung carcinoma NCI-H417 cell . REF100137 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 230 nM . . . Invasive breast carcinoma MCF-7 cell . REF101871 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 235 nM . . . Normal HaCaT cell . REF101753 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 24 ng/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100718 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 24 nM . . . Lung carcinoma A-427 cell . REF100280 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 24 nM . . . Colon adenocarcinoma LoVo cell . REF100349 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 24 nM . . . Endocervical adenocarcinoma HeLa cell . REF101427 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 24 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100941 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 24 nM . . . Osteosarcoma U2OS cell . REF100644 DRG00019 Methotrexate Half Maximal Growth Inhibition (GI50) = 24 nM . . . Invasive breast carcinoma MCF-7 cell . REF101465 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 24 nM . . . Lymphoblastic leukemia L1210 cell . REF100177 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 24 nM . . . Lymphoblastic leukemia L1210 cell . REF102205 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 24 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102199 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 24 uM . . . Colon adenocarcinoma LoVo cell . REF102217 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 24.267 uM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF102455 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 24.27 uM . . . Lung adenocarcinoma A-549 cell . REF101984 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 24.3 ng/mL . . . Colon cancer HT29 cell . REF101911 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 24.3 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100234 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 24.5 uM . . . Colon cancer HT29 cell . REF101145 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 24.69 uM . . . Astrocytoma U-251MG cell . REF102360 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 24.8 ng/mL . . . Lung small cell carcinoma NCI-H446 cell . REF100858 DRG00101 Vidarabine Half Maximal Inhibitory Concentration (IC50) = 24.8 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100055 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 24.82 ug/mL . . . Mouse reticulum cell sarcoma J774.A1 cell . REF101257 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Pancreatic ductal adenocarcinoma BxPC-3 cell . REF100650 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Invasive breast carcinoma MCF-7 cell . REF101892 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Endocervical adenocarcinoma HeLa cell . REF101792 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Colon adenocarcinoma LoVo cell . REF101653 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Colon cancer HT29 cell . REF101623 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Colon adenocarcinoma SW620 cell . REF100969 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100855 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100794 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Hepatoblastoma Hep-G2 cell . REF100751 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Normal HBL-100 cell . REF100723 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF101861 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Hepatoma SK-HEP1 cell . REF101128 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 240 nM . . . Endocervical adenocarcinoma HeLa cell . REF102449 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 245.47 nM . . . Melanoma LOX IMVI cell . REF100123 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 248.27 nM . . . Lung adenocarcinoma A549/TR cell . REF101634 DRG00011 Doxorubicin Inhibitory Concentration = 25 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100656 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 25 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100656 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 25 nM . . . Lung adenocarcinoma A-549 cell . REF100685 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 25 nM . . . Lymphoblastic leukemia L1210 cell . REF100372 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 25 nM . . . Glioblastoma SF-295 cell . REF101624 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 25 nM . . . Non-small cell lung carcinoma HOP-92 cell . REF101624 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 25 nM . . . Endocervical adenocarcinoma HeLa cell . REF101426 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 25 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100559 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 25 nM . . . Renal adenocarcinoma ACHN cell . REF100544 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 25 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102333 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 25 nM . . . Acute myeloid leukemia HL-60 cell . REF101628 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 25 nM . . . Colon adenocarcinoma WiDr cell . REF100168 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 25 nM . . . Pancreatic ductal adenocarcinoma Capan-1 cell . REF101838 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 25 nM . . . Endocervical adenocarcinoma HeLa cell . REF102356 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 25 ug/mL . . . Clear cell renal cell carcinoma Caki-1 cell . REF100157 DRG00003 Fluorouracil Half Maximal Lethal Concentration (IC50) = 25 uM . . . Normal HEK293 cell . REF102328 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 25 uM . . . Normal TERT-RPE1 cell . REF101710 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 25 uM . . . Glioblastoma T98G cell . REF102217 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 25 uM . . . Acute monocytic leukemia U1 cell . REF100067 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 25 uM . . . Normal HEK293 cell . REF102445 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 25.08 uM . . . Colon cancer HT29 cell . REF101290 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 25.1 nM . . . Skin squamous cell carcinoma A431 cell . REF100679 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 25.1 uM . . . Colon cancer HT29 cell . REF101657 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 25.1 uM . . . Prostate carcinoma PC-3 cell . REF102256 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 25.11 uM . . . Lung adenocarcinoma A-549 cell . REF100587 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 25.11886 uM . . . Colon adenocarcinoma SW620 cell . REF100098 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 25.12 uM . . . Ovarian endometrioid adenocarcinoma A2780/Taxol cell . REF101544 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 25.12 uM . . . Melanoma UACC-257 cell . REF100987 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 25.17 uM . . . Hepatoblastoma Hep-G2 cell . REF102360 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 25.4 uM . . . Colon cancer HT29 cell . REF100902 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 25.4 uM . . . Colon cancer HT29 cell . REF100902 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 25.4 uM . . . Prostate carcinoma PC-3 cell . REF101360 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 25.54 uM . . . Gastric cancer MGC-803 cell . REF102410 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 25.64 uM . . . Glioma C6 cell . REF101850 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 250 nM . . . Invasive breast carcinoma MCF-7 cell . REF102247 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 250 nM . . . Chronic myeloid leukemia K562 cell . REF101265 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 250 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101165 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 250 nM . . . Prostate carcinoma PC-3 cell . REF101018 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 250 nM . . . Invasive breast carcinoma T-47D cell . REF100864 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 250 nM . . . Lung small cell carcinoma NCI-H187 cell . REF100761 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 250 nM . . . Gastric carcinoma NUGC-3 cell . REF100746 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 250 nM . . . Lung small cell carcinoma H69AR cell . REF100917 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 250 nM . . . Acute myeloid leukemia HL-60 cell . REF101142 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 250 nM . . . Pancreatic adenocarcinoma SW1990 cell . REF100126 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 251 nM . . . Colon cancer HT29 cell . REF100987 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 251.19 nM . . . Melanoma M14 cell . REF102222 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 253.64 uM . . . Endocervical adenocarcinoma HeLa cell . REF100068 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 26 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF101045 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 26 nM . . . Colon cancer HT29 cell . REF100349 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 26 nM . . . Invasive breast carcinoma T-47D cell . REF100740 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 26 nM . . . Lung adenocarcinoma NCI-H838 cell . REF100689 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 26 nM . . . Melanoma LOX IMVI cell . REF100246 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 26 nM . . . Invasive breast carcinoma MCF-7 cell . REF102138 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 26 ug/mL . . . Erythroleukemia HEL cell . REF100043 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 26 uM . . . Lung adenocarcinoma A-549 cell . REF101959 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 26 uM . . . Normal Vero cell . REF100005 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 26.0±8.0 nM 24 h . . Melanoma B16 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 26.1 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101639 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 26.1 uM . . . Invasive breast carcinoma MCF-7 cell . REF101153 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 26.18 uM . . . Endocervical adenocarcinoma HeLa cell . REF102354 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 26.18 uM . . . Renal carcinoma UO-31 cell . REF101566 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 26.2 ng/ml . . . Prostate carcinoma PC-3 cell . REF100234 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 26.2 ng/ml . . . Colon cancer HT29 cell . REF100224 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 26.2 uM . . . Breast carcinoma MCF7R cell . REF102157 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 26.26 uM . . . Colon adenocarcinoma SW480 cell . REF102166 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 26.34 uM . . . Hepatoblastoma Hep-G2 cell . REF102519 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 26.34 uM . . . Lung large cell carcinoma NCI-H460 cell . REF102519 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 26.4 nM . . . Ovarian serous adenocarcinoma OVCAR-5 cell . REF102292 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 26.41 nM 72 h . . Glioblastoma U-87MG cell "Further, IC50values of SN-38 and T7-SN-38 on U87MG cells at 72 h were determined. An estimated IC50value of 26.41nM was obtained for SN-38, which was considerably lower than an IC50value of 70.07nM obtained for the T7-SN-38 conjugate. These IC50data confirm the greater cytotoxicity of the pure drug compared to the conjugate at 72 h (p< 0.05)." REF00293 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 26.43 uM . . . Endocervical adenocarcinoma HeLa cell . REF100068 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 26.67 uM . . . Invasive breast carcinoma MCF-7 cell . REF102166 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 26.79 uM . . . Colon adenocarcinoma Caco-2 cell . REF101677 DRG00101 Vidarabine 50% inhibited minimum concentration (MIC50) = 26.8 ug/mL . . . Normal Vero cell . REF102026 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 26.81 uM . . . Lung adenocarcinoma A-549 cell . REF101316 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 26.9 uM . . . Invasive breast carcinoma MCF-7 cell . REF101748 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 260 nM . . . Colon adenocarcinoma HCT 15 cell . REF101489 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 260 nM . . . Lung adenocarcinoma A-549 cell . REF101484 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 260 nM . . . Hepatoma Bel-7402 cell . REF101013 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 260 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101013 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 260 nM . . . Colon cancer HT29 cell . REF100917 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 260 nM . . . Colon cancer HT29 cell . REF101851 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 260 nM . . . Colon adenocarcinoma HCC 2998 cell . REF101480 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 260 nM . . . Gingival squamous cell carcinoma Ca9-22 cell . REF100981 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 260 nM . . . Normal COLO205 cell . REF100513 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 260 nM . . . Colon cancer HT29 cell . REF102112 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 266 uM . . . Acute myeloid leukemia HL-60 cell . REF102273 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 27 ng/mL . . . Prostate carcinoma PC-3 cell . REF100572 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 27 nM . . . Acute myeloid leukemia HL-60 cell . REF100749 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 27 nM . . . Small cell lung carcinoma NCI-H69 cell . REF100351 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 27 nM . . . Melanoma B16 cell . REF101950 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 27 nM . . . Colon adenocarcinoma DLD-1 cell . REF100307 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 27 nM . . . Squamous carcinoma SCC-25 cell . REF100246 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 27 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100917 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 27.1 nM . . . Invasive breast carcinoma MCF-7 cell . REF101226 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 27.23 uM . . . Gliosarcoma SF539 cell . REF101566 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 27.5 ng/ml . . . Colon cancer HT29 cell . REF100188 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 27.5±9.1 nM 24 h . . Amelanotic melanoma HT168-M1/M9 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 27.6 ng/ml . . . Prostate carcinoma PC-3 cell . REF100258 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 27.8 ug/mL . . . Cervical squamous cell carcinoma ME-180 cell . REF100103 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 27.89 uM . . . Invasive breast carcinoma MCF-7 cell . REF102439 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 270 nM . . . Invasive breast carcinoma MCF-7 cell . REF102519 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 270 nM . . . Colon carcinoma HCT 116 cell . REF101789 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 270 nM . . . Lung adenocarcinoma A-549 cell . REF100992 DRG00024 Thapsigargin Half Maximal Inhibitory Concentration (IC50) = 270 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101074 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 273 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100688 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 275 nM . . . Lung carcinoma SW1573 cell . REF102148 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 28 ng/mL . . . Acute myeloid leukemia HL-60 cell . REF100300 DRG00045 Duocarmycin Sa Half Maximal Inhibitory Concentration (IC50) = 28 nM 72 h . . Invasive breast carcinoma MCF-7 cell "All cell lines demonstrated sensitivity toward the DSA-PABA payload 5 in the nanomolar range. The cleaved peptide 6, and the benzyl protected control peptide 4, had no appreciable effect on cell proliferation (>100 µM), suggesting that any observed cytotoxic activity is due to the DSA warhead. Interestingly, PDC 7, without the cathepsin B cleavable sequence, also had no appreciable effect on cell proliferation (>100 µM), despite possessing the active DSA DNA alkylating moiety. Perhaps this PDC is either not being taken up into cells or not being broken down by proteases and peptidases in the cell. In both cases, the warhead may not be reaching the nucleus, the site of action of the duocarmycins. Cell lines that demonstrated appreciable levels of TFα were sensitive to PDC 3. Interestingly, HCT116, which had relatively high TFα expression and cathepsin B activity, demonstrated the greatest sensitivity to PDC 3, approaching similar potency to the payload 5. Excitingly, A549, H292, and 16HBE14o, which showed no detectable TFα expression, appeared unaffected by PDC 3 up to 100 µM, suggesting that TFα expression is required for the efficacy of PDC 3." REF00117 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 28 nM . . . Acute myeloid leukemia HL-60 cell . REF101180 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 28 nM . . . Colon adenocarcinoma HCT 15 cell . REF100856 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 28 nM . . . Melanoma SK-MEL-2 cell . REF100772 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 28 nM . . . Invasive breast carcinoma MCF-7 cell . REF100310 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 28 nM . . . Melanoma B16 cell . REF101943 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 28 nM . . . Hepatoblastoma Hep-G2 cell . REF101249 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 28 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101111 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 28 nM . . . Lung adenocarcinoma A-549 cell . REF100492 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 28 nM . . . Lung adenocarcinoma A-549 cell . REF101890 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 28 nM . . . Melanoma UACC-62 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 28 nM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF100270 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 28 uM . . . Normal Vero cell . REF100047 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 28.1 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101568 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 28.2 pM . . . Chronic myeloid leukemia K562 cell . REF102468 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 28.3 uM . . . Lung adenocarcinoma A-549 cell . REF101153 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 28.4 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100242 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 28.4 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101841 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 28.7 ng/ml . . . Colon cancer HT29 cell . REF100455 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 28.7 nM . . . Colon adenocarcinoma SW626 cell . REF100354 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 28.7 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100354 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 28.8 uM . . . Hepatoblastoma Hep-G2 cell . REF101542 DRG00107 Betulinic acid Half Maximal Cytotoxicity Concentration (CC50) = 28.9 uM . . . Cervical squamous cell carcinoma SiHa cell . REF101568 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 280 nM . . . Gastric carcinoma SNU-638 cell . REF101138 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 280 nM . . . Invasive breast carcinoma MCF-7 cell . REF100823 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 280 nM . . . Colon cancer HT29 cell . REF101870 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 280 nM . . . Breast adenocarcinoma SK-BR-3 cell . REF101774 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 280 nM . . . Chronic myeloid leukemia K562 cell . REF101438 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 280 nM . . . Normal V79 cell . REF101334 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 280 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100761 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 280 nM . . . Colon cancer HT29 cell . REF100243 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 280 nM . . . Prostate carcinoma DU145 cell . REF102389 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 280 ug/mL . . . Small cell lung carcinoma NCI-H69 cell . REF102285 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 287.6±35.1 nM 24 h . . Normal MRC-5 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 29 ng/mL . . . Glioma XF498 cell . REF100768 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 29 ng/mL . . . Prostate carcinoma PC-3 cell . REF100338 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 29 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100152 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 29 nM . . . Prostate carcinoma DU145 cell . REF101241 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 29 nM . . . Lymphoblastic leukemia L1210 cell . REF100535 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 29 nM . . . Lung adenocarcinoma A-549 cell . REF100147 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 29 nM . . . Invasive breast carcinoma MCF-7 cell . REF100126 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 29 uM . . . Lung large cell carcinoma NCI-H460 cell . REF101042 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 29 uM . . . Minimally invasive lung adenocarcinoma NCI-H322M cell . REF101689 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 29 uM . . . Gastric carcinoma SGC-7901 cell . REF102295 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 29 uM . . . Normal Vero cell . REF100082 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 29.2 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100141 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 29.3 nM . . . Invasive breast carcinoma MCF-7 cell . REF101226 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 29.5 uM . . . Lung adenocarcinoma A-549 cell . REF101732 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 29.53 uM . . . Cervical carcinoma L02 cell . REF102473 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 29.6 uM . . . Gastric adenocarcinoma AGS cell . REF102395 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 29.87 uM . . . Hepatoblastoma Hep-G2 cell . REF102293 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 29.98 uM . . . Hepatoblastoma Hep-G2 cell . REF102314 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 290 nM . . . Colon adenocarcinoma SW480 cell . REF101693 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 290 nM . . . Endocervical adenocarcinoma HeLa cell . REF100842 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 290 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100454 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 290 nM . . . Glioblastoma SF-295 cell . REF100658 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 291 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100532 DRG00023 Tesaglitazar Mcp-1 level = 298 pg/mL Every day 2.5 μM db/db mice model. . . "Whereas in the vehicle/untreated mice, the HbA1C values increased by approximately 2%, a graduated reduced increase was seen for [F7, P34]-NPY (2), peptide conjugate (3), and tesa (Figure 8A). Body temperature, which decreased to 35 C in the vehicle/untreated db/db controls, was normalized to 36 C in all of the treated mice including the mice treated with [F7, P34]-NPY (2) (Figure 8B). Treatment with tesa and tesa-NPY (3) led to normalization of the plasma concentration of ketone bodies and adiponectin, whereas [F7, P34]-NPY (2) and vehicle/untreated showed no effect (Figure 8C/E). Treatment had no major influence on the insulin and Mcp-1 levels (Figure 8D/G). The serum leptin concentration was reduced in the mice treated with tesa, whereas no reduction was detectable in all of the other treated mice (Figure 8F)." REF00088 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 299 nM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100374 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 299 nM . . . Breast carcinoma MCF7R cell . REF100245 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 µM 36 h . . Amelanotic melanoma LO #2 cell "Doxorubicin (DOX) is one of the most effective anticancer drugs and has been successfully used in clinical practice. However, DOX cannot differentiate between cancer cells and normal cells, which may induce unwanted side effects and severe toxicity. Compared with traditional small-molecule anticancer drugs, the peptide-drug conjugates (PDCs) have enhanced targeting specificity and water solubility. Based on these advantages, to further explore the function of 10a, we designed and prepared a anticancer PDC drug compound RGD-GFLG-DOX containing the tetrapeptide linker Gly-Phe-Leu-Gly, which can be cleaved in presence of cathepsin B, a highly upregulated enzyme in malignant tumors, to release the drug. RGD-GFLG was synthesized as a control. The inhibitory effects of RGD-GFLG-DOX on cancer cell lines were assessed using cytotoxicity assay. Specifically, the effects of RGD-GFLG-DOX were evaluated on integrin αvβ3-positive cancer cell lines, including A549 and U87MG cells, integrin αvβ3-negative cancer cell lines such as HeLa and MCF-7 cells, as well as normal cell lines, namely LO2 and MIHA cells. RGD-GFLG-DOX exhibited a lower cytotoxicity on HeLa, MCF-7, LO2 and MIHA cells, but a stronger cytotoxicity than DOX on A549 and U87MG cells. For comparison, RGD-GFLG demonstrated minimal cytotoxicity. In addition, the cytotoxicity of RGD-GFLG-DOX with various concentrations (040µM) on A549 and U87MG cells was studied. The results showed that the cytotoxicity of RGD-GFLG-DOX on A549 and U87MG cells was dose-dependent. These indicate that RGD-GFLG-DOX has a good specificity and inhibitory activity toward integrin αvβ3-overexpressed A549 and U87MG cells." REF00270 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 3 ng/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100768 DRG00019 Methotrexate Half Maximal Infective Dose (ID50) = 3 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102001 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 3 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102065 DRG00009 Camptothecin Half Maximal Cytotoxicity Concentration (CC50) = 3 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102288 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101468 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Invasive breast carcinoma MCF-7 cell . REF101253 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Hepatocellular carcinoma SMMC-7721 cell . REF101001 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Colon adenocarcinoma HCT 15 cell . REF100751 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100650 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100540 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101342 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100839 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 3 nM . . . Lung adenocarcinoma A-549 cell . REF100724 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Normal MT4 cell . REF100687 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100518 DRG00012 Paclitaxel Half Maximal Lethal Concentration (IC50) = 3 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102524 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101829 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Endocervical adenocarcinoma HeLa cell . REF101811 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Invasive breast carcinoma MCF-7 cell . REF101805 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101624 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Ovarian mixed germ cell tumor PA-1 cell . REF101549 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Lung adenocarcinoma A-549 cell . REF101293 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3 nM . . . Astrocytoma U-251MG cell . REF101218 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3 nM . . . Ovarian carcinoma 2008 cell . REF101151 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3 nM . . . Normal COLO205 cell . REF100987 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Colon cancer HT29 cell . REF100936 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100908 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 3 nM . . . Prostate carcinoma DU145 cell . REF100862 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3 nM . . . Colon adenocarcinoma HCC 2998 cell . REF100587 DRG00013 Gemcitabine Half Maximal Growth Inhibition (GI50) = 3 nM . . . Colon adenocarcinoma HCT 15 cell . REF102202 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Growth Inhibition (GI50) = 3 nM . . . Invasive breast carcinoma MCF-7 cell . REF102448 DRG00019 Methotrexate Half Maximal Infective Dose (ID50) = 3 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100022 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 3 nM . . . Normal MT4 cell . REF102053 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 3 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102053 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF102463 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Lymphoblastic leukemia L1210 cell . REF102404 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 3 nM . . . Cutaneous melanoma SK-MEL-5 cell . REF102357 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 3 nM . . . Colon adenocarcinoma SW620 cell . REF102315 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 3 nM . . . Colon carcinoma HCT 116 cell . REF102315 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 3 nM . . . Plasma cell myeloma RPMI-8226 cell . REF102290 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Normal HBL-100 cell . REF102237 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Lung large cell carcinoma NCI-H460 cell . REF102096 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3 nM . . . Endocervical adenocarcinoma HeLa cell . REF101277 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3 uM . . . Lung large cell carcinoma NCI-H460 cell . REF102260 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 3 uM . . . Breast adenocarcinoma SK-BR-3 cell . REF100823 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 uM . . . Endocervical adenocarcinoma HeLa cell . REF101868 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 uM . . . Prostate carcinoma PC-3 cell . REF101868 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 uM . . . HPV-related endocervical adenocarcinoma M-HeLa cell . REF101837 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 uM . . . Invasive breast carcinoma MCF-7 cell . REF101766 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 uM . . . Small cell lung carcinoma NCI-H69 cell . REF100610 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100408 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 3 uM . . . Normal COLO205 cell . REF102228 DRG00221 Acyclovir Half Maximal Effective Concentration (EC50) = 3 uM . . . Normal Vero cell . REF100060 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.01 nM . . . Endocervical adenocarcinoma HeLa cell . REF101386 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.02±0.49 µM 48 h . . Normal MCF-10A cell "HER2 positive SK-BR-3, NCIN87 and SK-OV-3 cells, and HER2 negative MDA-MB-231 and MCF-10A cells were selected to determine the cell activity of the target conjugates. From Table 3, most conjugates showed certain cytotoxicity to three HER2 positive cell lines. Among the three connection sites (S1S3), compounds 1, 4, and 7 with the first connection mode showed better activity. In the three HER2 positive SK-BR-3, NCIN87 and SK-OV-3 cells, conjugate 4 exhibited superior activity (IC50s of 0.53 0.17 µM, 1.58 0.41 µM, 2.50 0.78 µM, respectively), which almost equal to that of CPT (IC50s of 0.38 0.11 µM, 2.07 0.67 µM, 4.07 1.82 µM, respectively). The activity of conjugate 4 on HER2 positive cells was superior to that of conjugate 1 and 7. In MDA-MB-231 and MCF-10A cells, IC50s of conjugate 4 were 18.44 2.09 µM and 17.76 1.35 µM, respectively, which showed great tumor cell selectivity. Based on the above, conjugate 4 with better in vitro antitumor activity was selected for subsequent biological study." REF00288 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.04 uM . . . Laryngeal carcinoma HEp-2 cell . REF101556 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.05±1.24 µM 48 h . . Normal MCF-10A cell "To evaluated the in vitro anti-tumor activity of the conjugates, HER2-positive SK-BR-3, NCI-N87, HER2-negative MDA-MB-231 and normal MCF-10A cells were selected. As shown in Table 2, nearly all conjugates exhibited obvious anti-proliferation activity against SK-BR-3 cells, while most of the conjugates, except for Z6 and Z9, demonstrated different degrees of inhibitory activity on NCI-N87 cells. Taken together, Z8 and Z11 exhibited superior anti-tumor activity. The antiproliferative activity of Z8 against NCI-N87 cells (IC50 = 1.91 0.71 µM) was comparable to that of CPT (IC50 = 2.10 1.34 µM), while the antiproliferative activity of Z11 against SK-BR-3 cells (IC50 = 0.41 0.13 µM) was comparable to that of CPT (IC50 = 0.26 0.06 µM). Additionally, the IC50 values of these two conjugates against MDA-MB-231 and MCF-10A cells were significantly increased, showing their ability to selectively inhibit tumor cells. Based on the above results, Z8 and Z11, which exhibited better activity and apparent selectivity, were selected for subsequent studies." REF00312 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.09 uM . . . Bladder carcinoma T24 cell . REF101722 DRG00023 Tesaglitazar Insulin level = 3.1 ng/mL Every day 2.5 μM db/db mice model. . . "Whereas in the vehicle/untreated mice, the HbA1C values increased by approximately 2%, a graduated reduced increase was seen for [F7, P34]-NPY (2), peptide conjugate (3), and tesa (Figure 8A). Body temperature, which decreased to 35 C in the vehicle/untreated db/db controls, was normalized to 36 C in all of the treated mice including the mice treated with [F7, P34]-NPY (2) (Figure 8B). Treatment with tesa and tesa-NPY (3) led to normalization of the plasma concentration of ketone bodies and adiponectin, whereas [F7, P34]-NPY (2) and vehicle/untreated showed no effect (Figure 8C/E). Treatment had no major influence on the insulin and Mcp-1 levels (Figure 8D/G). The serum leptin concentration was reduced in the mice treated with tesa, whereas no reduction was detectable in all of the other treated mice (Figure 8F)." REF00088 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.1 ng/mL . . . Colon cancer HT29 cell . REF101998 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.1 ng/mL . . . Mouse melanoma B16-F10 cell . REF101998 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.1 nM . . . Invasive breast carcinoma MCF-7 cell . REF100280 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.1 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101675 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.1 nM . . . Invasive breast carcinoma MCF-7 cell . REF101432 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.1 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100806 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.1 nM . . . Invasive breast carcinoma MCF-7 cell . REF102229 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.1 nM . . . Lymphoma P388 cell . REF102196 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 3.1 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100657 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.1 uM . . . Colon adenocarcinoma LoVo cell . REF100880 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.1 uM . . . Lung adenocarcinoma A-549 cell . REF100711 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.1 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101715 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 3.1 uM . . . Invasive breast carcinoma MCF-7 cell . REF100140 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 3.1 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100193 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.1 uM . . . Colon cancer HT29 cell . REF102510 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.13 uM . . . Lung adenocarcinoma A-549 cell . REF101283 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.137 uM . . . Acute myeloid leukemia HL-60 cell . REF100989 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.14 nM . . . Lung adenocarcinoma A-549 cell . REF100990 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.14 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100875 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.16 uM . . . Lung adenocarcinoma A-549 cell . REF101692 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.16 uM . . . Prostate carcinoma PC-3 cell . REF100821 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.162 nM . . . Gliosarcoma SF539 cell . REF100274 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.162 nM . . . Invasive breast carcinoma MCF-7 cell . REF100274 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.162 nM . . . Invasive breast carcinoma Hs 578T cell . REF100274 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.162 nM . . . Normal COLO205 cell . REF100274 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.162 nM . . . Lymphoma P388 cell . REF102086 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.16228 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100274 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 3.16228 uM . . . Non-small cell lung carcinoma NCI-H522 cell . REF100756 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 3.16228 uM . . . Cutaneous melanoma SK-MEL-28 cell . REF102222 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.164 uM . . . Ovarian endometrioid adenocarcinoma A2780/Taxol cell . REF101883 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.17±1.15 µM 48 h . . Breast adenocarcinoma MDA-MB-231 cell "To evaluated the in vitro anti-tumor activity of the conjugates, HER2-positive SK-BR-3, NCI-N87, HER2-negative MDA-MB-231 and normal MCF-10A cells were selected. As shown in Table 2, nearly all conjugates exhibited obvious anti-proliferation activity against SK-BR-3 cells, while most of the conjugates, except for Z6 and Z9, demonstrated different degrees of inhibitory activity on NCI-N87 cells. Taken together, Z8 and Z11 exhibited superior anti-tumor activity. The antiproliferative activity of Z8 against NCI-N87 cells (IC50 = 1.91 0.71 µM) was comparable to that of CPT (IC50 = 2.10 1.34 µM), while the antiproliferative activity of Z11 against SK-BR-3 cells (IC50 = 0.41 0.13 µM) was comparable to that of CPT (IC50 = 0.26 0.06 µM). Additionally, the IC50 values of these two conjugates against MDA-MB-231 and MCF-10A cells were significantly increased, showing their ability to selectively inhibit tumor cells. Based on the above results, Z8 and Z11, which exhibited better activity and apparent selectivity, were selected for subsequent studies." REF00312 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 3.184 uM . . . Colon cancer HT29 cell . REF101871 DRG00009 Camptothecin Half Maximal Effective Dosage (ED50) = 3.2 nM . . . Invasive breast carcinoma MCF-7 cell . REF100549 DRG00009 Camptothecin Half Maximal Effective Dosage (ED50) = 3.2 nM . . . Ovarian adenocarcinoma A2780-1A9 cell . REF100549 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.2 nM . . . Colon cancer HT29 cell . REF101967 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.2 nM . . . Osteosarcoma SJSA-1 cell . REF100626 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.2 nM . . . Colon adenocarcinoma HCT 15 cell . REF102479 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 3.2 nM . . . Lymphoma P388 cell . REF102040 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.2 ug/mL . . . Lung adenocarcinoma A-549 cell . REF101973 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.2 ug/mL . . . Normal Vero cell . REF100697 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.2 uM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF102273 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.2 uM . . . Diffuse large B-cell lymphoma RL cell . REF100763 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.2 uM . . . Prostate carcinoma DU145 cell . REF100841 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.2 uM . . . Lymph node metastasis of prostate carcinoma LNCaP C4-2 cell . REF101619 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.2 uM . . . Neuroblastoma IMR-32 cell . REF101495 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 3.2 uM . . . Cutaneous melanoma SK-MEL-5 cell . REF100140 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.2 uM . . . Invasive breast carcinoma MCF-7 cell . REF101260 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 3.2 uM . . . Colon carcinoma HCT 116 cell . REF102383 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.2 uM . . . Chronic myeloid leukemia K562 cell . REF102196 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.21 nM . . . Colon carcinoma HCT 116 cell . REF100831 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.22 uM . . . Invasive breast carcinoma MCF-7 cell . REF101985 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.22 uM . . . Hepatocellular carcinoma SMMC-7721 cell . REF102192 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 3.23 nM . . . Invasive breast carcinoma MCF-7 cell . REF100482 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.24 uM . . . Lung adenocarcinoma A-549 cell . REF101826 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.24 uM . . . Normal NIH3T3 cell . REF101163 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.24 uM . . . Endocervical adenocarcinoma HeLa cell . REF100796 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.27 uM . . . Prostate carcinoma DU145 cell . REF101931 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.27 uM . . . Cervical carcinoma L02 cell . REF102522 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 3.28 nM . . . Lymphoblastic leukemia L1210 cell . REF100174 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.28 uM . . . Invasive breast carcinoma MCF-7 cell . REF101658 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 3.28 uM . . . Invasive breast carcinoma MCF-7 cell . REF102185 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.29 nM . . . Stomach adenocarcinoma BGC-823 cell . REF100999 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.29 uM . . . Ileocecal adenocarcinoma HCT-8 cell . REF100666 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 3.29-0.44 µM 72 h . . Endocervical adenocarcinoma HeLa cell "To deliver the functional molecule into the cells, we attached an anticancer drug, methotrexate (MTX), to the N-terminus of STRAPs. The peptides were tested for their capability to deliver the active drug molecule in breast and cervical cancer cells. MDA-MB-231 and HeLa cells were treated with varying concentrations of MTX and STRAP-MTX conjugates for 72 h. Cell viability was assessed using the MTT assay. The cytotoxicity of MTX increased when delivered as peptideMTX conjugates to the cells. This resulted in an overall reduction in the inhibitory concentration cytotoxic to 50% of cells (IC50) for MTX. The MTX resistance for MDA-MB-231 cells is well-established. The IC50 for MTX in MDA-MB-231 cells was minimum when delivered as a STRAP-4MTX conjugate. Similar lowering of IC50 values in HeLa cells was observed. We also treated HEK-293 cells with MTXSTRAP conjugates. The peptidedrug conjugates showed no significant toxicity to the HEK-293 cells under the tested conditions, thereby confirming the earlier reported observation of higher uptake rates in cancerous cells." REF00225 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.3 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF101796 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.3 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101315 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.3 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101248 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.3 nM . . . Stomach adenocarcinoma BGC-823 cell . REF100759 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.3 nM . . . Normal COLO205 cell . REF100536 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 3.3 nM . . . Lung large cell carcinoma NCI-H460 cell . REF102180 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.3 nM . . . Endocervical adenocarcinoma HeLa cell . REF101682 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 3.3 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100889 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.3 ug/mL . . . Colon carcinoma HCT 116 cell . REF100866 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.3 uM . . . Lung adenocarcinoma A-549 cell . REF101416 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.3 uM . . . Prostate carcinoma PC-3 cell . REF100868 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.3 uM . . . Endocervical adenocarcinoma HeLa cell . REF100530 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 3.36 uM . . . Acute monocytic leukemia MV4-11 cell . REF102211 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.388 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101433 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.39 uM . . . Normal COLO205 cell . REF102320 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.39 uM . . . Hepatoblastoma Hep-G2 cell . REF101415 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.4 ng/mL . . . Lung adenocarcinoma A-549 cell . REF101918 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.4 nM . . . Lung adenocarcinoma A-549 cell . REF101701 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.4 nM . . . Prostate carcinoma DU145 cell . REF101308 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.4 nM . . . Osteosarcoma U2OS cell . REF101107 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.4 nM . . . Colon cancer HT29 cell . REF100765 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.4 nM . . . Prostate carcinoma PC-3 cell . REF100465 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.4 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100230 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 3.4 nM . . . Lymphoblastic leukemia L1210 cell . REF100138 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.4 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101860 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 3.4 ug/mL . . . Colon carcinoma KM-20L2 cell . REF102113 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.4 uM . . . Lung adenocarcinoma A-549 cell . REF101687 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.4 uM . . . Osteosarcoma U2OS cell . REF101085 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.4 uM . . . Normal HMEC-1 cell . REF102445 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 3.41 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100184 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.41 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101980 DRG00407 Combretastatin A4 Half Maximal Effective Concentration (EC50) = 3.45 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF102377 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.45 uM . . . Hepatoblastoma Hep-G2 cell . REF101276 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.46 uM . . . Acute myeloid leukemia HL-60 cell . REF102417 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.5 ng/mL . . . Lung adenocarcinoma A-549 cell . REF101352 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.5 ng/mL . . . Embryonic hepatoma WRL68 cell . REF100483 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.5 nM . . . Endocervical adenocarcinoma HeLa cell . REF101294 DRG00407 Combretastatin A4 Half Maximal Effective Concentration (EC50) = 3.5 nM . . . Skin squamous cell carcinoma A431 cell . REF102125 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.5 nM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF101632 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.5 nM . . . Breast ductal carcinoma BT-549 cell . REF100974 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.5 ug/mL . . . Acute monocytic leukemia U-937 cell . REF102013 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 3.5 ug/mL . . . Breast adenocarcinoma MDA-MB-231 cell . REF100657 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.5 uM . . . Invasive breast carcinoma MCF-7 cell . REF101053 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.5 uM . . . Hepatoblastoma Hep-G2 cell . REF101291 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 3.5 uM . . . Normal Vero cell . REF100090 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 3.5 uM . . . Colon carcinoma HCT 116 cell . REF102367 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.52 uM . . . Lung adenocarcinoma A-549 cell . REF101640 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 3.54 uM . . . Endocervical adenocarcinoma HeLa cell . REF102467 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 3.54813 uM . . . Chronic myeloid leukemia K562 cell . REF100123 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 3.55 uM . . . Colon cancer HT29 cell . REF101768 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.55±0.21 µM 48 h . . Lung adenocarcinoma A-549 cell "DOX showed strong in vitro cytotoxicity against all four kinds of cells without tumor selectivity, with IC50 values of 1.65 0.20 M (U87), 1.58 0.19 M (HepG2), 3.55 0.21 M (A549), and 1.29 0.18 M (LO2), respectively" REF00315 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 3.56 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100189 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.57 uM . . . Prostate carcinoma DU145 cell . REF100798 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.6 nM . . . Lung adenocarcinoma A-549 cell . REF101967 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.6 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101519 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.6 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF100759 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.6 nM . . . Colon cancer HT29 cell . REF100230 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.6 nM . . . Chronic myeloid leukemia K562 cell . REF102189 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.6 uM . . . Colon adenocarcinoma HCT 15 cell . REF100896 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.6 uM . . . Lung adenocarcinoma A-549 cell . REF100883 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.6 uM . . . Gastric cancer MGC-803 cell . REF101773 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.6 uM . . . Normal Vero cell . REF100884 DRG00012 Paclitaxel 30% Inhibitory Concentration (IC30) = 3.6 uM . . . Lung large cell carcinoma NCI-H460 cell . REF100964 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.6 uM . . . Ileocecal adenocarcinoma HCT-8 cell . REF100832 DRG00314 9-Aminoacridine Half Maximal Inhibitory Concentration (IC50) = 3.6 uM . . . Ovarian endometrioid adenocarcinoma TOV-112D cell . REF102474 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.6 uM . . . Colon cancer HT29 cell . REF102224 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.61 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100797 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.66 nM . . . Gliosarcoma SF539 cell . REF100197 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 3.67 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100264 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.69 uM . . . Invasive breast carcinoma MCF-7 cell . REF101044 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.7 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF101333 DRG00076 Estradiol Half Maximal Effective Concentration (EC50) = 3.7 pM . . . Invasive breast carcinoma MCF-7 cell . REF102170 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.7 uM . . . Breast ductal carcinoma BT-549 cell . REF101132 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.7 uM . . . Endocervical adenocarcinoma HeLa cell . REF100961 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.7 uM . . . Normal NIH3T3 cell . REF100821 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.73 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF101028 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.73 ug/mL . . . Colon carcinoma HCT 116 cell . REF100970 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.76 uM . . . Lung adenocarcinoma A-549 cell . REF101790 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.8 nM . . . Gastric cancer MGC-803 cell . REF101819 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.8 nM . . . Colon carcinoma HCT 116 cell . REF101701 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.8 nM . . . Lung adenocarcinoma A-549 cell . REF102321 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.8 nM . . . Hepatocellular carcinoma SMMC-7721 cell . REF101578 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.8 ug/mL . . . Chronic myeloid leukemia K562 cell . REF102013 DRG00221 Acyclovir Half Maximal Effective Dosage (ED50) = 3.8 ug/mL . . . EBV-related Burkitt lymphoma Raji cell . REF100012 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.8 uM . . . Endocervical adenocarcinoma HeLa cell . REF101512 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.8 uM . . . Normal COLO205 cell . REF101764 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.8 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101443 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.8 uM . . . Acute myeloid leukemia HL-60 cell . REF101355 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.8 uM . . . Chronic myeloid leukemia K562 cell . REF101355 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 3.8 uM . . . Colon cancer HT29 cell . REF102454 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 3.80189 uM . . . Astrocytoma SNB-19 cell . REF100123 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 3.81 uM . . . Astrocytoma SNB-19 cell . REF102305 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 3.81 uM . . . Hepatoblastoma Hep-G2 cell . REF102219 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.82±0.91 µM 48 h . . Ovarian serous cystadenocarcinoma SK-OV-3 cell "The cytotoxicity of conjugates was evaluated on cell lines with different expression levels of HER2. The results showed that among all conjugates with a single CPT molecule (I-1 to I-3), I-1 was the most cytotoxic against three HER2-positive cell lines (SK-BR-3, NCI-N87, and SK-OV-3 cells), and the calculated IC50 values for the three cells were 1.47 0.54, 3.29 0.67, and 4.29 1.11 µM, respectively. Similarly, among all conjugates with two CPT molecules (I-4 to I-6), I-4 showed the highest cytotoxicity toward HER2-positive cells, and the IC50 values for SK-BR-3, NCI-N87, and SK-OV-3 cells were 0.12 0.07, 1.78 0.47, and 1.27 0.38 µM, respectively. The activity of I-4 against SK-BR-3 cells was also slightly better than that of the positive control CPT (IC50 = 0.21 0.04 µM). The cytotoxicity of I-1 and I-4 against HER2-negative MDA-MB-231 cells was comparatively lower (calculated IC50s were 7.60 1.23 and 7.72 0.92 µM, respectively). In contrast, CPT itself showed higher cytotoxicity against MDA-MB-231 (IC50 = 1.06 0.42 µM), indicating that conjugates showed higher specificity in cell targeting. Furthermore, the cytotoxicity of I-1 and I-4 against normal cells MCF-10A (IC50 = 23.90 1.58 and 17.14 2.42 µM, respectively) was significantly lower than that of CPT alone (2.58 0.77 µM). Based on these results, I-1 and I-4 were selected for subsequent biological evaluation." REF00244 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.86 uM . . . Chronic myeloid leukemia K562 cell . REF102456 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.86 uM . . . Prostate carcinoma PC-3 cell . REF101738 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.87 uM . . . Breast adenocarcinoma MDA-MB-468 cell . REF101380 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.88 uM . . . Normal MRC5 cell . REF101864 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.884 uM . . . Lymphoblastic leukemia L1210 cell . REF100237 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.89 uM . . . Invasive breast carcinoma MCF-7 cell . REF101780 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.9 nM . . . Prostate carcinoma DU145 cell . REF100673 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.9 nM . . . Pleural epithelioid mesothelioma NCI-H226 cell . REF101860 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.9 nM . . . Cervical epithelial carcinoma KB 3-1 cell . REF100439 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 3.9 nM . . . Lymphoblastic leukemia L1210 cell . REF100161 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 3.9 nM . . . Hepatoblastoma Hep-G2 cell . REF102390 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 3.9 ug/mL . . . Colon cancer HT29 cell . REF100889 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 3.9 ug/mL . . . Colon cancer HT29 cell . REF100221 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.9 ug/mL . . . Breast adenocarcinoma MDA-MB-231 cell . REF100672 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.9 uM . . . Normal HEK293 cell . REF101659 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.92 uM . . . Endocervical adenocarcinoma HeLa cell . REF101376 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 3.93 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100254 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 3.94 uM . . . Chronic myeloid leukemia K562 cell . REF102486 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 3.97 uM . . . Colon carcinoma HCT 116 cell . REF100929 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 3.97 uM . . . Invasive breast carcinoma MCF-7 cell . REF101755 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.981 nM . . . Astrocytoma U-251MG cell . REF100274 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.981 nM . . . Colon adenocarcinoma HCC 2998 cell . REF100274 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.981 nM . . . Cutaneous melanoma SK-MEL-5 cell . REF100274 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 3.981 nM . . . Prostate carcinoma PC-3 cell . REF100274 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 3.98107 uM . . . Clear cell renal cell carcinoma Caki-1 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 3.98107 uM . . . Leukemia SR cell . REF100098 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 3.98107 uM . . . Colon carcinoma HCT 116 cell . REF100756 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 3.98107 uM . . . Non-small cell lung carcinoma NCI-H522 cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 3.98107 uM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF102222 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 3.99 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101614 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 30 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF102176 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 ng/mL . . . Acute myeloid leukemia HL-60 cell . REF100916 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 30 ng/mL . . . Invasive breast carcinoma MCF-7 cell . REF100889 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 30 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100873 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 ng/mL . . . Amelanotic melanoma MDA-MB-435 cell . REF100826 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 30 ng/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100488 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 30 ng/mL . . . Melanoma SK-MEL-2 cell . REF100404 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 ng/mL . . . Recurrent bladder carcinoma HT-1197 cell . REF100308 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 30 ng/mL . . . Colon cancer HT29 cell . REF100559 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 30 ng/mL . . . Lymphoma P388 cell . REF100248 DRG00296 Zidovudine Half Maximal Infective Dose (ID50) = 30 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100011 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Colon cancer HT29 cell . REF101761 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Colon carcinoma HCT 116 cell . REF101761 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Invasive breast carcinoma MCF-7 cell . REF101761 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Lung adenocarcinoma A-549 cell . REF101761 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 30 nM . . . Colon carcinoma HCT 116 cell . REF101222 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100950 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Prostate carcinoma PC-3 cell . REF100896 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Lymphoblastic leukemia L1210 cell . REF100362 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100291 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 30 nM . . . Colon adenocarcinoma SW620 cell . REF101954 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101953 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF101831 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 30 nM . . . Leukemia SR cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 30 nM . . . Non-small cell lung carcinoma NCI-H522 cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 30 nM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Colon adenocarcinoma Caco-2 cell . REF101403 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Acute myeloid leukemia HL-60 cell . REF101101 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF101073 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Lung small cell carcinoma NCI-H187 cell . REF100972 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 30 nM . . . Chronic myeloid leukemia K562 cell . REF100822 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Lymphoblastic leukemia CCRF-SB cell . REF100687 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100506 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100437 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Non-small cell lung carcinoma LXFL 529 cell . REF100394 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . EBV-related Burkitt lymphoma Raji cell . REF100371 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Lung squamous cell carcinoma SK-MES-1 cell . REF100370 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Prostate carcinoma DU145 cell . REF100370 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 30 nM . . . Invasive breast carcinoma T-47D cell . REF102118 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Osteosarcoma U2OS cell . REF101903 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101527 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 30 nM . . . Normal Vero cell . REF101218 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Promyelocytic leukemia NB-4 cell . REF101148 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 30 nM . . . Invasive breast carcinoma MCF-7 cell . REF101114 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 30 nM . . . Cervical squamous cell carcinoma SiHa cell . REF100828 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Endocervical adenocarcinoma HeLa cell . REF100805 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Lymphoma P388/ADR cell . REF100521 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Colon carcinoma HCT 116 cell . REF102406 DRG00019 Methotrexate Half Maximal Infective Dose (ID50) = 30 nM . . . Sezary syndrome H9 cell . REF102009 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Colon adenocarcinoma HCT 15 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Lymphoblastic leukemia L1210 cell . REF100167 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 30 nM . . . Sezary syndrome H9 cell . REF102010 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 30 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101761 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 30 uM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF102277 DRG00081 Cytarabine Half Maximal Effective Dosage (ED50) = 30 uM . . . Acute myeloid leukemia HL-60 cell . REF100017 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 30.1 ng/ml . . . Colon cancer HT29 cell . REF100189 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 30.21 uM . . . Endocervical adenocarcinoma HeLa cell . REF102428 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 30.3 nM . . . Prostate carcinoma TRAMP-C2H cell . REF100412 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 30.48 uM . . . Hepatoblastoma Hep-G2 cell . REF102398 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 30.5 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102014 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 30.62 uM . . . Astrocytoma U-251MG cell . REF101566 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 30.7 uM . . . Hepatoblastoma Hep-G2 cell . REF101051 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 30.74 uM . . . Hepatoblastoma Hep-G2 cell . REF100957 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 30.9 ug/mL . . . Colon cancer HT29 cell . REF100103 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 30.9 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100082 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Normal HaCaT cell . REF102271 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Invasive breast carcinoma MCF-7 cell . REF100763 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Lymphoblastic leukemia L1210 cell . REF100016 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Hepatoblastoma Hep-G2 cell . REF100675 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Hepatoblastoma Hep-G2 cell . REF101965 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 300 nM . . . Invasive breast carcinoma MCF-7 cell . REF101657 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 300 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101657 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Colon adenocarcinoma LoVo cell . REF101483 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Colon carcinoma HCT 116 cell . REF101085 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101006 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF101006 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Prostate carcinoma PC-3 cell . REF101006 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Burkitt lymphoma Daudi cell . REF100610 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 300 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100566 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 300 nM . . . Colon cancer HT29 cell . REF100566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100521 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100410 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Lung adenocarcinoma L2987 cell . REF100390 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Invasive breast carcinoma MCF-7 cell . REF100253 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Invasive breast carcinoma MCF-7 cell . REF101967 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Hepatoblastoma Hep-G2 cell . REF100598 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 300 nM . . . Colon adenocarcinoma HCT 15 cell . REF100448 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Endocervical adenocarcinoma HeLa cell . REF102501 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Lung adenocarcinoma A-549 cell . REF102501 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Prostate carcinoma LNCaP cell . REF101063 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 300 nM . . . Normal MT4 cell . REF102038 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 300 nM . . . Lung adenocarcinoma A-549 cell . REF101142 DRG00280 Erythromycin Half Maximal Inhibitory Concentration (IC50) = 300 ug/mL . . . Osteosarcoma MG-63 cell . REF100093 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 304 nM . . . Renal carcinoma Renca cell . REF100496 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 307 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101559 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 31 nM . . . Acute myeloid leukemia HL-60 cell . REF101460 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 31 nM . . . Lung adenocarcinoma A-549 cell . REF100640 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 31 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF100246 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 31 nM . . . Hypopharyngeal squamous cell carcinoma FaDu cell . REF100193 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 31 uM . . . Colon adenocarcinoma Caco-2 cell . REF101506 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 31 uM . . . Normal MT-2 cell . REF102010 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 31.04 uM . . . Invasive breast carcinoma MCF-7 cell . REF102473 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 31.3 uM . . . Hepatoblastoma Hep-G2 cell . REF101112 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 31.5 nM . . . Melanoma B16 cell . REF101996 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 31.6 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF102253 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 31.6 uM . . . Chronic myeloid leukemia K562 cell . REF101275 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 31.6 uM . . . Chronic myeloid leukemia K562 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 31.6 uM . . . Colon adenocarcinoma KM12 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 31.6 uM . . . Glioblastoma SF-295 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 31.6 uM . . . Leukemia SR cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 31.6 uM . . . Melanoma SK-MEL-2 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 31.6 uM . . . Non-small cell lung carcinoma NCI-H522 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 31.6 uM . . . Normal COLO205 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 31.6 uM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 31.6 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102249 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 31.6 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF102362 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 31.62 nM . . . Hepatoblastoma Hep-G2 cell . REF100517 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 31.62 nM . . . Normal H9c2 cell . REF100517 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 31.62 nM . . . Prostate carcinoma DU145 cell . REF100517 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 31.62 nM . . . Pleural epithelioid mesothelioma NCI-H226 cell . REF100274 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 31.62 nM . . . Chronic myeloid leukemia K562 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 31.62 nM . . . Colon adenocarcinoma HCT 15 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 31.62 nM . . . Colon carcinoma HCT 116 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 31.62 nM . . . Lung large cell carcinoma NCI-H460 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 31.62 nM . . . Prostate carcinoma PC-3 cell . REF100104 DRG00009 Camptothecin Tumor Growth Inhibition value (TGI) = 31.62 uM . . . Colon cancer HT29 cell . REF100902 DRG00009 Camptothecin Half Maximal Lethal Concentration (IC50) = 31.62 uM . . . Colon cancer HT29 cell . REF100902 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 31.62278 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100098 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 31.72 uM . . . Colon carcinoma HCT 116 cell . REF102275 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 31.9 uM . . . Chronic myelogenous leukemia K562/Adr cell . REF102480 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 310 nM . . . Lung squamous cell carcinoma SK-MES-1 cell . REF100154 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 310 nM . . . Colon cancer HT29 cell . REF101235 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 310 nM . . . Colon adenocarcinoma LoVo cell . REF100962 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 310 nM . . . Invasive breast carcinoma MCF-7 cell . REF100665 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 310 nM . . . Breast adenocarcinoma MDA-MB-468 cell . REF101963 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 310 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF102185 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 311 nM . . . Cervical squamous cell carcinoma SiHa cell . REF101779 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 312 nM . . . Colon adenocarcinoma SW480 cell . REF100395 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 316.22777 uM . . . Non-small cell lung carcinoma EKVX cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 316.23 nM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100123 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 316.23 nM . . . Pancreatic ductal adenocarcinoma BxPC-3 cell . REF100589 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 316.23 nM . . . Prostate carcinoma PC-3 cell . REF100589 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 316.23 nM . . . Invasive breast carcinoma MCF-7 cell . REF100517 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 319.3 nM . . . Lung carcinoma COR-L23 cell . REF100350 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 32 nM . . . Acute monocytic leukemia U-937 cell . REF100522 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 32 nM . . . Lymphoma P388 cell . REF100284 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 32 nM . . . Colon cancer HT29 cell . REF100246 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 32 nM . . . Acute myeloid leukemia HL-60 cell . REF101705 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 32 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101588 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 32 nM . . . Invasive breast carcinoma MCF-7 cell . REF102207 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 32 nM . . . Colon cancer HT29 cell . REF100749 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 32 uM . . . Prostate carcinoma PC-3 cell . REF100359 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 32.02 uM . . . Invasive breast carcinoma MCF-7 cell . REF100898 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 32.18 uM . . . Invasive breast carcinoma MCF-7 cell . REF101145 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 32.4 ug/mL . . . Renal carcinoma A498 cell . REF100982 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 32.4 uM . . . Melanoma M14 cell . REF102215 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 32.57 uM . . . Hepatoblastoma Hep-G2 cell . REF102486 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 32.6 uM . . . Hepatoblastoma Hep-G2 cell . REF102381 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 32.7±4.7 nM 24 h . . Prostate carcinoma PC-3 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 32.72 uM . . . Colon adenocarcinoma SW480 cell . REF101965 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 320 nM . . . Invasive breast carcinoma MCF-7 cell . REF100422 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 320 nM . . . Melanoma UACC-62 cell . REF102223 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 320 nM . . . Prostate carcinoma PC-3 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 320 nM . . . Invasive breast carcinoma MCF-7 cell . REF101418 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 320 nM . . . Colon cancer HT29 cell . REF101181 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 320 nM . . . Chronic myeloid leukemia K562 cell . REF100728 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 320 nM . . . Astrocytoma U-251MG cell . REF100516 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 320 nM . . . Prostate carcinoma PC-3 cell . REF100380 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 324 nM . . . Invasive breast carcinoma MCF-7 cell . REF100829 DRG00224 Pemetrexed Half Maximal Inhibitory Concentration (IC50) = 327 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101603 DRG00045 Duocarmycin Sa Half Maximal Inhibitory Concentration (IC50) = 33 nM 72 h . . Acute myeloid leukemia HL-60 cell "All cell lines demonstrated sensitivity toward the DSA-PABA payload 5 in the nanomolar range. The cleaved peptide 6, and the benzyl protected control peptide 4, had no appreciable effect on cell proliferation (>100 µM), suggesting that any observed cytotoxic activity is due to the DSA warhead. Interestingly, PDC 7, without the cathepsin B cleavable sequence, also had no appreciable effect on cell proliferation (>100 µM), despite possessing the active DSA DNA alkylating moiety. Perhaps this PDC is either not being taken up into cells or not being broken down by proteases and peptidases in the cell. In both cases, the warhead may not be reaching the nucleus, the site of action of the duocarmycins. Cell lines that demonstrated appreciable levels of TFα were sensitive to PDC 3. Interestingly, HCT116, which had relatively high TFα expression and cathepsin B activity, demonstrated the greatest sensitivity to PDC 3, approaching similar potency to the payload 5. Excitingly, A549, H292, and 16HBE14o, which showed no detectable TFα expression, appeared unaffected by PDC 3 up to 100 µM, suggesting that TFα expression is required for the efficacy of PDC 3." REF00117 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 33 nM . . . Lymphoblastic leukemia L1210 cell . REF101960 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 33 nM . . . Chronic myeloid leukemia K562 cell . REF100824 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 33 nM . . . Colon adenocarcinoma LoVo cell . REF100454 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 33 nM . . . Breast adenocarcinoma MDA-MB-361 cell . REF100287 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 33 nM . . . Plasma cell myeloma RPMI-8226 cell . REF100134 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 33 nM . . . Colon adenocarcinoma KM12 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 33 nM . . . Lung adenocarcinoma A-549 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 33 nM . . . Plasma cell myeloma RPMI-8226 cell . REF100270 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 33 nM . . . Colon adenocarcinoma SW620 cell . REF100246 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 33 pM . . . Endocervical adenocarcinoma HeLa cell . REF101004 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 33 uM . . . Prostate carcinoma PC-3 cell . REF102217 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 33.5 uM . . . Chronic myeloid leukemia K562 cell . REF102221 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 33.8 nM . . . Colon carcinoma HCT 116 cell . REF101606 DRG00061 KLUKLUKKLUKLUK Half Maximal Inhibitory Concentration (IC50) = 33.8±0.98 µM 48 h . . Normal Human umbilical vein endothelial cell "The effect of the peptide conjugate QR-KLU on the proliferation of Huh7 and HUVEC cells was assessed by CCK8 assays. First, we investigated anti-proliferation ability of three peptides QR, KLU and QR-KLU on Huh7 and HUVEC cells with different concentrations. As shown in Fig. Fig.3A,3A, B, cells were treated with QR peptide, KLU peptide, QR-KLU peptide, DOX with different concentration respectively. The inhibition rate increased in a dose-dependent manner in KLU and QR-KLU groups in both cell lines. In HUVEC cells, peptide QR-KLU (IC50 10.70.292µM) showed more potent inhibition effect than KLU (IC50 33.80.98µM), and in Huh7 cells, QR-KLU (IC50 7.30.74µM) also showed more potent anti-tumor effect than KLU (IC50 36.272.7µM). Meanwhile, peptide QR showed negligible toxicity even under 80µM." REF00235 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 33.9 uM . . . Invasive breast carcinoma MCF-7 cell . REF101229 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 33.98 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101175 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 330 nM . . . Lymphoblastic leukemia L1210 cell . REF102366 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 330 nM . . . Lymphoblastic leukemia L1210 cell . REF100396 DRG00010 Daunorubicin Tumor Growth Inhibition value (TGI) = 330 nM . . . Colon cancer HT29 cell . REF102204 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 330 nM . . . Invasive breast carcinoma Hs 578T cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 330 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100867 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 330 nM . . . Colon cancer HT29 cell . REF100717 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 330 nM . . . Endocervical adenocarcinoma HeLa cell . REF100437 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 330 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF102472 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 330 nM . . . Hepatoblastoma Hep-G2 cell . REF102449 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 331.13 nM . . . Lung adenocarcinoma NCI-H23 cell . REF100123 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 336.2 uM . . . Normal HEK293 cell . REF101568 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 34 nM . . . Colon carcinoma CT26 cell . REF100496 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 34 uM . . . Hepatoblastoma Hep-G2 cell . REF101042 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 34.27 uM . . . Lung adenocarcinoma A-549 cell . REF102371 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 34.3 uM . . . Lung adenocarcinoma A549/TR cell . REF101909 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 34.57 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101307 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 34.75 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101566 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 34.9 ng/mL . . . Prostate carcinoma PC-3 cell . REF101911 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 340 nM . . . Nasopharyngeal carcinoma CNE cell . REF101670 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 340 nM . . . Colon cancer HT29 cell . REF101725 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 340 nM . . . Endocervical adenocarcinoma HeLa cell . REF101235 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 340 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101068 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 340 nM . . . Colon cancer HT29 cell . REF100275 DRG00012 Paclitaxel Median lethal dose (LD50) = 35 mg/kg 24 h 200 nM . Glioblastoma U-87MG cell "The reported LD50 values for PTX and ABRAXANE (albumin-bonded PTX) are 35 and 47 mg/kg, respectively. " REF00077 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 35 ng/mL . . . Chronic myeloid leukemia K562 cell . REF100239 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 35 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100146 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 35 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100291 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 35 nM . . . Renal carcinoma A498 cell . REF100582 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 35 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100310 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 35 nM . . . Glioblastoma SF-295 cell . REF100278 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 35 nM . . . Lymphoblastic leukemia L1210 cell . REF100237 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 35 nM . . . Lung adenosquamous carcinoma NCI-H596 cell . REF101490 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 35 nM . . . Breast carcinoma MX1 cell . REF100908 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 35 nM . . . Invasive breast carcinoma T-47D cell . REF100712 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 35 nM . . . Colon carcinoma HCT 116 cell . REF100346 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 35 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF102228 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 35 nM . . . Gliosarcoma SF539 cell . REF100270 DRG00012 Paclitaxel Half Maximal Lethal dose (LD50) = 35 uM . . . Normal WI-38 cell . REF102471 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 35 uM . . . Barrett adenocarcinoma OE33 cell . REF102217 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 35.05 uM . . . Lung adenocarcinoma A-549 cell . REF102275 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 35.1 ng/ml . . . Colon cancer HT29 cell . REF100258 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 35.1±14.9 nM 24 h . . Melanoma A2058 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 35.3 nM . . . Prostate carcinoma PC-3 cell . REF100442 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 35.48134 uM . . . Non-small cell lung carcinoma HOP-62 cell . REF100848 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 35.6 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100906 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 35.6 ug/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102065 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 35.6 uM . . . Normal MT4 cell . REF102155 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 35.6 uM . . . Normal MT4 cell . REF100063 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 35.66 uM . . . Hepatocellular carcinoma PLC/PRF/5 cell . REF102402 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 35.7 ng/ml . . . Colon cancer HT29 cell . REF100244 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 35.91 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102418 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 350 nM . . . Lung large cell carcinoma NCI-H661 cell . REF101699 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 350 nM . . . Invasive breast carcinoma MCF-7 cell . REF101662 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 350 nM . . . Glioma XF498 cell . REF100772 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 350 nM . . . Colon cancer HT29 cell . REF100520 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 350 nM . . . Lung adenocarcinoma A-549 cell . REF101755 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 350 nM . . . Acute myeloid leukemia HL-60 cell . REF102107 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 357 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100230 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 36 nM . . . Breast adenocarcinoma MDA-MB-361 cell . REF100287 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 36 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100219 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 36 nM . . . Invasive breast carcinoma MCF-7 cell . REF100270 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 36 uM . . . Lung large cell carcinoma NCI-H460 cell . REF101542 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 36 uM . . . Prostate carcinoma LNCaP cell . REF102325 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 36.04 uM . . . Lung large cell carcinoma NCI-H460 cell . REF102317 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 36.16 uM . . . Prostate carcinoma DU145 cell . REF101307 DRG00061 KLUKLUKKLUKLUK Half Maximal Inhibitory Concentration (IC50) = 36.27±2.7 µM 48 h . . Hepatocellular carcinoma Huh-7 cell "The effect of the peptide conjugate QR-KLU on the proliferation of Huh7 and HUVEC cells was assessed by CCK8 assays. First, we investigated anti-proliferation ability of three peptides QR, KLU and QR-KLU on Huh7 and HUVEC cells with different concentrations. As shown in Fig. Fig.3A,3A, B, cells were treated with QR peptide, KLU peptide, QR-KLU peptide, DOX with different concentration respectively. The inhibition rate increased in a dose-dependent manner in KLU and QR-KLU groups in both cell lines. In HUVEC cells, peptide QR-KLU (IC50 10.70.292µM) showed more potent inhibition effect than KLU (IC50 33.80.98µM), and in Huh7 cells, QR-KLU (IC50 7.30.74µM) also showed more potent anti-tumor effect than KLU (IC50 36.272.7µM). Meanwhile, peptide QR showed negligible toxicity even under 80µM." REF00235 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 36.3 uM . . . Hepatoblastoma Hep-G2 cell . REF101288 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 36.62 uM . . . Hepatoblastoma Hep-G2 cell . REF102428 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 360 nM . . . Chronic myeloid leukemia K562 cell . REF101949 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 360 nM . . . Endocervical adenocarcinoma HeLa cell . REF101715 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 360 nM . . . Hepatocellular carcinoma Huh-7 cell . REF101467 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 360 nM . . . Lung adenocarcinoma A-549 cell . REF100579 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 37 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101241 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 37 nM . . . Acute myeloid leukemia HL-60 cell . REF101196 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 37 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101095 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 37 nM . . . Colon carcinoma HCT 116 cell . REF100582 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 37 nM . . . Colon cancer HT29 cell . REF100296 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 37 nM . . . Invasive breast carcinoma T-47D cell . REF100792 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 37 nM . . . Melanoma M21 cell . REF100659 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 37 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF100611 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 37 nM . . . Normal MT-2 cell . REF100049 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 37 nM . . . Lung adenocarcinoma A-549 cell . REF102436 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 37 uM . . . Invasive breast carcinoma MCF-7 cell . REF102300 DRG00162 Curcumin Half Maximal Effective Concentration (EC50) = 37 uM . . . Normal HEK293 cell . REF102206 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 37.4 ug/mL . . . Ehrlich ascites carcinoma Ehrlich cell . REF101447 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 37.57 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101976 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 37.7 nM . . . Lung large cell carcinoma NCI-H1299 cell . REF100439 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 37.7 uM . . . Colon carcinoma HCT 116 cell . REF101153 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 37.8 uM . . . Normal Vero cell . REF100053 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 37.9 uM . . . Lung large cell carcinoma NCI-H460 cell . REF100822 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Lymphoblastic leukemia L1210 cell . REF102232 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Hepatoblastoma Hep-G2 cell . REF101655 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 370 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101740 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Breast adenocarcinoma SK-BR-3 cell . REF101653 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Cervical epithelial carcinoma KB 3-1 cell . REF101610 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Endocervical adenocarcinoma HeLa cell . REF101518 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Lymphoblastic leukemia L1210 cell . REF101381 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Hepatocellular carcinoma SMMC-7721 cell . REF101071 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Skin squamous cell carcinoma A431 cell . REF100872 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Hepatoblastoma Hep-G2 cell . REF100773 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Invasive breast carcinoma MCF-7 cell . REF102079 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 370 nM . . . Invasive breast carcinoma MCF-7 cell . REF102475 DRG00012 Paclitaxel 90% Lethal Concentration (IC50) = 372 nM . . . Colon carcinoma NCI-H630 cell . REF100505 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 379 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100429 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 38 ng/mL . . . Invasive breast carcinoma MCF-7 cell . REF101251 DRG00012 Paclitaxel 90% Growth Inhibition (GI90) = 38 ng/mL . . . Lung adenocarcinoma A-549 cell . REF101409 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 38 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100789 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 38 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101688 DRG00059 Sunitinib Half Maximal Growth Inhibition (GI50) = 38 nM . . . Gastrointestinal stromal tumor GIST-T1 cell . REF102482 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 38 uM . . . Chronic myeloid leukemia K562 cell . REF102230 DRG00101 Vidarabine Half Maximal Cytotoxicity Concentration (CC50) = 38 uM . . . Normal Vero cell . REF100097 DRG00107 Betulinic acid Half Maximal Cytotoxicity Concentration (CC50) = 38.1 uM . . . Normal Vero cell . REF101568 DRG00407 Combretastatin A4 Half Maximal Cytotoxicity Concentration (CC50) = 38.3 uM . . . Hepatocellular carcinoma Huh-7 cell . REF102469 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 38.34 uM . . . Hepatoblastoma Hep-G2 cell . REF102326 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 38.61 uM . . . Prostate carcinoma PC-3 cell . REF102382 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 380 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100950 DRG00010 Daunorubicin Half Maximal Growth Inhibition (GI50) = 380 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100836 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 380 nM . . . ALK-positive anaplastic large cell lymphoma Karpas-299 cell . REF101775 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 380 nM . . . Renal carcinoma TK-10 cell . REF101480 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 380 nM . . . Normal NIH3T3 cell . REF100969 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 380 nM . . . Normal WI-38 VA13 cell . REF100456 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 380 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF101746 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 380 nM . . . Chronic myeloid leukemia K562 cell . REF101435 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 380 nM . . . Colon cancer HT29 cell . REF100854 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 380 uM . . . Colon adenocarcinoma SW620 cell . REF102272 DRG00003 Fluorouracil Half Maximal Cytotoxicity Concentration (CC50) = 384.4 uM . . . Colon adenocarcinoma Caco-2 cell . REF100100 DRG00012 Paclitaxel Minimum Inhibitory Concentration (MIC) = 39 ng/mL . . . Lung adenocarcinoma A-549 cell . REF101384 DRG00045 Duocarmycin Sa Half Maximal Inhibitory Concentration (IC50) = 39 nM 72 h . . Lung adenocarcinoma A-549 cell "All cell lines demonstrated sensitivity toward the DSA-PABA payload 5 in the nanomolar range. The cleaved peptide 6, and the benzyl protected control peptide 4, had no appreciable effect on cell proliferation (>100 µM), suggesting that any observed cytotoxic activity is due to the DSA warhead. Interestingly, PDC 7, without the cathepsin B cleavable sequence, also had no appreciable effect on cell proliferation (>100 µM), despite possessing the active DSA DNA alkylating moiety. Perhaps this PDC is either not being taken up into cells or not being broken down by proteases and peptidases in the cell. In both cases, the warhead may not be reaching the nucleus, the site of action of the duocarmycins. Cell lines that demonstrated appreciable levels of TFα were sensitive to PDC 3. Interestingly, HCT116, which had relatively high TFα expression and cathepsin B activity, demonstrated the greatest sensitivity to PDC 3, approaching similar potency to the payload 5. Excitingly, A549, H292, and 16HBE14o, which showed no detectable TFα expression, appeared unaffected by PDC 3 up to 100 µM, suggesting that TFα expression is required for the efficacy of PDC 3." REF00117 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 39 uM . . . Colon adenocarcinoma DLD-1 cell . REF100964 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 39.2 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100249 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 39.74 uM . . . Hepatoblastoma Hep-G2 cell . REF102364 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 39.8 uM . . . Colon adenocarcinoma HCT 15 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 39.8 uM . . . Colon adenocarcinoma SW620 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 39.8 uM . . . Colon adenocarcinoma HCC 2998 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 39.8 uM . . . Cutaneous melanoma SK-MEL-5 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 39.8 uM . . . Glioblastoma SNB-75 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 39.8 uM . . . Minimally invasive lung adenocarcinoma NCI-H322M cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 39.8 uM . . . Renal cell carcinoma SN12C cell . REF102249 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 39.81 nM . . . Clear cell renal cell carcinoma Caki-1 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 39.81 nM . . . Invasive breast carcinoma MCF-7 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 39.81 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 39.81 nM . . . Prostate carcinoma PC-3 cell . REF102222 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 39.81072 uM . . . Astrocytoma U-251MG cell . REF100098 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 39.81072 uM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF102222 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 390 nM . . . Lung adenocarcinoma A-549 cell . REF101739 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) = 392 uM . . . Burkitt lymphoma P3HR-1 cell . REF102100 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 392.5 nM . . . Vinblastine-resistant T-cell leukemia CEM-VLB cell . REF102497 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 398 nM . . . Renal adenocarcinoma ACHN cell . REF100587 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 398 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100246 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 398.11 nM . . . Renal carcinoma A498 cell . REF102227 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 398.11 nM . . . Non-small cell lung carcinoma EKVX cell . REF102222 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4 ng/mL . . . Lymphoma P388 cell . REF100421 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4 ng/mL . . . Neuroblastoma N2a cell . REF100416 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 4 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100332 DRG00045 Duocarmycin Sa Half Maximal Inhibitory Concentration (IC50) = 4 nM 72 h . . Breast adenocarcinoma SK-BR-3 cell "All cell lines demonstrated sensitivity toward the DSA-PABA payload 5 in the nanomolar range. The cleaved peptide 6, and the benzyl protected control peptide 4, had no appreciable effect on cell proliferation (>100 µM), suggesting that any observed cytotoxic activity is due to the DSA warhead. Interestingly, PDC 7, without the cathepsin B cleavable sequence, also had no appreciable effect on cell proliferation (>100 µM), despite possessing the active DSA DNA alkylating moiety. Perhaps this PDC is either not being taken up into cells or not being broken down by proteases and peptidases in the cell. In both cases, the warhead may not be reaching the nucleus, the site of action of the duocarmycins. Cell lines that demonstrated appreciable levels of TFα were sensitive to PDC 3. Interestingly, HCT116, which had relatively high TFα expression and cathepsin B activity, demonstrated the greatest sensitivity to PDC 3, approaching similar potency to the payload 5. Excitingly, A549, H292, and 16HBE14o, which showed no detectable TFα expression, appeared unaffected by PDC 3 up to 100 µM, suggesting that TFα expression is required for the efficacy of PDC 3." REF00117 DRG00009 Camptothecin Half Maximal Cytotoxicity Concentration (CC50) = 4 nM . . . Normal MT4 cell . REF102288 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Normal MT4 cell . REF101039 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Lymphoma P388 cell . REF100715 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100353 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100305 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Non-small cell lung carcinoma HOP-62 cell . REF100278 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Colon carcinoma HCT 116 cell . REF101997 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 4 nM . . . Colon adenocarcinoma SW620 cell . REF101860 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Invasive breast carcinoma MCF-7 cell . REF101830 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101756 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF101632 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 4 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101624 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 4 nM . . . Invasive breast carcinoma MCF-7 cell . REF101624 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Prostate carcinoma PC-3 cell . REF101403 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Embryonic hepatoma WRL68 cell . REF101135 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 4 nM . . . Colon adenocarcinoma KM12 cell . REF100987 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 4 nM . . . Glioblastoma SNB-75 cell . REF100987 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 4 nM . . . Lung adenocarcinoma A-549 cell . REF100987 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 4 nM . . . Prostate carcinoma PC-3 cell . REF100987 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Invasive breast carcinoma T-47D cell . REF100763 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100429 DRG00013 Gemcitabine Half Maximal Growth Inhibition (GI50) = 4 nM . . . Breast ductal carcinoma BT-549 cell . REF102202 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Prostate carcinoma DU145 cell . REF102163 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Colon carcinoma HCT 116 cell . REF101852 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Amelanotic melanoma A-375 cell . REF100917 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Prostate carcinoma PC-3 cell . REF100917 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 4 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102055 DRG00296 Zidovudine Half Maximal Effective Dosage (ED50) = 4 nM . . . Normal MT4 cell . REF102020 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Invasive breast carcinoma MCF-7 cell . REF102489 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Lung adenocarcinoma A-549 cell . REF102463 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Endocervical adenocarcinoma HeLa cell . REF102450 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 4 nM . . . Astrocytoma U-251MG cell . REF102357 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Colon carcinoma HCT 116 cell . REF101874 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF101632 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100116 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF101440 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101440 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100672 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4 uM . . . Colon carcinoma HCT 116 cell . REF102260 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101041 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4 uM . . . Gastric adenocarcinoma SNU-1 cell . REF100745 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 4 uM . . . Colon carcinoma HCT 116 cell . REF102411 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4 uM . . . Acute myeloid leukemia HL-60 cell . REF102445 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 4.07 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102467 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 4.07±1.82 µM 48 h . . Ovarian serous cystadenocarcinoma SK-OV-3 cell "HER2 positive SK-BR-3, NCIN87 and SK-OV-3 cells, and HER2 negative MDA-MB-231 and MCF-10A cells were selected to determine the cell activity of the target conjugates. From Table 3, most conjugates showed certain cytotoxicity to three HER2 positive cell lines. Among the three connection sites (S1S3), compounds 1, 4, and 7 with the first connection mode showed better activity. In the three HER2 positive SK-BR-3, NCIN87 and SK-OV-3 cells, conjugate 4 exhibited superior activity (IC50s of 0.53 0.17 µM, 1.58 0.41 µM, 2.50 0.78 µM, respectively), which almost equal to that of CPT (IC50s of 0.38 0.11 µM, 2.07 0.67 µM, 4.07 1.82 µM, respectively). The activity of conjugate 4 on HER2 positive cells was superior to that of conjugate 1 and 7. In MDA-MB-231 and MCF-10A cells, IC50s of conjugate 4 were 18.44 2.09 µM and 17.76 1.35 µM, respectively, which showed great tumor cell selectivity. Based on the above, conjugate 4 with better in vitro antitumor activity was selected for subsequent biological study." REF00288 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4.09 nM . . . Endocervical adenocarcinoma HeLa cell . REF100978 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.1 ng/mL . . . Mouse melanoma B16-F10 cell . REF101918 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.1 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101178 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.1 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100230 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4.1 nM . . . Endocervical adenocarcinoma HeLa cell . REF101176 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.1 uM . . . Normal WI-38 cell . REF102465 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.1 uM . . . Bladder carcinoma T24 cell . REF102050 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 4.1 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101541 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.12 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101989 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 4.12 uM . . . Endocervical adenocarcinoma HeLa cell . REF100967 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.14 uM . . . Chronic myeloid leukemia K562 cell . REF100634 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.15 uM . . . Hepatoblastoma Hep-G2 cell . REF100634 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.16 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100720 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 4.16 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100621 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.16 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100815 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4.165 uM . . . Colon cancer HT29 cell . REF102489 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.17 uM . . . Invasive breast carcinoma MCF-7 cell . REF101847 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.2 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100632 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.2 uM . . . Melanoma B16 cell . REF102313 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 4.2 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100841 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.2 uM . . . Uterine sarcoma MES-SA cell . REF100150 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 4.24 ng/ml . . . Renal carcinoma A498 cell . REF100258 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.24 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101464 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 4.28 ng/ml . . . Colon cancer HT29 cell . REF100235 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 4.3 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100288 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.3 ng/mL . . . Normal WI-38 VA13 cell . REF100537 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.3 nM . . . Normal WI-38 VA13 cell . REF100490 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 4.3 nM . . . Acute monocytic leukemia MV4-11 cell . REF102195 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4.3 nM . . . Melanoma M21 cell . REF100952 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.3 ug/mL . . . Chronic myeloid leukemia K562 cell . REF102052 DRG00221 Acyclovir 50% inhibited minimum concentration (MIC50) = 4.3 ug/mL . . . Normal Vero cell . REF102026 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.3 uM . . . Colon carcinoma HCT 116 cell . REF102505 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.3 uM . . . Lung adenocarcinoma A-549 cell . REF102441 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.3 uM . . . Invasive breast carcinoma T-47D cell . REF101761 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.3 uM . . . Lung carcinoma SW1573 cell . REF101761 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.3 uM . . . Normal HBL-100 cell . REF101761 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.3 uM . . . Hepatoblastoma Hep-G2 cell . REF101687 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.32 uM . . . Invasive breast carcinoma MCF-7 cell . REF102161 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.37 uM . . . Colon carcinoma HCT 116 cell . REF100722 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.4 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101123 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.4 nM . . . Hepatoblastoma Hep-G2 cell . REF101067 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.4 nM . . . Lung adenocarcinoma A-549 cell . REF100911 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 4.4 nM . . . Lymphoblastic leukemia L1210 cell . REF100155 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.4 uM . . . Glioblastoma SF-295 cell . REF100946 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 4.4 uM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF100409 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 4.43 uM . . . Ovarian adenocarcinoma OVCAR-4 cell . REF102305 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 4.45 ng/ml . . . Colon cancer HT29 cell . REF100135 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.45 nM . . . Acute monocytic leukemia U-937 cell . REF100815 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.46 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100720 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 4.46684 uM . . . Ovarian adenocarcinoma OVCAR-4 cell . REF100123 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.5 ng/mL . . . Colon adenocarcinoma COLO 320DM cell . REF100483 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.5 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100559 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 4.5 nM . . . Lung squamous cell carcinoma NCI-H520 cell . REF101549 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 4.5 nM . . . Normal MT4 cell . REF102011 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4.5 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101624 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.5 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100714 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 4.5 ug/mL . . . Clear cell renal cell carcinoma Caki-1 cell . REF100157 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 4.5 ug/mL . . . Gastric epithelial carcinoma MKN-28 cell . REF100009 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.5 uM . . . Colon adenocarcinoma DLD-1 cell . REF102143 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.5 uM . . . Hepatoblastoma Hep-G2 cell . REF101897 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.5 uM . . . Invasive breast carcinoma MCF-7 cell . REF101007 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.52 uM . . . Colon carcinoma HCT 116 cell . REF102304 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 4.55 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101729 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 4.5521 mM . . . Leukemia C8166 cell . REF102136 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 4.56 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100263 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.57 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100840 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.57 uM . . . Prostate carcinoma PC-3 cell . REF101577 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.59 uM . . . Lung adenocarcinoma A549/CDDP cell . REF101612 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 4.6 ng/mL . . . Colon cancer HT29 cell . REF100338 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.6 nM . . . Endocervical adenocarcinoma HeLa cell . REF101593 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.6 nM . . . Hepatoblastoma Hep-G2 cell . REF101237 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.6 nM . . . Amelanotic melanoma A-375 cell . REF100911 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.6 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100400 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 4.6 nM . . . Lymphoblastic leukemia L1210 cell . REF100159 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.6 uM . . . Invasive breast carcinoma MCF-7 cell . REF101881 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.6 uM . . . Prostate carcinoma LNCaP cell . REF100530 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 4.63 ng/mL . . . Lung squamous cell carcinoma QG-56 cell . REF100199 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.69 uM . . . Colon carcinoma HCT 116 cell . REF101735 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 4.69 uM . . . Renal carcinoma RXF 393 cell . REF101566 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.7 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF100947 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 4.7 nM . . . Endocervical adenocarcinoma HeLa cell . REF102511 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.7 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101447 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.7 uM . . . Invasive breast carcinoma MCF-7 cell . REF102274 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 4.707 uM . . . Hepatocellular carcinoma Huh-7 cell . REF102400 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.73 nM . . . Adrenal gland neuroblastoma GOTO cell . REF100720 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.73 uM . . . Melanoma SK-MEL3 cell . REF102527 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.73 uM . . . Melanoma SK-MEL-24 cell . REF101818 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 4.74 ng/mL . . . Lymphoma P388 cell . REF100199 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.77 uM . . . Invasive breast carcinoma MCF-7 cell . REF101065 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.78 uM . . . Melanoma SK-MEL-2 cell . REF100899 DRG00059 Sunitinib Half Maximal Growth Inhibition (GI50) = 4.789 uM . . . Normal BaF3 cell . REF102438 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 4.79 uM . . . Hepatoblastoma Hep-G2 cell . REF101707 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.8 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101031 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.8 nM . . . Ovarian adenocarcinoma A2780-1A9 cell . REF100542 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.8 uM . . . Hepatoblastoma Hep-G2 cell . REF102281 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.8 uM . . . Invasive breast carcinoma MCF-7 cell . REF102137 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.8 uM . . . Prostate carcinoma DU145 cell . REF100896 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.8 uM . . . Endocervical adenocarcinoma HeLa cell . REF101470 DRG00221 Acyclovir 90% Lethal Concentration (IC50) = 4.8 uM . . . Normal MRC5 cell . REF100018 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 4.83 ng/ml . . . Colon cancer HT29 cell . REF100136 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.84 uM . . . Prostate carcinoma DU145 cell . REF100764 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.875 uM . . . Normal NIH3T3 cell . REF101691 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.875 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100978 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.89 nM . . . Prostate carcinoma DU145 cell . REF100345 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.89 uM . . . Hepatoblastoma Hep-G2 cell . REF101931 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.9 ng/mL . . . Renal carcinoma A498 cell . REF100266 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.9 nM . . . Invasive breast carcinoma MCF-7 cell . REF101944 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.9 nM . . . Amelanotic melanoma A-375 cell . REF100999 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.9 nM . . . Lung adenocarcinoma A-549 cell . REF100505 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.9 uM . . . Lymphoblastic leukemia L1210 cell . REF102232 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.9 uM . . . Endocervical adenocarcinoma HeLa cell . REF101232 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 4.9 uM . . . Prostate carcinoma LNCaP cell . REF100084 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 4.9 uM . . . Prostate carcinoma PC-3 cell . REF101333 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 4.9 uM . . . Hepatoblastoma Hep-G2 cell . REF102467 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 4.91 uM . . . Lung adenocarcinoma A-549 cell . REF101831 DRG00224 Pemetrexed Half Maximal Inhibitory Concentration (IC50) = 4.94 nM . . . Normal R2 cell . REF100994 DRG00030 Gambogic acid Half Maximal Inhibitory Concentration (IC50) = 4.95 µM 24 h . . Bladder cancer Bladder cancer cell "The 50% inhibitory concentration (IC50) of GA-TAT at 24 h was 1.24 µM, which was lower than that of the GA treatment (4.95 µM)." REF00037 DRG00107 Betulinic acid Half Maximal Effective Dosage (ED50) = 4.98 ug/mL . . . Mouse melanoma B16-F10 cell . REF102108 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 4.98 uM . . . Normal CCD-841CoN cell . REF101890 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 4.99 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100258 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > 40 µM 72 h . . Breast adenocarcinoma MDA-MB-231 cell "To deliver the functional molecule into the cells, we attached an anticancer drug, methotrexate (MTX), to the N-terminus of STRAPs. The peptides were tested for their capability to deliver the active drug molecule in breast and cervical cancer cells. MDA-MB-231 and HeLa cells were treated with varying concentrations of MTX and STRAP-MTX conjugates for 72 h. Cell viability was assessed using the MTT assay. The cytotoxicity of MTX increased when delivered as peptideMTX conjugates to the cells. This resulted in an overall reduction in the inhibitory concentration cytotoxic to 50% of cells (IC50) for MTX. The MTX resistance for MDA-MB-231 cells is well-established. The IC50 for MTX in MDA-MB-231 cells was minimum when delivered as a STRAP-4MTX conjugate. Similar lowering of IC50 values in HeLa cells was observed. We also treated HEK-293 cells with MTXSTRAP conjugates. The peptidedrug conjugates showed no significant toxicity to the HEK-293 cells under the tested conditions, thereby confirming the earlier reported observation of higher uptake rates in cancerous cells." REF00225 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 40 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101947 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 ng/mL . . . Glioblastoma SF-295 cell . REF100826 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 ng/mL . . . Lung small cell carcinoma NCI-H187 cell . REF100766 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 ng/mL . . . Ileocecal adenocarcinoma HCT-8 cell . REF100595 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 40 ng/mL . . . Melanoma SK-MEL-2 cell . REF100495 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 40 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100444 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 40 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100342 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 40 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100314 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 40 ng/ml . . . Colon cancer HT29 cell . REF100233 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 40 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100802 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Lung adenocarcinoma A-549 cell . REF100760 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Lymphoblastic leukemia L1210 cell . REF100372 DRG00010 Daunorubicin Half Maximal Infective Dose (ID50) = 40 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100026 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Lymphoblastic leukemia L1210 cell . REF101951 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 40 nM . . . Invasive breast carcinoma MCF-7 cell . REF101917 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Melanoma B16-F10-luc2 cell . REF101904 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Normal MRC5 cell . REF101846 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Acute myeloid leukemia HL-60 cell . REF101822 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Lung adenocarcinoma A-549 cell . REF101581 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF101472 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Bone metastasis of prostate carcinoma PC-3M cell . REF101334 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 40 nM . . . Astrocytoma SNB-19 cell . REF101165 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101110 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101101 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Astrocytoma SF268 cell . REF100627 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Endocervical adenocarcinoma HeLa cell . REF100601 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Invasive breast carcinoma MCF-7 cell . REF100601 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 40 nM . . . Invasive breast carcinoma ZR-75-1 cell . REF100574 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 40 nM . . . Prostate carcinoma LNCaP cell . REF100574 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Non-small cell lung carcinoma LXFL 529 cell . REF100373 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Laryngeal carcinoma HEp-2 cell . REF100371 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Renal adenocarcinoma ACHN cell . REF100370 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Uterine sarcoma MES-SA cell . REF100150 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Prostate carcinoma PC-3 cell . REF101294 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 40 nM . . . Astrocytoma SNB-19 cell . REF101147 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Lymphoma P388 cell . REF100963 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Normal WI-38 cell . REF100509 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Invasive breast carcinoma MCF-7 cell . REF100398 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Prostate carcinoma PC-3 cell . REF102193 DRG00019 Methotrexate Half Maximal Growth Inhibition (GI50) = 40 nM . . . Colon cancer HT29 cell . REF101161 DRG00019 Methotrexate Half Maximal Lethal Concentration (IC50) = 40 nM . . . Invasive breast carcinoma MCF-7 cell . REF100902 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Bladder carcinoma RT-4 cell . REF100710 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . EBV-related Burkitt lymphoma Raji cell . REF100647 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Renal adenocarcinoma ACHN cell . REF100270 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . Thyroid gland medullary carcinoma TT cell . REF102323 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 40 nM . . . Normal MT4 cell . REF102037 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 40 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100071 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 40 pM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101396 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 40 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF102285 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 40 ug/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102028 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 40 uM . . . Normal HEK293 cell . REF101436 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 40 uM . . . Prostate carcinoma PC-3 cell . REF100115 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 40.791 uM . . . Pancreatic ductal adenocarcinoma Capan-2 cell . REF102455 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Prostate carcinoma PC-3 cell . REF101579 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Prostate carcinoma DU145 cell . REF101329 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Chronic myeloid leukemia K562 cell . REF101190 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Endocervical adenocarcinoma HeLa cell . REF101113 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100976 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Invasive breast carcinoma MCF-7 cell . REF101063 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 400 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102139 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Colon carcinoma HCT 116 cell . REF101928 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101815 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Lung adenocarcinoma A-549 cell . REF101721 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Lymphoblastic leukemia L1210 cell . REF101681 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Gastric cancer MGC-803 cell . REF101652 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Invasive breast carcinoma MCF-7 cell . REF101594 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 400 nM . . . Lung adenocarcinoma NCI-H23 cell . REF101321 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Normal COLO205 cell . REF100949 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 400 nM . . . Colon cancer HT29 cell . REF100789 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 400 nM . . . Colon cancer HT29 cell . REF100566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Hepatoblastoma Hep-G2 cell . REF100437 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Normal Farage cell . REF100291 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Renal adenocarcinoma ACHN cell . REF100291 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 400 nM . . . Cutaneous melanoma SK-MEL-28 cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 400 nM . . . Melanoma SK-MEL-2 cell . REF101860 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100744 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Esophageal adenocarcinoma OE19 cell . REF100598 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100270 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 400 nM . . . Prostate carcinoma PC-3 cell . REF101012 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 400 uM . . . Lymphoblastic leukemia L1210 cell . REF101605 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 400 uM . . . Cervical epithelial carcinoma KB 3-1 cell . REF100634 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 404.0±9.4 nM 24 h . . Ovarian serous adenocarcinoma OVCAR-3 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 41 ng/mL . . . Ovarian adenocarcinoma 1A9/ptx-10 cell . REF100393 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 41 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100636 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 41 nM . . . Invasive breast carcinoma MCF-7 cell . REF102491 DRG00221 Acyclovir Half Maximal Infective Dose (ID50) = 41 ug/mL . . . Lymphoblastic leukemia L1210 cell . REF100013 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 41.221 uM . . . Pancreatic ductal adenocarcinoma CFPAC-1 cell . REF102455 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 41.3±1.5 nM 24 h . . Glioblastoma U87MG-PR cell "Furthermore, it was also observed that PDC shows time-dependent cytotoxicity against U87MG cells, as at 12 h drug treatment. PDC shows a slightly lower inhibitory effect on cell survival (EC50 = 25.82 0.31 nM) than PTX alone (EC50 = 12.25 0.13 nM), and CPPSA alone shows higher EC50 = 54.37 0.24 in U87MG cells. Besides this, it was previously observed that CPP-treated healthy VERO cells showed 88.05 0.86% viable cells even using 10 µM concentration, indicating the specificity of CPP for glioblastoma cells. However, at 24 h incubation period, our PDC shows a significantly enhanced cell survival inhibitory effect with EC50 = 8.32 0.09 nM, suggesting the delayed effect of PDC because of the time required for the intracellular pH to cause maximal cleavage of PTX from the PDC. Moreover, it also shows that CPPSA has a lower cytotoxicity effect on glioblastoma cells compared with PTX alone and PDC, indicating its specificity as a carrier and selectivity for integrin receptors overexpressed on the cell surface. Additionally, we have also studied the potential of our novel-designed PDC to internalize into PTX-resistant glioblastoma (U87MG-PR) cells to show cytotoxic activity upon intracellular cleavage of PTX from CPP. The data presented in Figure 3b reveal approximately 15% viability increases in U87MG-PR cells compared with parent U87MG cells. It can be seen in the inset in Figure 3b that PTX alone (EC50 = 41.3 1.5 nM) showed significantly 2-fold reduced cytotoxic activity in U87MG-PR cells in comparison with our novel-designed PDC having EC50 = 20.55 1.02 nM. It was also observed in Figure 3b that at lower concentrations (010 nM) the viable cell count was 75%; however, it significantly decreased to 20% viability with an increase in concentration (40 nM) of the test samples, highlighting the dose-dependent cytotoxicity behavior of PDC in a 24 h incubation period." REF00266 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 41.5 uM . . . Colon carcinoma HCT 116 cell . REF102295 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 41.6 ng/ml . . . Colon cancer HT29 cell . REF100242 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 41.73 uM . . . Gastric adenocarcinoma MKN45 cell . REF102286 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 410 nM 24 h . . Breast adenocarcinoma SK-BR-3 cell "Tumor-targeting peptidedrug conjugates (PDCs) have become a focus of research in recent years. However, due to the instability of peptides and their short in vivo effective half-life, they have limited clinical application. Herein, we propose a new DOX PDC based on a homodimer HER-2-targeting peptide and acid-sensitive hydrazone bond, which could enhance the anti-tumor effect of DOX and reduce systemic toxicities. The PDC could accurately deliver DOX into HER2-positive SKBR-3 cells, with it showing 2.9 times higher cellular uptake than free DOX and enhanced cytotoxicity with respect to IC50of 140 nM (vs. 410 nM for free DOX). In vitro assays showed that the PDC had high cellular internalization efficiency and cytotoxicity. In vivo anti-tumor experiments indicated that the PDC could significantly inhibit the growth of HER2-positive breast cancer xenografts in mice and reduce the side effects of DOX. In summary, we constructed a novel PDC molecule targeting HER2-positive tumors, which may overcome some deficiencies of DOX in breast cancer therapy." REF00254 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 410 nM . . . Non-small cell lung carcinoma EKVX cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 410 nM . . . Lung adenocarcinoma A-549 cell . REF101134 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 410 nM . . . Renal adenocarcinoma ACHN cell . REF100746 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 410 nM . . . Endocervical adenocarcinoma HeLa cell . REF100692 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 410 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101746 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 410 nM . . . Chronic myeloid leukemia K562 cell . REF101120 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 410 nM . . . Colon carcinoma HCT 116 cell . REF102440 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 410 nM . . . Invasive breast carcinoma MCF-7 cell . REF102276 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 411 nM . . . Lung adenocarcinoma A-549 cell . REF101186 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 419 uM . . . Chronic myeloid leukemia K562 cell . REF100460 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 419.8 nM . . . Gastric tubular adenocarcinoma NCI-N87 cell . REF100911 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 42 ng/mL . . . Lung small cell carcinoma NCI-H187 cell . REF100743 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 42 nM . . . Colon adenocarcinoma KM12 cell . REF100246 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 42 nM . . . Malignant neoplasms of the mouse mammary gland FM3A cell . REF102404 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 42 nM . . . Invasive breast carcinoma MCF-7 cell . REF102349 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 42.52 uM . . . Invasive breast carcinoma MCF-7 cell . REF100972 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 42.78 uM . . . Invasive breast carcinoma MCF-7 cell . REF102371 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 42.8 nM . . . Invasive breast carcinoma MCF-7 cell . REF100731 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 42.8 uM . . . Invasive breast carcinoma MCF-7 cell . REF100690 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 420 nM . . . Endocervical adenocarcinoma HeLa cell . REF101240 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 420 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101461 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 420 nM . . . Invasive breast carcinoma MCF-7 cell . REF101035 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 420 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101035 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 420 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF101015 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 420 nM . . . Hepatoblastoma Hep-G2 cell . REF100778 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 420 nM . . . Laryngeal carcinoma HEp-2 cell . REF100630 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 420 nM . . . Lung adenocarcinoma A-549 cell . REF102192 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 424 nM . . . Chronic myeloid leukemia K562 cell . REF101373 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 429 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100806 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 43 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100208 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 43 nM . . . Invasive breast carcinoma MCF-7 cell . REF100492 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 43 nM . . . Lung adenocarcinoma NCI-H23 cell . REF100270 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) = 43 ug/mL . . . Normal Vero cell . REF100046 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 43 uM . . . Gliosarcoma SF539 cell . REF102228 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 43.39 uM . . . Hepatoma Bel-7402 cell . REF102133 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 43.48 uM . . . Plasma cell myeloma U-266 cell . REF102402 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 430 nM . . . Normal IMR-90 cell . REF101091 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 430 nM . . . Lung adenocarcinoma A-549 cell . REF101620 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 430 nM . . . Chronic myeloid leukemia K562 cell . REF101060 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 430 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100908 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 430 nM . . . Hepatocellular carcinoma Huh-7 cell . REF102356 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 438 nM . . . Colon adenocarcinoma HCT 15 cell . REF100439 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 44 nM . . . Breast ductal carcinoma HCC70 cell . REF101754 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 44 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100922 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 44 uM . . . Mouse reticulum cell sarcoma J774 cell . REF102149 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 44.06 uM . . . Colon carcinoma HCT 116 cell . REF102402 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 44.89 uM . . . Colon adenocarcinoma LoVo cell . REF100628 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 44.9 uM . . . Breast adenocarcinoma MDA-MB-468 cell . REF102401 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 440 nM . . . Endocervical adenocarcinoma HeLa cell . REF100755 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) = 440 uM . . . Erythroleukemia HEL cell . REF102366 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 45 nM . . . Colon carcinoma Col2 cell . REF100564 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 45 nM . . . Prostate carcinoma DU145 cell . REF100270 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 45 nM . . . Sezary syndrome H9 cell . REF102088 DRG00406 Monastrol Half Maximal Inhibitory Concentration (IC50) = 45 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF102242 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 45 uM . . . Pancreatic adenocarcinoma SW1990 cell . REF101042 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 45.1 uM . . . Nasopharyngeal carcinoma CNE cell . REF102326 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 45.14 uM . . . Lung large cell carcinoma NCI-H460 cell . REF102326 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 45.3 nM . . . Prostate carcinoma LNCaP cell . REF100525 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 45.44 uM . . . Lung large cell carcinoma NCI-H460 cell . REF102430 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 45.6±33.5 nM 24 h . . Oral cavity squamous cell carcinoma PE/CA-PJ41 "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 450 nM . . . Hepatocellular carcinoma SMMC-7721 cell . REF101693 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 450 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF101626 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 450 nM . . . Glioblastoma SF-295 cell . REF101547 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 450 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101411 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 450 nM . . . Endocervical adenocarcinoma HeLa cell . REF101351 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 450 nM . . . Cervical squamous cell carcinoma SiHa cell . REF100954 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 450 nM . . . Normal CH1 cell . REF100290 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 450 nM . . . Colon cancer HT29 cell . REF101128 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 450 nM . . . Non-small cell lung carcinoma NCI-H522 cell . REF100270 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 451 nM . . . Endocervical adenocarcinoma HeLa cell . REF101152 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 456 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101928 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 459 nM . . . Lung adenocarcinoma A-549 cell . REF101167 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 46 ng/mL . . . Lymphoma P388 cell . REF101918 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 46 nM . . . Acute myeloid leukemia HL-60 cell . REF101792 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 46 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100772 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 46 nM . . . Endocervical adenocarcinoma HeLa cell . REF101676 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 46 nM . . . Breast carcinoma MX1 cell . REF100744 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 46 nM . . . Colon carcinoma Col2 cell . REF100419 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 46 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100071 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 46 nM . . . Chronic myeloid leukemia K562 cell . REF102192 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 46 uM . . . Cervical carcinoma L02 cell . REF101542 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 46 uM . . . Colon cancer HT29 cell . REF100822 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 46 uM . . . Invasive breast carcinoma MCF-7 cell . REF100822 DRG00162 Curcumin 70% Inhibitory Concentration (IC70) = 46.2 uM . . . Breast carcinoma MCF7R cell . REF102157 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 46.55 uM . . . Amelanotic melanoma A-375 cell . REF102275 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 46.69 uM . . . Chronic myeloid leukemia K562 cell . REF101057 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 46.8 nM . . . Hepatoblastoma Hep-G2 cell . REF100639 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 460 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100753 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 460 nM . . . Chronic myeloid leukemia K562 cell . REF101776 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 460 nM . . . Normal HEK293 cell . REF101666 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 464.433 uM . . . Endocervical adenocarcinoma HeLa cell . REF102183 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 467 nM . . . Invasive breast carcinoma MCF-7 cell . REF102521 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 467.74 nM . . . Cutaneous melanoma SK-MEL-5 cell . REF102227 DRG00012 Paclitaxel 90% Lethal Concentration (IC50) = 47 ng/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100483 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 47 nM . . . Pancreatic ductal adenocarcinoma CFPAC-1 cell . REF100865 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 47 nM . . . Squamous carcinoma SCC-25 cell . REF102109 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 47 nM . . . Acute myeloid leukemia HL-60 cell . REF101726 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 47.3 uM . . . Invasive breast carcinoma of no special type BT-20 cell . REF101093 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 47.39 uM . . . Gastric cancer MGC-803 cell . REF102338 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 47.82 ug/mL . . . Colon cancer HT29 cell . REF101697 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 47.97 uM . . . Non-small cell lung carcinoma EKVX cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 470 nM . . . Endocervical adenocarcinoma HeLa cell . REF101350 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 470 nM . . . Endocervical adenocarcinoma HeLa cell . REF100500 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 477 nM . . . Lung adenocarcinoma A-549 cell . REF101003 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 48 uM . . . Colon adenocarcinoma HCT 15 cell . REF102228 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 48.2 uM . . . Invasive breast carcinoma MCF-7 cell . REF101345 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 48.68 uM . . . Astrocytoma U-251MG cell . REF102371 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 48.7 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100197 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 48.7 uM . . . Normal HEK293 cell . REF102331 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 480 nM . . . Prostate carcinoma PC-3 cell . REF100926 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 480 nM . . . Glioblastoma SF-295 cell . REF100727 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 480 nM . . . Melanoma SK-MEL-24 cell . REF101818 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 484.3 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100499 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 49 nM . . . Invasive breast carcinoma MCF-7 cell . REF100713 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 49 nM . . . Acute myeloid leukemia HL-60 cell . REF101074 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 49.1 uM . . . Prostate carcinoma PC-3 cell . REF102451 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 49.4 ng/mL . . . Colon cancer HT29 cell . REF100220 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 49.8 ng/ml . . . Colon cancer HT29 cell . REF100236 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 49.8 nM . . . Prostate carcinoma PC-3 cell . REF100367 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 49.8 uM . . . Invasive breast carcinoma MCF-7 cell . REF101033 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 49.8±22.9 nM 24 h . . Melanoma WM983B cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 490 nM . . . Glioblastoma SF-295 cell . REF102514 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 490 nM . . . Lymphoblastic leukemia L1210 cell . REF102271 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 490 nM . . . Lymphoma P388 cell . REF100065 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 490 nM . . . Invasive breast carcinoma T-47D cell . REF101613 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 490 nM . . . Cutaneous melanoma SK-MEL-28 cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 490 nM . . . Renal carcinoma UO-31 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 490 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101517 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 490 nM . . . Cutaneous melanoma SK-MEL-5 cell . REF101480 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 490 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100336 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5 mM . . . Colon carcinoma HCT 116 cell . REF101058 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 5 ng/mL . . . Lymphoma P388 cell . REF101921 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 5 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100401 DRG00009 Camptothecin Half Maximal Cytotoxicity Concentration (CC50) = 5 nM . . . Hereditary spherocytosis WIL2-NS cell . REF102257 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . T acute lymphoblastic leukemia RPMI-8402 cell . REF100387 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Colon adenocarcinoma HCT 15 cell . REF101090 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 5 nM . . . Lung adenocarcinoma NCI-H23 cell . REF100967 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Breast adenocarcinoma MDA-MB-468 cell . REF100305 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100230 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101861 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5 nM . . . Colon cancer HT29 cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5 nM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF101860 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Endocervical adenocarcinoma HeLa cell . REF101731 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5 nM . . . Gliosarcoma SF539 cell . REF101624 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5 nM . . . Melanoma LOX IMVI cell . REF101624 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101624 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Breast adenocarcinoma MDA-MB-468 cell . REF101333 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5 nM . . . Invasive breast carcinoma MCF-7 cell . REF101218 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Acute myeloid leukemia HL-60 cell . REF100633 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Prostate carcinoma DU145 cell . REF100633 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Pancreatic carcinoma PT-45 cell . REF100598 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Normal WI-38 VA13 cell . REF100562 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100505 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100502 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Uterine sarcoma MES-SA cell . REF100502 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Lung adenocarcinoma A-549 cell . REF100834 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Lymphoblastic leukemia L1210 cell . REF100163 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Prostate carcinoma DU145 cell . REF101886 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 5 nM . . . Normal MT4 cell . REF100057 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Normal MT4 cell . REF100035 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Invasive breast carcinoma MCF-7 cell . REF102299 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 5 nM . . . Melanoma UACC-62 cell . REF102290 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101315 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 5 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF101129 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5 ug . . . Invasive breast carcinoma MCF-7 cell . REF101487 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 5 ug/mL . . . Erythroleukemia HEL cell . REF100043 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 5 ug/mL . . . Colon cancer HT29 cell . REF100095 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5 uM . . . Hepatoblastoma Hep-G2 cell . REF102368 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5 uM . . . Normal CHO cell . REF100036 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5 uM . . . Invasive breast carcinoma MCF-7 cell . REF101785 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5 uM . . . Hepatoblastoma Hep-G2 cell . REF101538 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5 uM . . . Hepatoma Bel-7402 cell . REF100876 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5 uM . . . Normal Vero cell . REF100340 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 uM . . . Normal WI-38 VA13 cell . REF100575 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5 uM . . . Uterine sarcoma MES-SA/Dx5 cell . REF100502 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 5.01 uM . . . Chronic myeloid leukemia K562 cell . REF100902 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 5.01187 uM . . . Plasma cell myeloma RPMI-8226 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 5.01187 uM . . . Renal carcinoma UO-31 cell . REF100098 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 5.01187 uM . . . Chronic myeloid leukemia K562 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 5.01187 uM . . . Lung adenocarcinoma A-549 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 5.01187 uM . . . Normal COLO205 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 5.01187 uM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 5.01187 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100756 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 5.01187 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102222 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5.012 nM . . . Acute myeloid leukemia HL-60 cell . REF100274 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5.012 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF100274 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5.012 nM . . . Melanoma SK-MEL-2 cell . REF100274 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 5.012 uM . . . Plasma cell myeloma RPMI-8226 cell . REF100987 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 5.05 uM . . . Lung adenocarcinoma A-549 cell . REF102467 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.1 nM . . . Neuroblastoma IMR-32 cell . REF101488 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 5.1 nM . . . Colon cancer HT29 cell . REF102509 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 5.1 uM . . . Thymoma EL4 cell . REF101320 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.12 uM . . . Normal Vero cell . REF100845 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.15 nM . . . Buccal mucosa squamous cell carcinoma NB-1 cell . REF100815 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 5.15 uM . . . Lung large cell carcinoma NCI-H460 cell . REF101905 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.17 uM . . . Endocervical adenocarcinoma HeLa cell . REF101672 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.18 uM . . . Lung large cell carcinoma NCI-H460 cell . REF101446 DRG00008 Dexamethasone Half Maximal Inhibitory Concentration (IC50) = 5.2 uM . . . Mouse reticulum cell sarcoma J774 cell . REF101813 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.2 uM . . . Endocervical adenocarcinoma HeLa cell . REF101341 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 5.21±0.31 µM 48 h . . Colon carcinoma HCT-116/CPT cell "MTT assay was preformed to measure the in vitro cytotoxicities of the compounds against cancer cells (HCT-116, SGC-7901, MCF-7, HCT-116/CPT, SGC-7901/CPT and MCF-7/C4) and benign cells (NCM460, GES-1 and LO2). As present in Table 1, all the peptides (Kb-C01, 0207) exhibited certain selective anticancer activities, which are comparable to their parent counterpart KM8-Aib. The target PDCs (Kb-CC01, 0207) were further obtained by coupling the peptides with CPT, displaying markedly improved antiproliferative activities and selectivities against cancer cell lines over CPT. Studies have revealed that cancer cell membranes are negatively charged due to the presence of substantial amounts of acid phospholipids. Therefore, positively charged CAPs are capable of binding to cancer cell surface through electrostatic interactions, making them specific to cancer cells. In this project, since the PDCs were composed of CAP KM8-Aib and CPT, they potentially inherited the antineoplastic activities of KM8-Aib against cancer cells, as well as low toxicities to non-malignant cells." REF00278 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5.23 nM . . . Prostate carcinoma DU145 cell . REF100924 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.23 uM . . . Colon carcinoma HCT 116 cell . REF101794 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.23 uM . . . Prostate carcinoma LNCaP cell . REF101023 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.23 uM . . . Hepatoblastoma Hep-G2 cell . REF100874 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.3 ng/mL . . . Colon cancer HT29 cell . REF100504 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.3 nM . . . Endocervical adenocarcinoma HeLa cell . REF101230 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.3 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100400 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.3 uM . . . Endocervical adenocarcinoma HeLa cell . REF101042 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.3 uM . . . Invasive breast carcinoma MCF-7 cell . REF100552 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.3 uM . . . Endocervical adenocarcinoma HeLa cell . REF101448 DRG00012 Paclitaxel Minimum Inhibitory Concentration (MIC) = 5.32 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF101384 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 5.4 nM . . . Fibroblast sarcoma CCRF S-180 cell . REF100175 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.4 ug/mL . . . Normal Vero cell . REF101372 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.4 uM . . . Lung small cell carcinoma N592 cell . REF100212 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 5.4014 mM . . . Leukemia C8166 cell . REF102245 DRG00314 9-Aminoacridine Half Maximal Inhibitory Concentration (IC50) = 5.43 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF102474 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5.46 nM . . . Lung adenocarcinoma A-549 cell . REF101036 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.46 uM . . . Invasive breast carcinoma MCF-7 cell . REF101021 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 5.47 uM . . . Colon carcinoma HCT 116 cell . REF101537 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 5.48 mM . . . Colon adenocarcinoma LoVo cell . REF100612 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.49 mM . . . Invasive breast carcinoma MCF-7 cell . REF101208 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.5 nM . . . Invasive breast carcinoma MCF-7 cell . REF100358 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 5.5 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100974 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.5 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100970 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 5.5 ug/mL . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100510 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.5 uM . . . Normal hTERT-BJ cell . REF101761 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 5.5 uM . . . Normal HBL-100 cell . REF100753 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 5.5 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101806 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 5.5 uM . . . Lung adenocarcinoma A-549 cell . REF101651 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.5 uM . . . Invasive breast carcinoma MCF-7 cell . REF101797 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 5.5 uM . . . Colon cancer HT29 cell . REF100140 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 5.51 nM . . . Melanoma UACC-62 cell . REF102316 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.51 uM . . . Invasive breast carcinoma MCF-7 cell . REF101850 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.51 uM . . . Amelanotic melanoma A-375 cell . REF101024 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 5.52 uM . . . Lung carcinoma A-427 cell . REF100710 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.54 uM . . . Gastric carcinoma SGC-7901 cell . REF102478 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5.568 nM . . . Prostate carcinoma DU145 cell . REF101197 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.57 uM . . . Endocervical adenocarcinoma HeLa cell . REF101865 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5.58 nM . . . Lung adenocarcinoma A-549 cell . REF100913 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 5.6 ng/ml . . . Prostate carcinoma PC-3 cell . REF100295 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 5.6 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF100383 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.6 nM . . . Endocervical adenocarcinoma HeLa cell . REF100591 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 5.6 nM . . . Endocervical adenocarcinoma HeLa cell . REF101315 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 5.6 nM . . . Invasive breast carcinoma MCF-7 cell . REF100952 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.6 uM . . . Lung adenocarcinoma A-549 cell . REF102238 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.6 uM . . . Lung large cell carcinoma NCI-H460 cell . REF101080 DRG00407 Combretastatin A4 Half Maximal Effective Dosage (ED50) = 5.6 uM . . . Invasive breast carcinoma MCF-7 cell . REF100140 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 5.60171 mM . . . Leukemia C8166 cell . REF102243 DRG00081 Cytarabine Half Maximal Effective Concentration (EC50) = 5.614 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100762 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.63 uM . . . Chronic myeloid leukemia K562 cell . REF100722 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.64 uM . . . Lung adenocarcinoma A-549 cell . REF101029 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.7 nM . . . Lung adenocarcinoma A-549 cell . REF101899 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 5.7 nM . . . Endocervical adenocarcinoma HeLa cell . REF101624 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.7 uM . . . Invasive breast carcinoma MCF-7 cell . REF101558 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.7 uM . . . Normal WI-38 cell . REF101558 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.7 uM . . . Endocervical adenocarcinoma HeLa cell . REF101900 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 5.7 uM . . . Invasive breast carcinoma MCF-7 cell . REF101541 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.7 uM . . . Hepatoblastoma Hep-G2 cell . REF101422 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.71 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101662 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.73 uM . . . Normal WI-38 cell . REF101525 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 5.8 nM . . . Squamous carcinoma SCC-7 cell . REF100204 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.8 uM . . . Lymphoma P388 cell . REF102384 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.8 uM . . . Endocervical adenocarcinoma HeLa cell . REF102340 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.8 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100876 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.8 uM . . . Chronic myeloid leukemia K562 cell . REF101724 DRG00012 Paclitaxel 90% Growth Inhibition (GI90) = 5.81 ug/mL . . . Acute monocytic leukemia THP-1 cell . REF101437 DRG00012 Paclitaxel 90% Growth Inhibition (GI90) = 5.814 ug/mL . . . Acute monocytic leukemia THP-1 cell . REF101352 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.82 uM . . . Lung adenocarcinoma A-549 cell . REF101595 DRG00059 Sunitinib Half Maximal Growth Inhibition (GI50) = 5.88 uM . . . Gastrointestinal stromal tumor GIST-T1 cell . REF102396 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.898 uM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100729 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.9 nM . . . Normal WI-38 VA13 cell . REF100497 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.9 nM . . . Histiocytic lymphoma U-937/GTB cell . REF100494 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 5.9 nM . . . Colon cancer HT29 cell . REF100937 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 5.9 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101674 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5.9 uM . . . Normal Farage cell . REF100941 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 5.91 uM . . . Lung adenocarcinoma A-549 cell . REF100755 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 5.93 uM . . . Lung adenocarcinoma A-549 cell . REF101556 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 5.943 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF101622 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.96 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101258 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 5.98 nM . . . Renal cell carcinoma SN12C cell . REF102316 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 5.98 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101623 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 5.99 uM . . . Lung adenocarcinoma A-549 cell . REF102434 DRG00023 Tesaglitazar Leptin level = 50 ng/mL Every day 2.5 μM db/db mice model. . . "Whereas in the vehicle/untreated mice, the HbA1C values increased by approximately 2%, a graduated reduced increase was seen for [F7, P34]-NPY (2), peptide conjugate (3), and tesa (Figure 8A). Body temperature, which decreased to 35 C in the vehicle/untreated db/db controls, was normalized to 36 C in all of the treated mice including the mice treated with [F7, P34]-NPY (2) (Figure 8B). Treatment with tesa and tesa-NPY (3) led to normalization of the plasma concentration of ketone bodies and adiponectin, whereas [F7, P34]-NPY (2) and vehicle/untreated showed no effect (Figure 8C/E). Treatment had no major influence on the insulin and Mcp-1 levels (Figure 8D/G). The serum leptin concentration was reduced in the mice treated with tesa, whereas no reduction was detectable in all of the other treated mice (Figure 8F)." REF00088 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100960 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100469 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 50 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100466 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 ng/mL . . . Lung large cell carcinoma NCI-H460 cell . REF100453 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 50 ng/mL . . . Melanoma SK-MEL-2 cell . REF100435 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 50 ng/mL . . . Lymphoma P388 cell . REF101934 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 50 ng/mL . . . Hepatoblastoma Hep-G2 cell . REF100550 DRG00008 Dexamethasone Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Acute monocytic leukemia THP-1 cell . REF100660 DRG00009 Camptothecin Half Maximal Cytotoxicity Concentration (CC50) = 50 nM . . . Lung squamous cell carcinoma SK-MES-1 cell . REF102288 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Prostate carcinoma DU145 cell . REF101754 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 50 nM . . . Endocervical adenocarcinoma HeLa cell . REF101125 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Leukemia C8166 cell . REF101925 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Lymphoblastic leukemia CCRF-SB cell . REF101925 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Normal MT4 cell . REF101925 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF101925 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Colon adenocarcinoma Caco-2 cell . REF101866 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Astrocytoma U-251MG cell . REF101784 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 50 nM . . . Colon cancer HT29 cell . REF101750 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Acute myeloid leukemia HL-60 cell . REF101645 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 50 nM . . . Breast adenocarcinoma MDA-MB-468 cell . REF101480 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Endocervical adenocarcinoma HeLa cell . REF101472 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101418 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Acute monocytic leukemia MV4-11 cell . REF101359 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Normal NIH3T3 cell . REF100969 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Acute monocytic leukemia THP-1 cell . REF100779 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100545 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Invasive breast carcinoma MCF-7 cell . REF100371 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Lymphoblastic leukemia L1210 cell . REF100301 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 50 nM . . . Melanoma Malme-3M cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 50 nM . . . Renal carcinoma RXF 393 cell . REF101147 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Hepatoblastoma Hep-G2 cell . REF101026 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Colon adenocarcinoma DLD-1 cell . REF100948 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Astrocytoma SF268 cell . REF100708 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Lymphoma P388 cell . REF100708 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100708 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Colon cancer HT29 cell . REF100598 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Lung adenocarcinoma A-549 cell . REF102379 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Chronic myeloid leukemia K562 cell . REF102319 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Invasive breast carcinoma MCF-7 cell . REF100710 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101568 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Chronic myeloid leukemia K562 cell . REF102193 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Lymphoblastic leukemia L1210 cell . REF102046 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 50 nM . . . Mouse melanoma B16-F10 cell . REF102504 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 50 ug/mL . . . Small cell lung carcinoma PC-6 cell . REF102014 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) = 50 ug/mL . . . Erythroleukemia HEL cell . REF100042 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 50 uM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF102296 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 50 uM . . . Invasive breast carcinoma MCF-7 cell . REF100468 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 50 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102148 DRG00221 Acyclovir Half Maximal Effective Concentration (EC50) = 50 uM . . . Normal MRC5 cell . REF100060 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 50.1 uM . . . Gliosarcoma SF539 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 50.1 uM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 50.1 uM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 50.1 uM . . . Pleural epithelioid mesothelioma NCI-H226 cell . REF102249 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 50.11872 uM . . . Astrocytoma SF268 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 50.11872 uM . . . Cutaneous melanoma SK-MEL-28 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 50.11872 uM . . . Glioblastoma SF-295 cell . REF100098 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 50.11872 uM . . . Cutaneous melanoma SK-MEL-28 cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 50.11872 uM . . . Renal carcinoma UO-31 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 50.12 nM . . . Colon adenocarcinoma KM12 cell . REF102222 DRG00009 Camptothecin Tumor Growth Inhibition value (TGI) = 50.12 uM . . . Chronic myeloid leukemia K562 cell . REF100902 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 50.3±13.4 nM 24 h . . Minimally invasive lung adenocarcinoma H1650 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 50.35 uM . . . Melanoma LOX IMVI cell . REF101480 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 50.43 uM . . . Lung adenocarcinoma A-549 cell . REF102480 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 50.5±38.7 nM 24 h . . Tongue squamous cell carcinoma PE/CA-PJ15 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) > 500 µM 1 h . . Adult T acute lymphoblastic leukemia Molt-3 T cell "We next determined whether treatment of HCAEC and Molt-3 T cells with peptides, MTX, and MTX-peptide conjugates resulted in inhibition of cell proliferation. Both HCAEC and Molt-3 T cells were affected by test compound in different levels. None of the molecules caused growth stimulation or total culture extinction. A net cell killing of HCAEC was observed upon treatment with MTX at all test concentrations while MTX affected net killing at 1.0 µM in Molt-3 T cells. The MTX-peptide conjugates were less toxic than MTX. In HCAEC, the net cell killing was at lower concentration for MTX at 0.1 µM compared to MTX-peptide conjugates at 500 µM. The net cell killing of Molt-3 T cells was found at 1.0 µM for MTX and 50 µM for MTX-peptide conjugates. For all test concentrations, the conjugates only resulted in HCAEC partial growth inhibition. For Molt-3 T cells, a total growth inhibition emerged at 100 µM for cLABL and cLBEL; however, 500 µM cLABL and cLBEL did not cause total cell killing for T cells." REF00259 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Colon adenocarcinoma HCT 15 cell . REF100819 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Endocervical adenocarcinoma HeLa cell . REF100569 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Cervical squamous cell carcinoma ME-180 cell . REF101981 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Colon carcinoma HCT 116 cell . REF101876 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Endocervical adenocarcinoma HeLa cell . REF101809 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 500 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101471 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Prostate carcinoma PC-3 cell . REF101225 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Invasive breast carcinoma MCF-7 cell . REF101130 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Bone marrow neuroblastoma SH-SY5Y cell . REF100980 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Hepatoblastoma Hep-G2 cell . REF100954 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100662 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100291 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Invasive breast carcinoma MCF-7 cell . REF101174 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 500 nM . . . Acute monocytic leukemia THP-1 cell . REF102219 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 500 ug/mL . . . Sezary syndrome H9 cell . REF102076 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 500 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102042 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 500 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100035 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 501 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101152 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 51 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF100139 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 51 nM . . . Prostate carcinoma DU145 cell . REF101775 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 51 nM . . . Lung adenocarcinoma A-549 cell . REF101676 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 51 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF101133 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 51 nM . . . Ovarian adenocarcinoma 1A9/ptx-22 cell . REF100568 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 51.29 uM . . . Lung large cell carcinoma NCI-H460 cell . REF101566 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 51.3 uM . . . Lung large cell carcinoma NCI-H460 cell . REF101033 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 51.4 nM . . . Normal COLO205 cell . REF102166 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 51.5 uM . . . T acute lymphoblastic leukemia Jurkat cell . REF101720 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 51.64 uM . . . Lung adenocarcinoma A-549 cell . REF102330 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 51.7 uM . . . Invasive breast carcinoma T-47D cell . REF102370 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 51.8 uM . . . Invasive breast carcinoma T-47D cell . REF102293 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 510 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 510 nM . . . Endocervical adenocarcinoma HeLa cell . REF101364 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 510 nM . . . Gastric carcinoma NUGC-3 cell . REF101169 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 510 nM . . . Lung adenocarcinoma NCI-H23 cell . REF100746 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 510.6 nM . . . Colon adenocarcinoma DLD-1 cell . REF101767 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 512 nM . . . Prostate carcinoma LNCaP cell . REF100967 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 52 nM . . . Astrocytoma U-251MG cell . REF101855 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 52 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101417 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 52 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101112 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 52 nM . . . Astrocytoma SF268 cell . REF100270 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 52 nM . . . Breast carcinoma MX1 cell . REF102306 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 52.07 uM . . . Invasive breast carcinoma MCF-7 cell . REF102480 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 52.48 nM . . . Colon adenocarcinoma HCC 2998 cell . REF100123 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 52.8 nM . . . Prostate carcinoma DU145 cell . REF100293 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 520 nM . . . Melanoma UACC-62 cell . REF102305 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 520 nM . . . Burkitt lymphoma CA46 cell . REF101336 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 520 nM . . . Invasive breast carcinoma Hs 578T cell . REF101660 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 520 nM . . . Lung papillary adenocarcinoma PC-12 cell . REF101620 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 520 nM . . . Colon carcinoma HCT 116 cell . REF100907 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 520 nM . . . Lung adenocarcinoma A-549 cell . REF100895 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 520 nM . . . Colon carcinoma Col2 cell . REF100428 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 520 nM . . . Normal CHO-TAX 5-6 cell . REF100952 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 520.2 nM . . . Colon adenocarcinoma LoVo cell . REF101767 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 525.9±24.7 nM 24 h . . Pancreatic ductal adenocarcinoma PANC-1 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 53 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100151 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 53 nM . . . Colon adenocarcinoma WiDr cell . REF100310 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 53 nM . . . Gastric adenocarcinoma AGS cell . REF101819 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 53 ug/mL . . . Colon adenocarcinoma LoVo cell . REF100281 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 53 uM . . . Gastric adenocarcinoma AGS cell . REF101800 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 53 uM . . . Normal Vero cell . REF102302 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 53 uM . . . Normal MT4 cell . REF102011 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 53.3 nM . . . Cervical carcinoma L02 cell . REF101643 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 53.3 uM . . . Acute myeloid leukemia HL-60 cell . REF100876 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 53.46 uM . . . Melanoma B16 cell . REF102133 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 53.52 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102330 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 53.84 uM . . . Colon carcinoma HCT 116 cell . REF102402 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 530 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101878 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 530 nM . . . Rhabdomyosarcoma RD cell . REF101555 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 530 nM . . . Normal BALB/3T3 cell . REF101359 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 530 nM . . . Invasive breast carcinoma MCF-7 cell . REF100741 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 532 nM . . . Acute myeloid leukemia HL-60 cell . REF101493 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 54 ng/mL . . . Normal Vero cell . REF100259 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 54 nM . . . Colon adenocarcinoma DLD-1 cell . REF100740 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 54 nM . . . Invasive breast carcinoma MCF-7 cell . REF100659 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 54 nM . . . Colon cancer HT29 cell . REF102358 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 54.247 uM . . . Pancreatic ductal adenocarcinoma Capan-2 cell . REF102455 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 54.6±7.4 nM 24 h . . Breast adenocarcinoma MDA-MB-231 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 54.72 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF102480 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 54.8 uM . . . Invasive ductal carcinoma MCF7/PTX cell . REF101724 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 540 nM . . . Endocervical adenocarcinoma HeLa cell . REF102366 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 540 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101617 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 540 nM . . . Minimally invasive lung adenocarcinoma NCI-H322M cell . REF101480 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 540 nM . . . Hepatoblastoma Hep-G2 cell . REF101474 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 540 nM . . . Invasive breast carcinoma MCF-7 cell . REF100897 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 540 nM . . . Astrocytoma U-251MG cell . REF102329 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 547 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100230 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 55 nM . . . Invasive breast carcinoma MCF-7 cell . REF100341 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 55 nM . . . Colon cancer HT29 cell . REF100147 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 55.2 uM . . . Hepatoblastoma Hep-G2 cell . REF102346 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 550 nM . . . Cervical squamous cell carcinoma SiHa cell . REF101586 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 550 nM . . . Lung adenocarcinoma A-549 cell . REF101702 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 550 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101156 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 550 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100521 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 550 nM . . . Breast carcinoma MCF7R cell . REF100484 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 56 ng/mL . . . T acute lymphoblastic leukemia MOLT-4 cell . REF102028 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 56 nM . . . Invasive breast carcinoma MCF-7 cell . REF101002 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 56 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100732 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 56 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100635 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 56 nM . . . Colon cancer HT29 cell . REF100348 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 56 uM . . . Lung adenocarcinoma A-549 cell . REF101124 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 56 uM . . . Melanoma B16 cell . REF101314 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 56.0±14.7 nM 24 h . . Mammary carcinoma 4T1 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 56.4 nM . . . Colon cancer HT29 cell . REF100293 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 56.5 uM . . . Endocervical adenocarcinoma HeLa cell . REF101959 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 56.6 uM . . . Ovarian endometrioid adenocarcinoma A2780/Taxol cell . REF101428 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 56.83 uM . . . Chronic myeloid leukemia K562 cell . REF101020 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 560 nM . . . Lung adenocarcinoma A-549 cell . REF101142 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 560 nM . . . Acute myeloid leukemia HL-60 cell . REF102397 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 567 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100262 DRG00045 Duocarmycin Sa Half Maximal Inhibitory Concentration (IC50) = 57 nM 72 h . . Colon carcinoma HCT 116 cell "All cell lines demonstrated sensitivity toward the DSA-PABA payload 5 in the nanomolar range. The cleaved peptide 6, and the benzyl protected control peptide 4, had no appreciable effect on cell proliferation (>100 µM), suggesting that any observed cytotoxic activity is due to the DSA warhead. Interestingly, PDC 7, without the cathepsin B cleavable sequence, also had no appreciable effect on cell proliferation (>100 µM), despite possessing the active DSA DNA alkylating moiety. Perhaps this PDC is either not being taken up into cells or not being broken down by proteases and peptidases in the cell. In both cases, the warhead may not be reaching the nucleus, the site of action of the duocarmycins. Cell lines that demonstrated appreciable levels of TFα were sensitive to PDC 3. Interestingly, HCT116, which had relatively high TFα expression and cathepsin B activity, demonstrated the greatest sensitivity to PDC 3, approaching similar potency to the payload 5. Excitingly, A549, H292, and 16HBE14o, which showed no detectable TFα expression, appeared unaffected by PDC 3 up to 100 µM, suggesting that TFα expression is required for the efficacy of PDC 3." REF00117 DRG00009 Camptothecin Half Maximal Effective Dosage (ED50) = 57 nM . . . Colon carcinoma Col2 cell . REF100419 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 57 nM . . . Chronic myeloid leukemia K562 cell . REF100280 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 57 nM . . . Prostate carcinoma PC-3 cell . REF100296 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 57 nM . . . Colon adenocarcinoma LoVo cell . REF100200 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 57 ug/mL . . . Prostate carcinoma DU145 cell . REF100095 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 57 uM . . . Colon adenocarcinoma SW480 cell . REF102228 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 57.2 uM . . . Prostate carcinoma PC-3 cell . REF101051 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 57.7 ng/ml . . . Prostate carcinoma PC-3 cell . REF100455 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 570 nM . . . Invasive breast carcinoma MCF-7 cell . REF100836 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 570 nM . . . Hepatoblastoma Hep-G2 cell . REF101734 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 570 nM . . . Hepatocellular carcinoma SMMC-7721 cell . REF101346 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 570 nM . . . Renal carcinoma TK-10 cell . REF100341 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 570 nM . . . Invasive breast carcinoma MCF-7 cell . REF102373 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 570 nM . . . T acute lymphoblastic leukemia RPMI-8402 cell . REF100387 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 578.2 nM . . . Hepatoma Bel-7402 cell . REF100911 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 58 ng/mL . . . Lung small cell carcinoma NCI-H187 cell . REF100733 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 58 nM . . . Lung adenocarcinoma A-549 cell . REF100719 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 58 nM . . . Lung adenocarcinoma A-549 cell . REF101302 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 58 uM . . . Gastric cancer MGC-803 cell . REF102460 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 58.61 uM . . . Colon adenocarcinoma SW620 cell . REF101566 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 58.74 uM . . . Cervical carcinoma L02 cell . REF102430 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 580 nM . . . Endocervical adenocarcinoma HeLa cell . REF100775 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 580 nM . . . Normal MCF-10A cell . REF101653 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 580 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101461 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 580 nM . . . Hepatoma Bel-7402 cell . REF100800 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 59 nM . . . Laryngeal carcinoma HEp-2 cell . REF100454 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 59 nM . . . Hepatoblastoma Hep-G2 cell . REF100738 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 59.5 nM . . . Lung adenocarcinoma A-549 cell . REF100581 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 590 nM . . . Chronic myeloid leukemia K562 cell . REF100904 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 590 nM . . . Prostate carcinoma PC-3 cell . REF101753 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 590 nM . . . Hepatoblastoma Hep-G2 cell . REF101157 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 590 nM . . . Lung adenocarcinoma A-549 cell . REF100981 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 590 nM . . . Invasive breast carcinoma MCF-7 cell . REF100855 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 590 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101199 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 595 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100193 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6 µM 36 h . . Glioblastoma U-87MG cell "Doxorubicin (DOX) is one of the most effective anticancer drugs and has been successfully used in clinical practice. However, DOX cannot differentiate between cancer cells and normal cells, which may induce unwanted side effects and severe toxicity. Compared with traditional small-molecule anticancer drugs, the peptide-drug conjugates (PDCs) have enhanced targeting specificity and water solubility. Based on these advantages, to further explore the function of 10a, we designed and prepared a anticancer PDC drug compound RGD-GFLG-DOX containing the tetrapeptide linker Gly-Phe-Leu-Gly, which can be cleaved in presence of cathepsin B, a highly upregulated enzyme in malignant tumors, to release the drug. RGD-GFLG was synthesized as a control. The inhibitory effects of RGD-GFLG-DOX on cancer cell lines were assessed using cytotoxicity assay. Specifically, the effects of RGD-GFLG-DOX were evaluated on integrin αvβ3-positive cancer cell lines, including A549 and U87MG cells, integrin αvβ3-negative cancer cell lines such as HeLa and MCF-7 cells, as well as normal cell lines, namely LO2 and MIHA cells. RGD-GFLG-DOX exhibited a lower cytotoxicity on HeLa, MCF-7, LO2 and MIHA cells, but a stronger cytotoxicity than DOX on A549 and U87MG cells. For comparison, RGD-GFLG demonstrated minimal cytotoxicity. In addition, the cytotoxicity of RGD-GFLG-DOX with various concentrations (040µM) on A549 and U87MG cells was studied. The results showed that the cytotoxicity of RGD-GFLG-DOX on A549 and U87MG cells was dose-dependent. These indicate that RGD-GFLG-DOX has a good specificity and inhibitory activity toward integrin αvβ3-overexpressed A549 and U87MG cells." REF00270 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6 µM 36 h . . Lung adenocarcinoma A-549 cell "Doxorubicin (DOX) is one of the most effective anticancer drugs and has been successfully used in clinical practice. However, DOX cannot differentiate between cancer cells and normal cells, which may induce unwanted side effects and severe toxicity. Compared with traditional small-molecule anticancer drugs, the peptide-drug conjugates (PDCs) have enhanced targeting specificity and water solubility. Based on these advantages, to further explore the function of 10a, we designed and prepared a anticancer PDC drug compound RGD-GFLG-DOX containing the tetrapeptide linker Gly-Phe-Leu-Gly, which can be cleaved in presence of cathepsin B, a highly upregulated enzyme in malignant tumors, to release the drug. RGD-GFLG was synthesized as a control. The inhibitory effects of RGD-GFLG-DOX on cancer cell lines were assessed using cytotoxicity assay. Specifically, the effects of RGD-GFLG-DOX were evaluated on integrin αvβ3-positive cancer cell lines, including A549 and U87MG cells, integrin αvβ3-negative cancer cell lines such as HeLa and MCF-7 cells, as well as normal cell lines, namely LO2 and MIHA cells. RGD-GFLG-DOX exhibited a lower cytotoxicity on HeLa, MCF-7, LO2 and MIHA cells, but a stronger cytotoxicity than DOX on A549 and U87MG cells. For comparison, RGD-GFLG demonstrated minimal cytotoxicity. In addition, the cytotoxicity of RGD-GFLG-DOX with various concentrations (040µM) on A549 and U87MG cells was studied. The results showed that the cytotoxicity of RGD-GFLG-DOX on A549 and U87MG cells was dose-dependent. These indicate that RGD-GFLG-DOX has a good specificity and inhibitory activity toward integrin αvβ3-overexpressed A549 and U87MG cells." REF00270 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6 µM 36 h . . Normal MIHA cell "Doxorubicin (DOX) is one of the most effective anticancer drugs and has been successfully used in clinical practice. However, DOX cannot differentiate between cancer cells and normal cells, which may induce unwanted side effects and severe toxicity. Compared with traditional small-molecule anticancer drugs, the peptide-drug conjugates (PDCs) have enhanced targeting specificity and water solubility. Based on these advantages, to further explore the function of 10a, we designed and prepared a anticancer PDC drug compound RGD-GFLG-DOX containing the tetrapeptide linker Gly-Phe-Leu-Gly, which can be cleaved in presence of cathepsin B, a highly upregulated enzyme in malignant tumors, to release the drug. RGD-GFLG was synthesized as a control. The inhibitory effects of RGD-GFLG-DOX on cancer cell lines were assessed using cytotoxicity assay. Specifically, the effects of RGD-GFLG-DOX were evaluated on integrin αvβ3-positive cancer cell lines, including A549 and U87MG cells, integrin αvβ3-negative cancer cell lines such as HeLa and MCF-7 cells, as well as normal cell lines, namely LO2 and MIHA cells. RGD-GFLG-DOX exhibited a lower cytotoxicity on HeLa, MCF-7, LO2 and MIHA cells, but a stronger cytotoxicity than DOX on A549 and U87MG cells. For comparison, RGD-GFLG demonstrated minimal cytotoxicity. In addition, the cytotoxicity of RGD-GFLG-DOX with various concentrations (040µM) on A549 and U87MG cells was studied. The results showed that the cytotoxicity of RGD-GFLG-DOX on A549 and U87MG cells was dose-dependent. These indicate that RGD-GFLG-DOX has a good specificity and inhibitory activity toward integrin αvβ3-overexpressed A549 and U87MG cells." REF00270 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 6 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100363 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Acute myeloid leukemia HL-60 cell . REF100751 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Plasma cell myeloma RPMI-8226 cell . REF100681 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Bladder carcinoma T24 cell . REF100532 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . T acute lymphoblastic leukemia RPMI-8402 cell . REF100443 DRG00009 Camptothecin Half Maximal Cytotoxicity Concentration (CC50) = 6 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100269 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Colon carcinoma HCT 116 cell . REF100751 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Cisplatin-resistant ovarian carcinoma A2780 cisR cell . REF100454 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100305 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Colon carcinoma HCT 116 cell . REF101829 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101540 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Hepatoma Bel-7402 cell . REF101133 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Invasive breast carcinoma MCF-7 cell . REF101062 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Colon cancer HT29 cell . REF101034 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Breast ductal carcinoma BT-549 cell . REF100948 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100948 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Lung adenocarcinoma A-549 cell . REF100493 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Cervical epithelial carcinoma KB 3-1 cell . REF100433 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100313 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Pancreatic ductal adenocarcinoma BxPC-3 cell . REF102412 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Colon carcinoma HCT 116 cell . REF102228 DRG00013 Gemcitabine Half Maximal Growth Inhibition (GI50) = 6 nM . . . Prostate carcinoma PC-3 cell . REF102202 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Colon carcinoma CT26 cell . REF100967 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Lung carcinoma NCI-H128 cell . REF100327 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101262 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Lymphoblastic leukemia L1210 cell . REF101549 DRG00296 Zidovudine Half Maximal Effective Dosage (ED50) = 6 nM . . . Normal MT4 cell . REF102030 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 6 nM . . . Normal MT4 cell . REF102011 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100071 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Chronic myeloid leukemia K562 cell . REF102403 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 6 nM . . . Renal carcinoma A498 cell . REF102357 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 6 nM . . . Astrocytoma SF268 cell . REF102315 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 6 nM . . . Melanoma UACC-62 cell . REF102315 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 6 nM . . . Renal adenocarcinoma ACHN cell . REF102315 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 6 nM . . . Renal cell carcinoma SN12C cell . REF102290 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 6 nM . . . Astrocytoma U-251MG cell . REF102105 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101585 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Invasive breast carcinoma MCF-7 cell . REF101159 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 6 nM . . . Hepatocellular carcinoma SNU-423 cell . REF100116 DRG00019 Methotrexate Half Maximal Infective Dose (ID50) = 6 nmol/L . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102003 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6 ug . . . Endocervical adenocarcinoma HeLa cell . REF100226 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 6 uM . . . Invasive breast carcinoma MCF-7 cell . REF100926 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 6 uM . . . Tongue squamous cell carcinoma SAS cell . REF100622 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6 uM . . . Prostate carcinoma DU145 cell . REF101150 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6 uM . . . Prostate carcinoma PC-3 cell . REF101130 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6 uM . . . Colon adenocarcinoma LoVo cell . REF100196 DRG00221 Acyclovir Half Maximal Effective Concentration (EC50) = 6 uM . . . Normal Vero cell . REF100064 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 6 uM . . . Normal MT4 cell . REF102053 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.03 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101351 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 6.05 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100978 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.06 uM . . . Lung large cell carcinoma NCI-H460 cell . REF101037 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.072 uM . . . Prostate carcinoma DU145 cell . REF101353 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 6.08 uM . . . Colon adenocarcinoma HCT 15 cell . REF101358 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 6.1 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100455 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.1 nM . . . Ovarian carcinoma A121 cell . REF101967 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.1 nM . . . Breast adenocarcinoma MDA-MB-468 cell . REF101557 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.1 uM . . . Colon carcinoma HCT 116 cell . REF101854 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.1 uM . . . Normal HEK293 cell . REF101797 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.1 uM . . . Renal carcinoma A498 cell . REF101689 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.1 uM . . . Invasive breast carcinoma MCF-7 cell . REF101216 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 6.1 uM . . . Colon carcinoma HCT 116 cell . REF102256 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 6.1 uM . . . Colon carcinoma HCT 116 cell . REF102513 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.11 uM . . . Hepatoblastoma Hep-G2 cell . REF101600 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.18 uM . . . Colon carcinoma HCT 116 cell . REF100667 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.2 nM . . . Osteosarcoma SJSA-1 cell . REF100626 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.2 nM . . . Lung adenocarcinoma A-549 cell . REF101478 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.2 uM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF102384 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.2 uM . . . Colon adenocarcinoma T84 cell . REF101389 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.2 uM . . . Invasive breast carcinoma MCF-7 cell . REF101356 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.2 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101294 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 6.22 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100455 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.24 ug/mL . . . Gestational choriocarcinoma BeWo cell . REF102103 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.29 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101724 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 6.3 nM . . . Hepatoblastoma Hep-G2 cell . REF100294 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.3 nM . . . Normal CH1 cell . REF100319 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 6.3 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100296 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 6.3 nM . . . Chronic myeloid leukemia K562 cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 6.3 nM . . . Lung adenocarcinoma A-549 cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 6.3 nM . . . Lung adenocarcinoma NCI-H23 cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 6.3 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 6.3 nM . . . Prostate carcinoma PC-3 cell . REF101860 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 6.3 nM . . . Leukemia SR cell . REF101624 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.3 nM . . . Lung adenocarcinoma A-549 cell . REF101369 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.3 nM . . . Endocervical adenocarcinoma HeLa cell . REF101124 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.3 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100611 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.3 nM . . . Ovarian carcinoma A121 cell . REF100230 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.3 ug/mL . . . Colon carcinoma HCT 116 cell . REF101447 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.3 uM . . . Colon cancer HT29 cell . REF102355 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.3 uM . . . Endocervical adenocarcinoma HeLa cell . REF101705 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.3 uM . . . Normal Vero cell . REF100752 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 6.3 uM . . . Amelanotic melanoma MDA-MB-435 cell . REF101339 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 6.30957 uM . . . Colon adenocarcinoma HCT 15 cell . REF100098 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 6.30957 uM . . . Melanoma LOX IMVI cell . REF100098 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 6.30957 uM . . . Colon adenocarcinoma HCC 2998 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 6.30957 uM . . . Colon adenocarcinoma KM12 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 6.30957 uM . . . Melanoma UACC-257 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 6.30957 uM . . . Ovarian adenocarcinoma OVCAR-4 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 6.30957 uM . . . Renal carcinoma A498 cell . REF100756 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 6.30957 uM . . . Colon cancer HT29 cell . REF102222 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.36 uM . . . Colon carcinoma HCT 116 cell . REF102166 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 6.37 ug/mL . . . Prostate carcinoma PC-3 cell . REF100221 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.39 ng/mL . . . Invasive breast carcinoma ZR-75-1 cell . REF100323 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 6.4 ng/mL . . . Renal carcinoma A498 cell . REF100338 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 6.4 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101340 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.4 uM . . . Endocervical adenocarcinoma HeLa cell . REF102350 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 6.4 uM . . . Hepatoblastoma Hep-G2 cell . REF101046 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 6.4 uM . . . Lung adenocarcinoma A-549 cell . REF100880 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.46 uM . . . Gastric carcinoma SGC-7901 cell . REF102456 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.46 uM . . . Prostate carcinoma LNCaP cell . REF101351 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 6.49 ng/ml . . . Renal carcinoma A498 cell . REF100234 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.5 ug/mL . . . Normal Vero cell . REF102263 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 6.5 uM . . . Lung large cell carcinoma NCI-H460 cell . REF102277 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 6.5 uM . . . Invasive breast carcinoma MCF-7 cell . REF100112 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.52 uM . . . Lung adenocarcinoma PC-9 cell . REF102508 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 6.55 uM . . . Gastric cancer MGC-803 cell . REF101665 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.57±0.61 µM 72 h . . Neuroblastoma Kelly-ADR cell "The cytotoxic effect of the peptide-drug conjugate on Kelly-WT cells was comparable to that of 9, but not as strong as the one of the native drug. Contrary to the other utilized substances, the antiproliferative action of the bioconjugate in wild-type and drug-resistant cells was nearly the same. In comparison with doxorubicin the cytotoxicity of 10 against Kelly-ADR cells was increased by a factor of 3 according to the obtained IC50 values. Even the unmodified dimer had roughly the same cytotoxic effect on Kelly-ADR cells as doxorubicin." REF00017 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.6 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101571 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.6 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101242 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.6 uM . . . Normal Vero cell . REF101565 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 6.6 uM . . . Lung adenocarcinoma PC-9 cell . REF102046 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.61 uM . . . Lung adenocarcinoma A-549 cell . REF101029 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.68 uM . . . Normal WI-38 cell . REF101672 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 6.69 mM . . . Colon carcinoma HCT 116 cell . REF101946 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 6.69 ng/ml . . . Colon cancer HT29 cell . REF100209 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.7 uM . . . Colon adenocarcinoma Caco-2 cell . REF100946 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.7 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100476 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.71 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF100784 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.75 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101424 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.75 uM . . . Invasive breast carcinoma MCF-7 cell . REF101252 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.76 uM . . . Lung adenocarcinoma A-549 cell . REF102348 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 6.78 µM 24 h . . Endocervical adenocarcinoma HeLa cell "First, we probed the novel PDCs in non-cancerous human foreskin fibroblasts (HFF-1 cells). After 24 h treatment with different concentrations of PDCs, HFF-1 cells were still viable, while after adding doxorubicin viability was decreased up to 72%. In comparison, when we elucidated PDC activity in HeLa cells and exposed them for 24 h to various concentrations of the conjugates (2.570 M), all of the PDCs, as well as free Dox, exhibited EC50 values in the lower micromolar range (PDC-1: 15.34 M, PDC-2: 14.47 M, PDC-3: 27.01 M, Dox: 6.78 M data not shown). The higher activity compared to HFF cells might be attributed to the fact that the PDCs were internalized to far less of an extent into the non-cancerous cell line. This observation might be advantageous and could reflect some selectivity of the more basic and positively charged peptides towards cancerous cells. We also noted that the obtained EC50 values somehow agreed with the results of the former assays. For example, sC18δE was taken up to a significantly higher extent compared to sC18* and should, therefore, exhibit higher activity, e.g., drug delivery. However, surprisingly, the EC50 values of the PDCs containing sC18 and sC18δE were quite similar, although sC18δE significantly outcompeted sC18 in internalization activity." REF00240 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.8 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101648 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.8 nM . . . Pleural epithelioid mesothelioma NCI-H226 cell . REF100514 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 6.8 nM . . . Colon carcinoma HCT 116 cell . REF102457 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.8 uM . . . Colon carcinoma RKO cell . REF102355 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.8 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100932 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 6.8 uM . . . Invasive breast carcinoma MCF-7 cell . REF102477 DRG00162 Curcumin Half Maximal Inhibitory Concentration (IC50) = 6.81 uM . . . Chronic myeloid leukemia K562 cell . REF100618 DRG00011 Doxorubicin 90% Lethal Concentration (IC50) = 6.82 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100820 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.82 uM . . . Gastric cancer MGC-803 cell . REF101834 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 6.84 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100144 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 6.9 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101743 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 6.9 nM . . . Colon adenocarcinoma T84 cell . REF101852 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 6.9 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF100537 DRG00005 Primaquine Half Maximal Inhibitory Concentration (IC50) = 6.9 uM . . . Invasive breast carcinoma MCF-7 cell . REF102198 DRG00224 Pemetrexed Half Maximal Inhibitory Concentration (IC50) = 6.9 uM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF102420 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 6.92 nM . . . Acute myeloid leukemia HL-60 cell . REF100563 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 6.96 uM . . . Colon adenocarcinoma SW620 cell . REF101803 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 6.96 uM . . . Prostate carcinoma PC-3 cell . REF101570 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 6.98 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102387 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 ng/mL . . . Ileocecal adenocarcinoma HCT-8 cell . REF100916 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 60 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100495 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 60 ng/mL . . . Glioma XF498 cell . REF100495 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 60 ng/mL . . . Melanoma SK-MEL-2 cell . REF100403 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 ng/mL . . . Melanoma UACC-62 cell . REF100328 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 60 ng/mL . . . Colon cancer HT29 cell . REF100314 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 ng/mL . . . Colon cancer HT29 cell . REF100216 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 60 ng/mL . . . Ileocecal adenocarcinoma HCT-8 cell . REF100580 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Hepatocellular carcinoma Huh-7 cell . REF101108 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 60 nM . . . Chronic myeloid leukemia K562 cell . REF100836 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Invasive breast carcinoma MCF-7 cell . REF100786 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Invasive breast carcinoma MCF-7 cell . REF100261 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Colon adenocarcinoma SW480 cell . REF101926 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101879 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 60 nM . . . Lung adenocarcinoma A-549 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Lung small cell carcinoma NCI-H187 cell . REF101560 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 60 nM . . . Invasive breast carcinoma T-47D cell . REF101480 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Acute myeloid leukemia HL-60 cell . REF101102 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Endocervical adenocarcinoma HeLa cell . REF101073 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Invasive breast carcinoma MCF-7 cell . REF101056 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100907 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF100787 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 60 nM . . . Colon cancer HT29 cell . REF100726 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 60 nM . . . Prostate carcinoma DU145 cell . REF100653 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Hepatoblastoma Hep-G2 cell . REF100623 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Renal carcinoma RXF 944 cell . REF100394 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Cutaneous melanoma SK-MEL-28 cell . REF100370 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Normal CHO cell . REF100260 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Lymphoblastic leukemia L1210 cell . REF100963 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Hepatoma Bel-7402 cell . REF100857 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF100774 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 60 nM . . . Colon carcinoma HCT 116 cell . REF100735 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Laryngeal carcinoma HEp-2 cell . REF101568 DRG00020 Docetaxel Half Maximal Cytotoxicity Concentration (CC50) = 60 nM . . . Laryngeal carcinoma HEp-2 cell . REF101568 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Acute myeloid leukemia RPMI 6410 cell . REF100023 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 60 nM . . . Normal MT4 cell . REF102006 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 60 uM . . . Lymphoblastic leukemia L1210 cell . REF100160 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 60 uM . . . Normal MT4 cell . REF102182 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 60.01 uM . . . Endocervical adenocarcinoma HeLa cell . REF101453 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 60.9 ug/mL . . . Renal carcinoma A498 cell . REF100982 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Invasive breast carcinoma T-47D cell . REF100763 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Colon cancer HT29 cell . REF100547 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Colon adenocarcinoma HCT 15 cell . REF101454 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Acute myeloid leukemia HL-60 cell . REF101045 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 600 nM . . . Endocervical adenocarcinoma HeLa cell . REF100417 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Astrocytoma SF268 cell . REF100950 DRG00010 Daunorubicin Half Maximal Growth Inhibition (GI50) = 600 nM . . . Astrocytoma SF268 cell . REF100836 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101863 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Lung adenocarcinoma A-549 cell . REF101646 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101594 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Chronic myeloid leukemia K562 cell . REF101575 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Lung mucoepidermoid carcinoma NCI-H292 cell . REF101466 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Endocervical adenocarcinoma HeLa cell . REF101263 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Prostate carcinoma PC-3 cell . REF101220 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Cutaneous melanoma SK-MEL-28 cell . REF100946 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Astrocytoma U-251MG cell . REF100748 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Invasive breast carcinoma ZR-75-1 cell . REF100662 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Endocervical adenocarcinoma HeLa cell . REF101001 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 600 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100760 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 606 nM . . . Endocervical adenocarcinoma HeLa cell . REF101493 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 61 ng/mL . . . Colon carcinoma KM-20L2 cell . REF102269 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 61 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100518 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 61 nM . . . Hepatocellular carcinoma SNU-398 cell . REF100735 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 61 nM . . . Renal carcinoma A498 cell . REF100514 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 61 uM . . . Normal MT4 cell . REF102181 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 61.2 nM . . . Lung small cell carcinoma DMS 114 cell . REF100197 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 61.8 nM . . . Colon cancer HT29 cell . REF100367 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 610 nM . . . Prostate carcinoma DU145 cell . REF100904 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 610 nM . . . Invasive breast carcinoma MCF-7 cell . REF100895 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 612 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100336 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 615 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100481 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 62.01 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100475 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 62.2 uM . . . Endocervical adenocarcinoma HeLa cell . REF101462 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 62.26 uM . . . Prostate carcinoma PC-3 cell . REF101023 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 62.303 uM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF102455 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 62.8 uM . . . Normal Vero cell . REF100053 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 62.8 uM . . . T acute lymphoblastic leukemia MOLT-4 cell . REF102091 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 620 nM . . . Chronic myeloid leukemia K562 cell . REF101485 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 620 nM . . . Colon adenocarcinoma WiDr cell . REF100229 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 620 nM . . . Minimally invasive lung adenocarcinoma NCI-H358 cell . REF100137 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 620 nM . . . Hepatoblastoma Hep-G2 cell . REF100667 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 620 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100474 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 620 nM . . . Invasive breast carcinoma MCF-7 cell . REF102046 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 63 nM . . . Uterine sarcoma MES-SA/Dx5 cell . REF100389 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 63 nM . . . Astrocytoma U-251MG cell . REF100270 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 63 nM . . . Colon adenocarcinoma HCC 2998 cell . REF102290 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 63.09573 uM . . . Ovarian adenocarcinoma OVCAR-4 cell . REF100098 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 63.09573 uM . . . Melanoma UACC-62 cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 63.09573 uM . . . Ovarian endometrioid adenocarcinoma IGROV-1 cell . REF102222 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 63.1 nM . . . Gliosarcoma SF539 cell . REF102227 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 63.1 nM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF102222 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 63.1 uM . . . Lung adenocarcinoma NCI-H23 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 63.1 uM . . . Melanoma Malme-3M cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 63.1 uM . . . Melanoma UACC-257 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 63.1 uM . . . Non-small cell lung carcinoma EKVX cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 63.1 uM . . . Ovarian adenocarcinoma OVCAR-4 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 63.1 uM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF102249 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 63.3 nM . . . Invasive breast carcinoma MCF-7 cell . REF101899 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 63.9±21.0 nM 24 h . . Invasive breast carcinoma MCF-7 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 630 nM . . . Lymphoblastic leukemia L1210 cell . REF102085 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 630 nM . . . Endocervical adenocarcinoma HeLa cell . REF100786 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 630 nM . . . Invasive breast carcinoma MCF-7 cell . REF101357 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 630 nM . . . Prostate carcinoma PC-3 cell . REF101159 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 630 nM . . . Hepatoblastoma Hep-G2 cell . REF100981 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 630 nM . . . Ovarian mixed germ cell tumor PA-1 cell . REF100723 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 630 nM . . . Ovarian adenocarcinoma OVCAR-4 cell . REF101860 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 630.96 nM . . . Colon cancer HT29 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 631 nM . . . Colon cancer HT29 cell . REF102253 DRG00008 Dexamethasone Minimum inhibitory concentration (MIC) > 64 µg/mL 18 h . . Klebsiella pneumoniae infection Klebsiella pneumoniae strain "To verify whether Omi-hyd-Dex@HA NPs inherited the antimicrobial activity of omiganan, the MICs were tested by the standardized agar doubling-dilution method as shown in Table 1. Omi-hyd-Dex@HA NPs and free omiganan showed similar extended broad-spectrum antibacterial activity for G+ bacteria, G- bacteria and fungi pathogens, including drug-sensitive strains (S. aureus, P. aeruginosa, K.P., Candida albicans) and drug-resistant strains (MRSA, MDR-K.P.). The MICs of Omi-hyd-Dex@HA NPs showed none or only a one-fold increase compared with the free Omiganan-NHNH2 group. In addition, free Dex did not show any antimicrobial activity for the tested pathogens, indicating that Dex moieties of Omi-hyd-Dex@HA NPs did not contribute to the bacterial killing effect. In contrast, vancomycin, as a standard drug regimen for drug-resistant G+ strains, showed inefficacious for G- strains and fungus. Similar results were also observed in oxacillin-treated groups. Therefore, Omi-hyd-Dex@HA NPs retained the broad-spectrum antimicrobial activity of omiganan." REF00291 DRG00008 Dexamethasone Minimum inhibitory concentration (MIC) > 64 µg/mL 18 h . . Klebsiella pneumoniae infection MDR Klebsiella pneumoniae strain "To verify whether Omi-hyd-Dex@HA NPs inherited the antimicrobial activity of omiganan, the MICs were tested by the standardized agar doubling-dilution method as shown in Table 1. Omi-hyd-Dex@HA NPs and free omiganan showed similar extended broad-spectrum antibacterial activity for G+ bacteria, G- bacteria and fungi pathogens, including drug-sensitive strains (S. aureus, P. aeruginosa, K.P., Candida albicans) and drug-resistant strains (MRSA, MDR-K.P.). The MICs of Omi-hyd-Dex@HA NPs showed none or only a one-fold increase compared with the free Omiganan-NHNH2 group. In addition, free Dex did not show any antimicrobial activity for the tested pathogens, indicating that Dex moieties of Omi-hyd-Dex@HA NPs did not contribute to the bacterial killing effect. In contrast, vancomycin, as a standard drug regimen for drug-resistant G+ strains, showed inefficacious for G- strains and fungus. Similar results were also observed in oxacillin-treated groups. Therefore, Omi-hyd-Dex@HA NPs retained the broad-spectrum antimicrobial activity of omiganan." REF00291 DRG00008 Dexamethasone Minimum inhibitory concentration (MIC) > 64 µg/mL 18 h . . Multiple-resistant Staphylococcus aureus infection Multiple-resistant staphylococcus aureus infection strain "To verify whether Omi-hyd-Dex@HA NPs inherited the antimicrobial activity of omiganan, the MICs were tested by the standardized agar doubling-dilution method as shown in Table 1. Omi-hyd-Dex@HA NPs and free omiganan showed similar extended broad-spectrum antibacterial activity for G+ bacteria, G- bacteria and fungi pathogens, including drug-sensitive strains (S. aureus, P. aeruginosa, K.P., Candida albicans) and drug-resistant strains (MRSA, MDR-K.P.). The MICs of Omi-hyd-Dex@HA NPs showed none or only a one-fold increase compared with the free Omiganan-NHNH2 group. In addition, free Dex did not show any antimicrobial activity for the tested pathogens, indicating that Dex moieties of Omi-hyd-Dex@HA NPs did not contribute to the bacterial killing effect. In contrast, vancomycin, as a standard drug regimen for drug-resistant G+ strains, showed inefficacious for G- strains and fungus. Similar results were also observed in oxacillin-treated groups. Therefore, Omi-hyd-Dex@HA NPs retained the broad-spectrum antimicrobial activity of omiganan." REF00291 DRG00008 Dexamethasone Minimum inhibitory concentration (MIC) > 64 µg/mL 18 h . . Staphylococcus aureus infection Staphylococcus aureus infection strain "To verify whether Omi-hyd-Dex@HA NPs inherited the antimicrobial activity of omiganan, the MICs were tested by the standardized agar doubling-dilution method as shown in Table 1. Omi-hyd-Dex@HA NPs and free omiganan showed similar extended broad-spectrum antibacterial activity for G+ bacteria, G- bacteria and fungi pathogens, including drug-sensitive strains (S. aureus, P. aeruginosa, K.P., Candida albicans) and drug-resistant strains (MRSA, MDR-K.P.). The MICs of Omi-hyd-Dex@HA NPs showed none or only a one-fold increase compared with the free Omiganan-NHNH2 group. In addition, free Dex did not show any antimicrobial activity for the tested pathogens, indicating that Dex moieties of Omi-hyd-Dex@HA NPs did not contribute to the bacterial killing effect. In contrast, vancomycin, as a standard drug regimen for drug-resistant G+ strains, showed inefficacious for G- strains and fungus. Similar results were also observed in oxacillin-treated groups. Therefore, Omi-hyd-Dex@HA NPs retained the broad-spectrum antimicrobial activity of omiganan." REF00291 DRG00008 Dexamethasone Minimum inhibitory concentration (MIC) > 64 µg/mL 18 h . . Pseudomonas aeruginosa strain infection Pseudomonas aeruginosa strain "To verify whether Omi-hyd-Dex@HA NPs inherited the antimicrobial activity of omiganan, the MICs were tested by the standardized agar doubling-dilution method as shown in Table 1. Omi-hyd-Dex@HA NPs and free omiganan showed similar extended broad-spectrum antibacterial activity for G+ bacteria, G- bacteria and fungi pathogens, including drug-sensitive strains (S. aureus, P. aeruginosa, K.P., Candida albicans) and drug-resistant strains (MRSA, MDR-K.P.). The MICs of Omi-hyd-Dex@HA NPs showed none or only a one-fold increase compared with the free Omiganan-NHNH2 group. In addition, free Dex did not show any antimicrobial activity for the tested pathogens, indicating that Dex moieties of Omi-hyd-Dex@HA NPs did not contribute to the bacterial killing effect. In contrast, vancomycin, as a standard drug regimen for drug-resistant G+ strains, showed inefficacious for G- strains and fungus. Similar results were also observed in oxacillin-treated groups. Therefore, Omi-hyd-Dex@HA NPs retained the broad-spectrum antimicrobial activity of omiganan." REF00291 DRG00008 Dexamethasone Minimum inhibitory concentration (MIC) > 64 µg/mL 18 h . . Candida albicans infection Candida albicans fungus strains "To verify whether Omi-hyd-Dex@HA NPs inherited the antimicrobial activity of omiganan, the MICs were tested by the standardized agar doubling-dilution method as shown in Table 1. Omi-hyd-Dex@HA NPs and free omiganan showed similar extended broad-spectrum antibacterial activity for G+ bacteria, G- bacteria and fungi pathogens, including drug-sensitive strains (S. aureus, P. aeruginosa, K.P., Candida albicans) and drug-resistant strains (MRSA, MDR-K.P.). The MICs of Omi-hyd-Dex@HA NPs showed none or only a one-fold increase compared with the free Omiganan-NHNH2 group. In addition, free Dex did not show any antimicrobial activity for the tested pathogens, indicating that Dex moieties of Omi-hyd-Dex@HA NPs did not contribute to the bacterial killing effect. In contrast, vancomycin, as a standard drug regimen for drug-resistant G+ strains, showed inefficacious for G- strains and fungus. Similar results were also observed in oxacillin-treated groups. Therefore, Omi-hyd-Dex@HA NPs retained the broad-spectrum antimicrobial activity of omiganan." REF00291 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 64 nM . . . Lung adenocarcinoma A-549 cell . REF100454 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 64 uM . . . Invasive breast carcinoma MCF-7 cell . REF102228 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 64.12 uM . . . Invasive breast carcinoma MCF-7 cell . REF101566 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 640 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100044 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) = 649 uM . . . Erythroleukemia HEL cell . REF102142 DRG00012 Paclitaxel 90% Lethal Concentration (IC50) = 65 ng/mL . . . Colon adenocarcinoma Caco-2 cell . REF100483 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 65 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102013 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 65 nM . . . Acute myeloid leukemia HL-60 cell . REF100798 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 65.3 uM . . . Acute myeloid leukemia HL-60 cell . REF102116 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 65.4 ug/mL . . . Normal MT4 cell . REF102239 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 65.6 nM . . . Mouse reticulum cell sarcoma J774 cell . REF101932 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 65.8 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100679 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 650 nM . . . Osteosarcoma U2OS cell . REF101268 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 650 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101206 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 650 nM . . . Invasive breast carcinoma MCF-7 cell . REF100648 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 650 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100291 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 650 nM . . . Normal Vero cell . REF101382 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 650 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100838 DRG00019 Methotrexate Half Maximal Effective Dosage (ED50) = 655 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100218 DRG00081 Cytarabine Half Maximal Effective Concentration (EC50) = 657.2 nM . . . Acute myeloid leukemia HL-60 cell . REF100762 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 66 nM . . . Renal adenocarcinoma ACHN cell . REF101481 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 66 nM . . . Mouse colon adenocarcinoma MC-38 cell . REF100210 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 66 nM . . . Lymphoma P388 cell . REF100156 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 66 nM . . . Colon cancer HT29 cell . REF100156 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) = 66 ug/mL . . . Malignant neoplasms of the mouse mammary gland FM3A cell . REF100014 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 66.22 uM . . . Plasma cell myeloma U-266 cell . REF102402 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 66.3 ng/mL . . . Renal carcinoma A498 cell . REF100220 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 660 nM . . . Prostate carcinoma DU145 cell . REF100786 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 660 nM . . . Normal L929 cell . REF101776 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 660 nM . . . Lung adenocarcinoma A-549 cell . REF100995 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 660 nM . . . Invasive breast carcinoma MCF-7 cell . REF101128 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 67 nM . . . Acute myeloid leukemia HL-60 cell . REF100775 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 67 nM . . . Lung adenocarcinoma A-549 cell . REF100306 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 67.2 uM . . . Acute myeloid leukemia HL-60 cell . REF102409 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 67.45 uM . . . Colon cancer HT29 cell . REF101566 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 67.61 uM . . . Non-small cell lung carcinoma HOP-62 cell . REF101566 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 67.76 uM . . . Minimally invasive lung adenocarcinoma NCI-H322M cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 670 nM . . . Invasive breast carcinoma MCF-7 cell . REF101517 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 670 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF100838 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 68 nM . . . Leukemia P388/S cell . REF100169 DRG00224 Pemetrexed Half Maximal Inhibitory Concentration (IC50) = 68 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101603 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 68.8 nM . . . Invasive breast carcinoma MCF-7 cell . REF101027 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 680 nM . . . Acute monocytic leukemia U-937 cell . REF100522 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 680 nM . . . Hepatoblastoma Hep-G2 cell . REF101602 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 680 nM . . . Colon cancer HT29 cell . REF101367 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 680 nM . . . Amelanotic melanoma A-375 cell . REF101923 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 680 nM . . . Acute monocytic leukemia MV4-11 cell . REF100449 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 69 nM . . . Lung adenocarcinoma A-549 cell . REF100921 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 69 nM . . . Lymphoblastic leukemia L1210 cell . REF100166 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 69.07 uM . . . Lung adenocarcinoma A-549 cell . REF102426 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 69.3±23.5 nM 24 h . . Lung adenocarcinoma A-549 cell "The anti-proliferative effect of the GnRH-III conjugates 1 and 2, as well as free Dau, was tested on wide range of cancer cell lines from different origin and also on MRC-5 (human fibroblast) as non-cancerous control cell line. The data showed that both conjugates possess an anti-proliferative effect on all cell types (Table 1). Except for the ovarian cancer cell lines A2780 and OVCAR-8, conjugate 2 displayed higher anti-proliferative activity than conjugate 1, depending on the type of cancer cells. The lowest activity was measured on PANC-1 pancreatic cancer cells, whereby a high IC50 value was also obtained on MRC-5 cells, showing selectivity of the conjugates for cancer cell lines. The obtained IC50 values of the conjugates vary mostly in the low micromolar range and were one to two order of magnitude higher when compared to free Dau that can enter cells non-specifically by passive diffusion. Moreover, the relative potency was calculated as a ratio of conjugates IC50 and free Daus IC50 in order to show the potency of the conjugates independently from the cell line, due to different activity of free Dau. A lower value of relative potency indicates that the conjugates IC50 value is closer to the free Daus IC50 value, which implies that the targeting capacity of the conjugate as well as its anti-tumor effect is stronger on a particular cell line, as compared to a cell line with higher relative potency. The BC cell lines showed good response to the conjugates by IC50 values, as well as by relative potency. Besides, the conjugates showed high anti-proliferative activity on mice CRC cell line C26, while the conjugates showed a moderate anti-proliferative activity on HT-29 human colon adenocarcinoma, but the relative potency was in the same range as for the BC cells." REF00075 DRG00005 Primaquine Half Maximal Inhibitory Concentration (IC50) = 69.7 uM . . . Colon cancer HT29 cell . REF102198 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 690 nM . . . Colon cancer HT29 cell . REF100156 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 690 nM . . . Endocervical adenocarcinoma HeLa cell . REF101749 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 690 nM . . . Normal NIH3T3 cell . REF100969 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 690 nM . . . Gastric carcinoma SNU-638 cell . REF100428 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 690 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF101963 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 690 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF102285 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 693.1 nM . . . Hepatoblastoma Hep-G2 cell . REF101643 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 699 nM . . . Normal WI-38 VA13 cell . REF100497 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 7 ng/ml . . . Colon cancer HT29 cell . REF100241 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 7 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101683 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF101086 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Lymphoma P388 cell . REF100377 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Cervical epithelial carcinoma KB 3-1 cell . REF101960 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 7 nM . . . Lung adenocarcinoma A-549 cell . REF100726 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100503 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100454 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Breast adenocarcinoma MDA-MB-468 cell . REF100413 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Invasive breast carcinoma T-47D cell . REF100413 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Prostate carcinoma PC-3 cell . REF101636 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Lung adenocarcinoma A-549 cell . REF101611 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Hepatoblastoma Hep-G2 cell . REF101033 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Colon cancer HT29 cell . REF100919 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 7 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100862 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF100619 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Stomach adenocarcinoma BGC-823 cell . REF100611 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Invasive breast carcinoma MCF-7 cell . REF100598 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 7 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100448 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 7 nM . . . Endocervical adenocarcinoma HeLa cell . REF100289 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Lymphoblastic leukemia L1210 cell . REF100967 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Thymoma EL4 cell . REF100967 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Colon carcinoma HCT 116 cell . REF102390 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 7 nM . . . Minimally invasive lung adenocarcinoma NCI-H322M cell . REF102315 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 7 nM . . . Glioblastoma SNB-75 cell . REF102290 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 7 nM . . . Lung squamous cell carcinoma NCI-H520 cell . REF102105 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102101 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 7 nM . . . Chronic myeloid leukemia K562 cell . REF101695 DRG00162 Curcumin Half Maximal Effective Dosage (ED50) = 7 ug/mL . . . Lung papillary adenocarcinoma PC-12 cell . REF100079 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7 uM . . . Invasive breast carcinoma MCF-7 cell . REF101041 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.01 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101960 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 7.03 nM . . . Lung adenocarcinoma A-549 cell . REF101531 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.1 nM . . . Invasive breast carcinoma MCF-7 cell . REF100576 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 7.1 nM . . . Lung adenocarcinoma A-549 cell . REF101301 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 7.1 ug/mL . . . Anaplastic thyroid carcinoma SW-1736 cell . REF100058 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.1 uM . . . Lung adenocarcinoma A-549 cell . REF102461 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.1 uM . . . Hepatoblastoma Hep-G2 cell . REF101042 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.1 uM . . . Renal cell carcinom 769-P cell . REF100854 DRG00065 Irinotecan Half Maximal Growth Inhibition (GI50) = 7.1 uM . . . Colon carcinoma HCT 116 cell . REF101092 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.12 uM . . . Invasive breast carcinoma MCF-7 cell . REF102368 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 7.16 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF101566 DRG00038 Monomethyl auristatin E Half Maximal Inhibitory Concentration (IC50) = 7.18 nM 72 h . . Gastric carcinoma HGC-27 cell "We next evaluated the in vitro cytotoxicity of 1131-MMAE. NUGC-4, MKN45 and HGC27 cells were drug-treated for 72 h and their viability was assessed. 1131-MMAE killed KK-LC-1 positive gastric cancer cells with high potency. The IC50 values of 1131-MMAE were 3.87 nM for NUGC-4 cells and 5.26 nM for MKN45 cells. However, although a very high concentration was used, 1131-MMAE could only moderately inhibit the viability of KK-LC-1 negative HGC27 cells. The IC50 value of 1131-MMAE for HGC27 cells was 100200 times higher than that in NUGC-4 and MNK45 cells. Free MMAE exerted cytotoxicity irrespective of the KK-LC-1 expression status. The IC50 values of free MMAE were 10.97 nM for NUGC-4 cells, 10.70 nM for MKN45 cells and 7.18 nM for HGC27 cells. Naked 1131 peptide showed no cytotoxicity to all three cell lines. These results were consistent with the KK-LC-1-dependent endocytosis and confirmed the target-selective killing of 1131-MMAE." REF00226 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 7.2 ng/mL . . . Invasive breast carcinoma MCF-7 cell . REF100109 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.2 nM . . . Acute myeloid leukemia HL-60 cell . REF101921 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.2 nM . . . Lung adenocarcinoma A-549 cell . REF101106 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.2 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100729 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.2 nM . . . Melanoma SK-MEL-2 cell . REF100505 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 7.2 nM . . . Acute myeloid leukemia HL-60 cell . REF101853 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 7.2 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101875 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.2 ug/mL . . . Lung large cell carcinoma NCI-H460 cell . REF102279 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.2 uM . . . Colon cancer HT29 cell . REF102384 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.2 uM . . . Invasive breast carcinoma MCF-7 cell . REF101990 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.2 uM . . . Endocervical adenocarcinoma HeLa cell . REF101933 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.2 uM . . . Normal HEK293 cell . REF101436 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.2 uM . . . Amelanotic melanoma A-375 cell . REF101283 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.22 uM . . . Neuroblastoma SK-N-SH cell . REF101761 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 7.24436 uM . . . Non-small cell lung carcinoma NCI-H522 cell . REF102227 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 7.25 uM . . . Lung adenocarcinoma A-549 cell . REF101050 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 7.28 uM . . . Non-small cell lung carcinoma NCI-H522 cell . REF102268 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.3 nM . . . Invasive breast carcinoma MCF-7 cell . REF101521 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 7.3 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101654 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.3 uM . . . Colon cancer HT29 cell . REF102289 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.3 uM . . . Hepatoblastoma Hep-G2 cell . REF101797 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.32 nM . . . Invasive breast carcinoma MCF-7 cell . REF101386 DRG00011 Doxorubicin 90% Lethal Concentration (IC50) = 7.32 ug/mL . . . Colon carcinoma HCT 116 cell . REF100820 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.36 uM . . . Hepatoma Bel-7402 cell . REF102476 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.36 uM . . . Hepatoblastoma Hep-G2 cell . REF101146 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.38 uM . . . Colon adenocarcinoma DLD-1 cell . REF102117 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 7.4 nM . . . Rat sarcoma YOSHIDA cell . REF101944 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.4 uM . . . Normal Vero cell . REF100818 DRG00162 Curcumin Half Maximal Cytotoxicity Concentration (CC50) = 7.4 uM . . . Normal MT4 cell . REF100269 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 7.42 uM . . . Invasive breast carcinoma MCF-7 cell . REF100788 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.47 uM . . . Lung adenocarcinoma A-549 cell . REF101210 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.5 nM . . . Ovarian endometrioid adenocarcinoma A2780S cell . REF101883 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 7.5 nM . . . Squamous carcinoma SCC-25 cell . REF100165 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.5 ug/mL . . . Normal Vero cell . REF101100 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.5 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101761 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.5 uM . . . Breast adenocarcinoma MDA-MB-468 cell . REF101761 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 7.51 uM . . . Endocervical adenocarcinoma HeLa cell . REF101375 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.52 nM . . . Invasive breast carcinoma MCF-7 cell . REF101662 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.52 uM . . . Gastric cancer MGC-803 cell . REF102394 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.53 nM . . . Gastric tubular adenocarcinoma NCI-N87 cell . REF101255 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 7.6 nM . . . Hepatoma SK-HEP1 cell . REF102292 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.6 nM . . . Melanoma B16 cell . REF100286 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 7.6 nM . . . Lung adenocarcinoma A-549 cell . REF101191 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.6 uM . . . Colon adenocarcinoma LoVo cell . REF100200 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.61 uM . . . Invasive breast carcinoma MCF-7 cell . REF102359 DRG00107 Betulinic acid Half Maximal Effective Dosage (ED50) = 7.62 ug/mL . . . Melanoma SK-MEL-2 cell . REF102108 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 7.68 uM . . . Astrocytoma SF268 cell . REF100815 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.7 nM . . . Endocervical adenocarcinoma HeLa cell . REF100886 DRG00003 Fluorouracil Half Maximal Effective Dosage (ED50) = 7.7 uM . . . Colon cancer HT29 cell . REF102309 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.8 ng/mL . . . Colon adenocarcinoma Caco-2 cell . REF100603 DRG00221 Acyclovir Minimum Inhibitory Concentration (MIC) = 7.8 ug/mL . . . Normal Vero cell . REF100046 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 7.8 uM . . . Normal MT4 cell . REF102038 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 7.88 uM . . . Lung adenocarcinoma A-549 cell . REF100642 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 7.9 ng/ml . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100234 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.9 nM . . . Rat sarcoma YOSHIDA cell . REF101944 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 7.9 nM . . . Normal COLO205 cell . REF101860 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.9 nM . . . Normal GES1 cell . REF101819 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 7.9 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF101624 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.9 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100759 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 7.94 nM . . . Lung adenocarcinoma NCI-H1975 cell . REF101255 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 7.94 uM . . . Colon adenocarcinoma KM12 cell . REF102320 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 7.94 uM . . . Normal HEK293 cell . REF101089 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 7.943 nM . . . Renal carcinoma RXF 393 cell . REF100274 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 7.94328 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 7.94328 uM . . . Lung large cell carcinoma NCI-H460 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 7.94328 uM . . . Prostate carcinoma PC-3 cell . REF100756 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 7.94328 uM . . . Renal adenocarcinoma ACHN cell . REF100756 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 7.981 uM . . . Renal carcinoma A498 cell . REF102400 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 7.99 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101546 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 70 ng/mL . . . Colon adenocarcinoma WiDr cell . REF100670 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 70 ng/mL . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100491 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 70 ng/mL . . . Invasive breast carcinoma MCF-7 cell . REF101378 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 70 ng/mL . . . Colon cancer HT29 cell . REF100889 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 70 ng/mL . . . Hepatoma SK-HEP1 cell . REF100613 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 70 ng/mL . . . Glioma XF498 cell . REF100529 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Invasive breast carcinoma T-47D cell . REF101680 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Astrocytoma SF268 cell . REF101091 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Invasive breast carcinoma MCF-7 cell . REF100940 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100291 DRG00010 Daunorubicin Half Maximal Growth Inhibition (GI50) = 70 nM . . . Colon cancer HT29 cell . REF102204 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Colon cancer HT29 cell . REF101994 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 70 nM . . . Colon carcinoma HCT 116 cell . REF101929 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 70 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101657 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 70 nM . . . Glioblastoma SNB-75 cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 70 nM . . . Melanoma LOX IMVI cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 70 nM . . . Renal cell carcinoma SN12C cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 70 nM . . . Invasive breast carcinoma MCF-7 cell . REF101510 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101472 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Colon carcinoma HCT 116 cell . REF100872 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 70 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100822 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Endocervical adenocarcinoma HeLa cell . REF100687 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Gastric carcinoma SNU-638 cell . REF100617 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Invasive breast carcinoma MCF-7 cell . REF100545 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Melanoma SK-MEL-2 cell . REF100531 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100708 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Lymphoma P388 cell . REF100708 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 70 nM . . . Acute monocytic leukemia U-937 cell . REF102392 DRG00019 Methotrexate Half Maximal Growth Inhibition (GI50) = 70 nM . . . Colon cancer HT29 cell . REF100434 DRG00296 Zidovudine Half Maximal Effective Dosage (ED50) = 70 nM . . . Normal MT-2 cell . REF102034 DRG00101 Vidarabine Minimum Inhibitory Concentration (MIC) = 70 ug/mL . . . Normal Vero cell . REF100015 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 70.3 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF100639 DRG00012 Paclitaxel 90% Growth Inhibition (GI90) = 70.6 ng/mL . . . Lung adenocarcinoma A-549 cell . REF101352 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 700 nM . . . Lung adenocarcinoma A-549 cell . REF101511 DRG00011 Doxorubicin Half Maximal Cytotoxicity Concentration (CC50) = 700 nM . . . Acute monocytic leukemia THP-1 cell . REF102499 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 700 nM . . . Prostate carcinoma LNCaP cell . REF102095 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 700 nM . . . Lung adenocarcinoma A-549 cell . REF101988 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 700 nM . . . Renal adenocarcinoma ACHN cell . REF101925 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 700 nM . . . Hepatoblastoma Hep-G2 cell . REF101671 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 700 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101523 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 700 nM . . . Normal COLO205 cell . REF101205 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 700 nM . . . Chronic myeloid leukemia K562 cell . REF101155 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 700 nM . . . Colon cancer HT29 cell . REF100292 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 700 nM . . . Invasive breast carcinoma of no special type UACC-812 cell . REF100763 DRG00221 Acyclovir 90% Lethal Concentration (IC50) = 700 nM . . . Normal MRC5 cell . REF100018 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 700 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102220 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 700 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100760 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 71 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100768 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 71 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100338 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 71 nM . . . Acute monocytic leukemia THP-1 cell . REF101045 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 71 nM . . . Endocervical adenocarcinoma HeLa cell . REF101522 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 71 nM . . . Breast carcinoma MX1 cell . REF102306 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 71.8 uM . . . Invasive breast carcinoma MCF-7 cell . REF100852 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 710 nM . . . Endocervical adenocarcinoma HeLa cell . REF101010 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 711 nM . . . Chronic myeloid leukemia K562 cell . REF101579 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 718 nM . . . Chronic myeloid leukemia K562 cell . REF100967 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 72 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100960 DRG00014 Baicalin Half Maximal Inhibitory Concentration (IC50) = 72 uM . . . Sezary syndrome H9 cell . REF102043 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 72.44 uM . . . Renal cell carcinoma SN12C cell . REF101165 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 720 nM . . . Lung adenocarcinoma A-549 cell . REF100727 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 720 nM . . . Acute myeloid leukemia HL-60 cell . REF100621 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 720 nM . . . Normal R1 cell . REF100206 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 720 nM . . . Colon cancer HT29 cell . REF102432 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 73 ng/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100338 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 73 nM . . . Endocervical adenocarcinoma HeLa cell . REF101266 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 730 nM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF101735 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 730 nM . . . Hepatocellular carcinoma SMMC-7721 cell . REF101652 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 730 nM . . . Prostate carcinoma PC-3 cell . REF100746 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) = 733 uM . . . Erythroleukemia HEL cell . REF100118 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 740 nM . . . Melanoma UACC-257 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 740 nM . . . Hepatoblastoma Hep-G2 cell . REF101272 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 740 nM . . . Melanoma UACC-62 cell . REF101165 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 740 nM . . . Invasive breast carcinoma MCF-7 cell . REF100579 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 740 nM . . . Lung adenocarcinoma A-549 cell . REF101963 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 75 nM . . . Colon adenocarcinoma DLD-1 cell . REF102118 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 75 uM . . . Normal MT4 cell . REF100080 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 75.9 nM . . . Prostate carcinoma TRAMP-C1A cell . REF100412 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 750 nM . . . Normal HEK-293T cell . REF101351 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 750 nM . . . Amelanotic melanoma A-375 cell . REF101142 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 750 nM . . . Invasive breast carcinoma MCF-7 cell . REF100872 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 750 nM . . . Glioblastoma SF-295 cell . REF100770 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 759.39 nM . . . Lung adenocarcinoma A549/TR cell . REF101634 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 76 nM . . . Uterine corpus leiomyosarcoma SK-UT-1 cell . REF101137 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 760 nM . . . Colon adenocarcinoma HCT 15 cell . REF100786 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 760 nM . . . Lung adenocarcinoma A-549 cell . REF101434 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 760 nM . . . Chronic myeloid leukemia LAMA-84 cell . REF100737 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 77 nM . . . Prostate carcinoma PC-3 cell . REF100559 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 77 nM . . . Pancreas adenocarcinoma DAN-G cell . REF100710 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 77.3 nM . . . Glioblastoma SNB-75 cell . REF100197 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 77.6 nM . . . Prostate carcinoma LNCaP cell . REF100879 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 770 nM . . . Endocervical adenocarcinoma HeLa cell . REF100642 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 770 nM . . . Prostate carcinoma PC-3 cell . REF101835 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 770 nM . . . Colon adenocarcinoma SW620 cell . REF101747 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 770 nM . . . Hepatoblastoma Hep-G2 cell . REF101282 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 78 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF100725 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 78 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100319 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 78 nM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100270 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 78.9 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101729 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 79 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100521 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 79 nM . . . Non-small cell lung carcinoma EKVX cell . REF101624 DRG00081 Cytarabine Half Maximal Infective Dose (ID50) = 79 ug/mL . . . Lymphoma L5178Y cell . REF100031 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 79.4 nM . . . Mouse reticulum cell sarcoma J774 cell . REF101932 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 79.4 pM . . . Colon carcinoma HCT 116 cell . REF102468 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 79.4 uM . . . Astrocytoma SNB-19 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 79.4 uM . . . Colon cancer HT29 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 79.4 uM . . . Cutaneous melanoma SK-MEL-28 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 79.4 uM . . . Melanoma LOX IMVI cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 79.4 uM . . . Ovarian serous adenocarcinoma OVCAR-5 cell . REF102249 DRG00406 Monastrol Half Maximal Growth Inhibition (GI50) = 79.4 uM . . . Renal adenocarcinoma ACHN cell . REF102249 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 79.43 nM . . . Invasive breast carcinoma MCF-7 cell . REF100123 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 79.43 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF102222 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 79.43 uM . . . Colon cancer HT29 cell . REF100902 DRG00012 Paclitaxel Half Maximal Lethal Concentration (IC50) = 79.43 uM . . . Colon cancer HT29 cell . REF100902 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 79.43282 uM . . . Colon adenocarcinoma SW620 cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 79.43282 uM . . . Leukemia SR cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 79.43282 uM . . . Melanoma Malme-3M cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 79.43282 uM . . . Minimally invasive lung adenocarcinoma NCI-H322M cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 79.43282 uM . . . Non-small cell lung carcinoma EKVX cell . REF102222 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 79.43282 uM . . . Renal carcinoma RXF 393 cell . REF102222 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 790 nM . . . Melanoma UACC-257 cell . REF100270 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 794 nM . . . Prostate carcinoma DU145 cell . REF100587 DRG00107 Betulinic acid Half Maximal Growth Inhibition (GI50) = 794.33 nM . . . Non-small cell lung carcinoma HOP-62 cell . REF100756 DRG00407 Combretastatin A4 Tumor Growth Inhibition value (TGI) = 794.33 nM . . . Colon adenocarcinoma KM12 cell . REF102222 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 794.33 nM . . . Glioblastoma SNB-75 cell . REF102222 DRG00019 Methotrexate Half Maximal Infective Dose (ID50) = 8 mM . . . Malignant neoplasms of the mouse mammary gland TA3 cell . REF100027 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8 ng/mL . . . Breast ductal carcinoma BT-549 cell . REF100239 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8 ng/mL . . . Normal HEK293 cell . REF101267 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8 ng/mL . . . Endocervical adenocarcinoma HeLa cell . REF101195 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8 ng/mL . . . Invasive breast carcinoma MCF-7 cell . REF100603 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8 ng/mL . . . Colon carcinoma HCT 116 cell . REF100600 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Lung adenocarcinoma A-549 cell . REF101045 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 8 nM . . . Colon adenocarcinoma LoVo cell . REF100926 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Acute monocytic leukemia THP-1 cell . REF100870 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100347 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Colon adenocarcinoma LoVo cell . REF100340 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Colon cancer HT29 cell . REF101686 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Endocervical adenocarcinoma HeLa cell . REF101277 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 8 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100987 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 8 nM . . . Lung adenocarcinoma A-549 cell . REF100862 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Hepatocellular carcinoma Huh-7 cell . REF100754 DRG00012 Paclitaxel 90% Lethal Concentration (IC50) = 8 nM . . . Colon carcinoma HCT 116 cell . REF100505 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Breast ductal carcinoma BT-549 cell . REF100967 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Pancreatic ductal adenocarcinoma Capan-1 cell . REF101812 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Gastric adenocarcinoma MKN45 cell . REF100327 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Prostate carcinoma PC-3 cell . REF101502 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 8 nM . . . Endocervical adenocarcinoma HeLa cell . REF102362 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 8 nM . . . Glioblastoma SNB-75 cell . REF102315 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102306 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101811 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 8 nM . . . Pancreatic ductal adenocarcinoma MIA PaCa-2 cell . REF100116 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8 uM . . . Lung large cell carcinoma NCI-H460 cell . REF101041 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8 uM . . . Endocervical adenocarcinoma HeLa cell . REF101069 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 8 uM . . . Invasive breast carcinoma MCF-7 cell . REF100561 DRG00162 Curcumin Half Maximal Growth Inhibition (GI50) = 8 uM . . . Colon adenocarcinoma DLD-1 cell . REF102208 DRG00043 JH-VII-139-1 Half Maximal growth inhibition concentration (GI50) = 8±0.2 µM . . . Endocervical adenocarcinoma HeLa cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00043 JH-VII-139-1 Half Maximal growth inhibition concentration (GI50) = 8±0.5 µM . . . Chronic myeloid leukemia K562 cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00043 JH-VII-139-1 Half Maximal Inhibitory Concentration (IC50) = 8±0.6 µM 48 h . . Invasive breast carcinoma MCF-7 cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.1 mM . . . Hepatoblastoma Hep-G2 cell . REF100575 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 8.1 nM . . . Acute myeloid leukemia HL-60 cell . REF100213 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8.1 uM . . . Colon adenocarcinoma SW480 cell . REF102141 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.1 uM . . . Endocervical adenocarcinoma HeLa cell . REF102517 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 8.1 uM . . . Normal 184B5 cell . REF101657 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.1 uM . . . Hepatoblastoma Hep-G2 cell . REF100562 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 8.11 uM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF100822 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.14 uM . . . Endocervical adenocarcinoma WISH cell . REF101672 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 8.14 uM . . . Lung adenocarcinoma A-549 cell . REF101375 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 8.15 uM . . . Cutaneous melanoma SK-MEL-5 cell . REF101566 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 8.18 nM . . . Lung adenocarcinoma A-549 cell . REF101119 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.19 uM . . . Prostate carcinoma DU145 cell . REF101210 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.2 nM . . . Lung squamous cell carcinoma NCI-H520 cell . REF101549 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.2 nM . . . Lung adenocarcinoma A-549 cell . REF101124 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 8.2 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100450 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 8.2 uM . . . Pancreatic ductal adenocarcinoma BxPC-3 cell . REF102277 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.2 uM . . . Lymphoma P388/ADR cell . REF100170 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.2 uM . . . Invasive breast carcinoma MCF-7 cell . REF100576 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8.28 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102283 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.3 uM . . . Endocervical adenocarcinoma HeLa cell . REF101543 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.3 uM . . . Invasive breast carcinoma MCF-7 cell . REF100716 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 8.3 uM . . . Lung adenocarcinoma A-549 cell . REF101559 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 8.31 uM . . . Lung adenocarcinoma A-549 cell . REF101546 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8.32 uM . . . Colon adenocarcinoma KM12 cell . REF102236 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.37 nM . . . Invasive breast carcinoma MCF-7 cell . REF101662 DRG00003 Fluorouracil Tumor Growth Inhibition value (TGI) = 8.4 nM . . . Pancreatic ductal adenocarcinoma BxPC-3 cell . REF102292 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.4 nM . . . Invasive breast carcinoma MCF-7 cell . REF101705 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.4 nM . . . Gastric carcinoma HGC-27 cell . REF101819 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 8.4 uM . . . Invasive breast carcinoma MCF-7 cell . REF101599 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.46 uM . . . Prostate carcinoma PC-3 cell . REF101082 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.49 uM . . . Neuroblastoma IMR-32 cell . REF101479 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.51 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101662 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8.51 uM . . . Colon carcinoma HCT 116 cell . REF102236 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.54 nM . . . Invasive breast carcinoma MCF-7 cell . REF101662 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.56 uM . . . Bone marrow neuroblastoma SH-SY5Y cell . REF100942 DRG00009 Camptothecin Half Maximal Effective Dosage (ED50) = 8.6 pmol/ml . . . Lymphoma P388 cell . REF102002 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.62 uM . . . Invasive breast carcinoma MCF-7 cell . REF101088 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 8.63 nM . . . Lung adenocarcinoma A-549 cell . REF101559 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.66 uM . . . Endocervical adenocarcinoma HeLa cell . REF101687 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 8.7 nM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF101740 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8.7 ug/mL . . . Gastric carcinoma SGC-7901 cell . REF102279 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.7 ug/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100486 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8.7 uM . . . Pancreatic adenocarcinoma PSN1 cell . REF102350 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.7 uM . . . Laryngeal carcinoma HEp-2 cell . REF101988 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.7 uM . . . Ileocecal adenocarcinoma HCT-8 cell . REF101443 DRG00221 Acyclovir Half Maximal Inhibitory Concentration (IC50) = 8.71 uM . . . Endocervical adenocarcinoma HeLa cell . REF100068 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.72 ug/mL . . . Endocervical adenocarcinoma HeLa cell . REF100784 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.76 nM . . . Lung adenocarcinoma A-549 cell . REF101662 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 8.8 nM . . . Colon carcinoma HCT 116 cell . REF102292 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.8 nM . . . Medulloblastoma Daoy cell . REF101751 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.8 nM . . . Invasive breast carcinoma MCF-7 cell . REF101588 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.8 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101478 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 8.8 nM . . . Osteosarcoma 143B cell . REF100222 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8.8 uM . . . Cecum adenocarcinoma NCI-H508 cell . REF102493 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 8.8 uM . . . Colon adenocarcinoma LoVo cell . REF100880 DRG00107 Betulinic acid Half Maximal Effective Concentration (EC50) = 8.8 uM . . . Endocervical adenocarcinoma HeLa cell . REF102361 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 8.81 uM . . . Colon cancer HT29 cell . REF100106 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.83 uM . . . Prostate carcinoma PC-3 cell . REF101171 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 8.87 nM . . . Prostate carcinoma PC-3 cell . REF100912 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 8.87 uM . . . Lung adenocarcinoma A-549 cell . REF101555 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.87 uM . . . Prostate carcinoma PC-3 cell . REF101897 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 8.87 uM . . . Colon adenocarcinoma HCT 15 cell . REF102389 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 8.9 nM . . . Amelanotic melanoma A-375 cell . REF101299 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 8.9 nM . . . Lymphoblastic leukemia L1210 cell . REF100145 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 8.9 nM . . . Acute myeloid leukemia HL-60 cell . REF101777 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8.9 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100065 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8.91 uM . . . Lung large cell carcinoma NCI-H1299 cell . REF101462 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.92 ug/mL . . . Invasive breast carcinoma BT-474 cell . REF100734 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 8.93 uM . . . Endocervical adenocarcinoma HeLa cell . REF101322 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 8.94 uM . . . Invasive breast carcinoma MCF-7 cell . REF100996 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 80 ng/mL . . . Lung adenocarcinoma A-549 cell . REF100529 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 80 ng/mL . . . Glioma XF498 cell . REF100342 DRG00296 Zidovudine Half Maximal Infective Dose (ID50) = 80 ng/mL . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100011 DRG00009 Camptothecin Half Maximal Cytotoxicity Concentration (CC50) = 80 nM . . . Invasive breast carcinoma MCF-7 cell . REF102288 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Invasive breast carcinoma T-47D cell . REF101362 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF101200 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 80 nM . . . Endocervical adenocarcinoma HeLa cell . REF100847 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Chronic myeloid leukemia K562 cell . REF100807 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Colon cancer HT29 cell . REF100306 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Prostate carcinoma PC-3 cell . REF101703 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 80 nM . . . Renal adenocarcinoma ACHN cell . REF101679 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Lung adenocarcinoma A-549 cell . REF101662 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 80 nM . . . Cutaneous melanoma SK-MEL-28 cell . REF101566 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 80 nM . . . Colon carcinoma HCT 116 cell . REF101480 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Colon carcinoma HCT 116 cell . REF101403 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Normal CHO cell . REF100969 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Lung small cell carcinoma NCI-H187 cell . REF100794 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Lymphoblastic leukemia L1210 cell . REF100477 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Colon adenocarcinoma LoVo cell . REF100340 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101716 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 80 nM . . . Lung large cell carcinoma NCI-H460 cell . REF101218 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100993 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Invasive breast carcinoma MCF-7 cell . REF100736 DRG00081 Cytarabine Half Maximal Growth Inhibition (GI50) = 80 nM . . . B acute lymphoblastic leukemia BALL-1 cell . REF102266 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Acute myeloid leukemia HL-60 cell . REF102107 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Lymphoblastic leukemia L1210 cell . REF100007 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100071 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 80 nM . . . Lung large cell carcinoma NCI-H460 cell . REF102414 DRG00012 Paclitaxel Half Maximal Growth Inhibition (GI50) = 80 uM . . . Lung adenocarcinoma A-549 cell . REF101946 DRG00107 Betulinic acid Half Maximal Cytotoxicity Concentration (CC50) = 80 uM . . . Normal HEK293 cell . REF101568 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Lung large cell carcinoma NCI-H1299 cell . REF101511 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Prostate carcinoma DU145 cell . REF101190 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Colon adenocarcinoma HCT 15 cell . REF100904 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Acute myeloid leukemia HL-60 cell . REF100745 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Endocervical adenocarcinoma HeLa cell . REF101773 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Lung adenocarcinoma A-549 cell . REF101286 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Prostate carcinoma DU145 cell . REF101263 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101220 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Normal WI-38 cell . REF101006 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Acute myeloid leukemia HL-60 cell . REF100961 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Astrocytoma SNB-19 cell . REF100946 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Acute monocytic leukemia U-937 cell . REF100891 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Ileocecal adenocarcinoma HCT-8 cell . REF100528 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Lung adenocarcinoma A-549 cell . REF101394 DRG00405 10-Hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 800 nM . . . Lung adenocarcinoma A-549 cell . REF102367 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 81 nM . . . Acute myeloid leukemia HL-60 cell . REF100853 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 810 nM . . . Amelanotic melanoma A-375 cell . REF100993 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 82 nM . . . Acute myeloid leukemia HL-60 cell . REF101144 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 82 nM . . . Colon adenocarcinoma HCT 15 cell . REF101098 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 82 nM . . . Lung adenocarcinoma A-549 cell . REF101253 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 82 nM . . . Gastric adenocarcinoma MKN45 cell . REF102115 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 82 uM . . . Astrocytoma U-251MG cell . REF102277 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 82.3 uM . . . Hepatoma Bel-7402 cell . REF100651 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 82.6 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF102127 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 820 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101662 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 820 nM . . . Colon adenocarcinoma HCT 15 cell . REF100804 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 820 nM . . . Hepatoblastoma Hep-G2 cell . REF100648 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 820 nM . . . Melanoma M14 cell . REF100640 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 820 nM . . . Hepatoblastoma Hep-G2 cell . REF100597 DRG00221 Acyclovir Half Maximal Cytotoxicity Concentration (CC50) = 820 ug/mL . . . Normal Vero cell . REF102065 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 83 nM . . . Colon carcinoma HCT 116 cell . REF101092 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 830 nM . . . Lymphoma P388 cell . REF101922 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 830 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100925 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 830 nM . . . Lymphoma P388 cell . REF100268 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 830 nM . . . Gastric cancer MGC-803 cell . REF101435 DRG00012 Paclitaxel 90% Lethal Concentration (IC50) = 832 nM . . . Prostate carcinoma PC-3 cell . REF100505 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 84 nM . . . Hepatoma H22 cell . REF101810 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 84 nM . . . Invasive breast carcinoma MCF-7 cell . REF101907 DRG00407 Combretastatin A4 Half Maximal Growth Inhibition (GI50) = 84.1 nM . . . Lung adenocarcinoma A-549 cell . REF101340 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 84.23 uM . . . Prostate carcinoma PC-3 cell . REF101862 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 84.28 uM . . . Lung adenocarcinoma A549/TR cell . REF102480 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 84.33 uM . . . Ovarian serous adenocarcinoma OVCAR-3 cell . REF101165 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 84.9 uM . . . Colon carcinoma HCT 116 cell . REF102363 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 840 nM . . . Lung adenocarcinoma A-549 cell . REF101952 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 840 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101374 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 840 nM . . . Hepatoma Bel-7402 cell . REF102185 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 85 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101266 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 85 nM . . . Normal MT4 cell . REF100038 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 85 uM . . . Hepatoblastoma Hep-G2 cell . REF101941 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 85.3 uM . . . Lung adenocarcinoma A-549 cell . REF100456 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 85.7 uM . . . Invasive breast carcinoma Hs 578T cell . REF101165 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 850 nM . . . Colon cancer HT29 cell . REF100798 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 850 nM . . . Cervical carcinoma L02 cell . REF101620 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 850 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101343 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 850 nM . . . Endocervical adenocarcinoma HeLa cell . REF101170 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 850 nM . . . Invasive breast carcinoma MCF-7 cell . REF100877 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 850 nM . . . Gastric cancer MGC-803 cell . REF101065 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 854 uM . . . Lung adenocarcinoma A-549 cell . REF101827 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 86.1 nM . . . Prostate carcinoma LNCaP cell . REF100354 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 86.7 uM . . . Renal carcinoma TK-10 cell . REF101165 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 86.87 uM . . . Hepatoblastoma Hep-G2 cell . REF101215 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 860 nM . . . Endocervical adenocarcinoma HeLa cell . REF100798 DRG00010 Daunorubicin Half Maximal Lethal Concentration (IC50) = 860 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102204 DRG00010 Daunorubicin Half Maximal Growth Inhibition (GI50) = 860 nM . . . Invasive breast carcinoma MCF-7 cell . REF100836 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 860 nM . . . Lung adenocarcinoma A-549 cell . REF100639 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 860 nM . . . Breast carcinoma MCF7R cell . REF100272 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 87 nM . . . Cutaneous melanoma SK-MEL-5 cell . REF100270 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 87 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100071 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 87 uM . . . T acute lymphoblastic leukemia Jurkat cell . REF102228 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 87.1 uM . . . Prostate carcinoma PC-3 cell . REF101566 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 87.2 nM . . . Colon cancer HT29 cell . REF101213 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 87.5 nM . . . Invasive breast carcinoma MCF-7 cell . REF101477 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 87.5 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101759 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 870 nM . . . Colon cancer HT29 cell . REF101463 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 870 nM . . . Lung adenocarcinoma A-549 cell . REF101272 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 870 nM . . . Small cell lung carcinoma NCI-H69 cell . REF100137 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 870 nM . . . Normal COLO205 cell . REF100270 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 88 nM . . . Bladder carcinoma T24 cell . REF100306 DRG00018 7-Ethyl-10-hydroxycamptothecin Half Maximal Inhibitory Concentration (IC50) = 88 nM . . . Lung adenocarcinoma A-549 cell . REF100742 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 880 nM . . . Normal MRC5 cell . REF100950 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 880 nM . . . Endocervical adenocarcinoma HeLa cell . REF101317 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 880 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101272 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 880 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100903 DRG00045 Duocarmycin Sa Half Maximal Inhibitory Concentration (IC50) = 89 nM 72 h . . Normal 16HBE14o- cell "All cell lines demonstrated sensitivity toward the DSA-PABA payload 5 in the nanomolar range. The cleaved peptide 6, and the benzyl protected control peptide 4, had no appreciable effect on cell proliferation (>100 µM), suggesting that any observed cytotoxic activity is due to the DSA warhead. Interestingly, PDC 7, without the cathepsin B cleavable sequence, also had no appreciable effect on cell proliferation (>100 µM), despite possessing the active DSA DNA alkylating moiety. Perhaps this PDC is either not being taken up into cells or not being broken down by proteases and peptidases in the cell. In both cases, the warhead may not be reaching the nucleus, the site of action of the duocarmycins. Cell lines that demonstrated appreciable levels of TFα were sensitive to PDC 3. Interestingly, HCT116, which had relatively high TFα expression and cathepsin B activity, demonstrated the greatest sensitivity to PDC 3, approaching similar potency to the payload 5. Excitingly, A549, H292, and 16HBE14o, which showed no detectable TFα expression, appeared unaffected by PDC 3 up to 100 µM, suggesting that TFα expression is required for the efficacy of PDC 3." REF00117 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 89 nM . . . Acute myeloid leukemia HL-60 cell . REF100719 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 89.06 uM . . . Gastric adenocarcinoma MKN45 cell . REF100689 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 89.7 ng/ml . . . Invasive breast carcinoma MCF-7 cell . REF101935 DRG00012 Paclitaxel Tumor Growth Inhibition value (TGI) = 89.9 nM . . . Gliosarcoma SF539 cell . REF100197 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 89.9 uM . . . Chronic myeloid leukemia K562 cell . REF102215 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 89.95 uM . . . Renal carcinoma TK-10 cell . REF101566 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 890 nM . . . Normal MRC5 cell . REF100950 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 890 nM . . . Bone marrow neuroblastoma SH-SY5Y cell . REF101621 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 890 nM . . . Invasive breast carcinoma MCF-7 cell . REF101425 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 890 nM . . . Endocervical adenocarcinoma HeLa cell . REF101065 DRG00224 Pemetrexed Half Maximal Inhibitory Concentration (IC50) = 894 nM . . . Normal R2 cell . REF101262 DRG00001 Brimonidine Duration of lower intraocular pressure = 8h . . Dutch Belted rabbits (23kg) model. . . "The HR97-brimonidine conjugate provided up to 18 days of IOP lowering with a single ICM injection in normotensive rabbits, which contrasts with the 8h-effect provided by a brimonidine eye drop." REF00263 DRG00045 Duocarmycin Sa Half Maximal Inhibitory Concentration (IC50) = 9 nM 72 h . . Lung mucoepidermoid carcinoma H292 cell "All cell lines demonstrated sensitivity toward the DSA-PABA payload 5 in the nanomolar range. The cleaved peptide 6, and the benzyl protected control peptide 4, had no appreciable effect on cell proliferation (>100 µM), suggesting that any observed cytotoxic activity is due to the DSA warhead. Interestingly, PDC 7, without the cathepsin B cleavable sequence, also had no appreciable effect on cell proliferation (>100 µM), despite possessing the active DSA DNA alkylating moiety. Perhaps this PDC is either not being taken up into cells or not being broken down by proteases and peptidases in the cell. In both cases, the warhead may not be reaching the nucleus, the site of action of the duocarmycins. Cell lines that demonstrated appreciable levels of TFα were sensitive to PDC 3. Interestingly, HCT116, which had relatively high TFα expression and cathepsin B activity, demonstrated the greatest sensitivity to PDC 3, approaching similar potency to the payload 5. Excitingly, A549, H292, and 16HBE14o, which showed no detectable TFα expression, appeared unaffected by PDC 3 up to 100 µM, suggesting that TFα expression is required for the efficacy of PDC 3." REF00117 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 9 nM . . . Colon carcinoma HCT 116 cell . REF101807 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 9 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100399 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 9 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102425 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 9 nM . . . Amelanotic melanoma A-375 cell . REF101856 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9 nM . . . Invasive breast carcinoma ZR-75-1 cell . REF100305 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9 nM . . . Hepatoblastoma Hep-G2 cell . REF101293 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9 nM . . . Mammary gland malignant neoplasms EMT6 cell . REF100256 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 9 nM . . . Lung small cell carcinoma DMS-53 cell . REF102287 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 9 nM . . . Lymphoblastic leukemia L1210 cell . REF100213 DRG00059 Sunitinib Half Maximal Inhibitory Concentration (IC50) = 9 nM . . . Acute monocytic leukemia MV4-11 cell . REF102226 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 9 nM . . . Prostate carcinoma LNCaP cell . REF100917 DRG00296 Zidovudine Half Maximal Effective Concentration (EC50) = 9 nM . . . Endocervical adenocarcinoma HeLa cell . REF102062 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 9 nM . . . Lung adenocarcinoma A-549 cell . REF101695 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9 uM . . . Invasive breast carcinoma MCF-7 cell . REF101069 DRG00043 JH-VII-139-1 Half Maximal growth inhibition concentration (GI50) = 9±0.2 µM . . . Invasive breast carcinoma MCF-7 cell "The cytotoxic activity of JH-VII-139-1 and JH-VII-139-1-c(RGDyK) hybrid compounds was evaluated at different concentrations (0.550 µM) over a panel of cell lines including HeLa cervical cancer, MCF7 mammary carcinoma, the triple-negative breast cancer MDA-MB-231 and K562 lymphoblast cells. Integrin receptors are highly overexpressed on the surface of many types of cancer. The metastatic breast cancer cell lines MDA-MB-435 and MCF-7, as well as HeLa cells, express high levels of αVβ3 integrins. On the other hand, K562 cells express very low levels of αVβ3 integrins. The cytotoxic and cytostatic activities of the JH-VII-139-1-c(RGDyK) hybrid compounds were estimated by three concentration-dependent parameters: GI50 (concentration that results in 50% growth inhibition), TGI (concentration that results in total growth inhibition or cytostatic effect), and IC50 (concentration that results in 50% growth cytotoxic effect). JH-VII-139-1 and the hybrid compounds, geo75 and geo77, showed a significant cytostatic (GI50 = 412 µM) and cytotoxic (IC50 = 318 µM) effect against HeLa, MCF-7, MDA-MB-231 and K562 cancer cells. The most active compound was geo77, showing IC50 and GI50 values of 3 µM and 4 µM, respectively in the most sensitive cell line MCF-7. Geo85 exhibited a slightly cytostatic effect (GI50 = 33 µM), with a minor cytotoxicity (IC50 = 45 µM) only against MCF-7 cells." REF00253 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9.1 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101732 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9.1 nM . . . Endocervical adenocarcinoma HeLa cell . REF101176 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9.1 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF100358 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 9.1 uM . . . Acute myeloid leukemia HL-60 cell . REF102234 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 9.12 uM . . . Colon carcinoma HCT 116 cell . REF102389 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 9.17 uM . . . Invasive breast carcinoma T-47D cell . REF101089 DRG00065 Irinotecan Half Maximal Growth Inhibition (GI50) = 9.17 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101017 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 9.19 uM . . . Lung adenocarcinoma A-549 cell . REF100642 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 9.2 ng/ml . . . Lung adenocarcinoma A-549 cell . REF100187 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9.2 nM . . . Skin squamous cell carcinoma A431 cell . REF100938 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 9.2 nM . . . Uterine sarcoma MES-SA/Dx5 cell . REF100345 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 9.2 nM . . . Normal Vero cell . REF100222 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9.265 uM . . . Lung adenocarcinoma A-549 cell . REF100977 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 9.29 uM . . . Prostate carcinoma DU145 cell . REF101089 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 9.3 nM . . . Prostate carcinoma DU145 cell . REF102131 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 9.3 nM . . . T-lymphoblastic leukemia MOLT-3 cell . REF100099 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 9.3 ug/mL . . . Hepatoblastoma Hep-G2 cell . REF102279 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9.3 uM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF100969 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 9.37 uM . . . Prostate carcinoma DU145 cell . REF102277 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9.4 uM . . . Lung large cell carcinoma NCI-H460 cell . REF100964 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9.49 uM . . . Hepatoblastoma Hep-G2 cell . REF100497 DRG00010 Daunorubicin Half Maximal Infective Dose (ID50) = 9.5 ng/ml . . . Lymphoma P388 cell . REF100020 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9.5 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100418 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 9.5 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100222 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 9.5 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102101 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 9.5 uM . . . Lung adenocarcinoma A-549 cell . REF101241 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 9.55 uM . . . Colon adenocarcinoma Caco-2 cell . REF100988 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 9.56 uM . . . Acute monocytic leukemia U-937 cell . REF102402 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 9.57 uM . . . Amelanotic melanoma MDA-MB-435 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9.58 uM . . . Prostate carcinoma PC-3 cell . REF101659 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9.6 ng/mL . . . Lymphoma P388 cell . REF100271 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9.6 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100319 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9.6 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF100250 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 9.6 uM . . . Breast adenocarcinoma MDA-MB-231 cell . REF102284 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 9.66 ng/ml . . . Colon cancer HT29 cell . REF100264 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9.7 nM . . . Uterine sarcoma MES-SA cell . REF100501 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 9.7 nM . . . Colon carcinoma HCT 116 cell . REF102166 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 9.7 nM . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF101123 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 9.7 uM . . . Chronic myeloid leukemia K562 cell . REF100918 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9.7 uM . . . Colon adenocarcinoma LoVo cell . REF100349 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 9.7 uM . . . Colon carcinoma HCT 116 cell . REF101836 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 9.71 uM . . . Colon adenocarcinoma HCT 15 cell . REF102272 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 9.74 ug/mL . . . Invasive breast carcinoma MCF-7 cell . REF101738 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9.74 uM . . . Colon carcinoma HCT 116 cell . REF101509 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 9.77 uM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF102365 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 9.77237 uM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF100123 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 9.8 nM . . . Colon carcinoma RKO cell . REF102390 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 9.8 uM . . . Prostate carcinoma PC-3 cell . REF101351 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9.8 uM . . . Cervical carcinoma KB-V1 cell . REF101526 DRG00130 "Coumarine, 7-Methoxy-2-oxo-2H-1-benzopyran-3-carboxylic acid" Half Maximal Effective Concentration (EC50) = 9.8 uM . . . Cervical squamous cell carcinoma SiHa cell . REF102308 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 9.9 nM . . . Pancreatic ductal adenocarcinoma PANC-1 cell . REF100682 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 9.9 nM . . . Colon adenocarcinoma HCT 15 cell . REF102166 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 9.9 uM . . . Colon carcinoma HCT 116 cell . REF102277 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 9.9 uM . . . Invasive breast carcinoma MCF-7 cell . REF102277 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 9.92 uM . . . Colon adenocarcinoma HCT 15 cell . REF101089 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 90 ng/mL . . . Hepatoblastoma Hep-G2 cell . REF101947 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 ng/mL . . . Melanoma SK-MEL-2 cell . REF100960 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 90 ng/mL . . . Melanoma UACC-62 cell . REF100889 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 ng/mL . . . Gingival squamous cell carcinoma Ca9-22 cell . REF100657 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 ng/mL . . . Glioma XF498 cell . REF100469 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 90 ng/mL . . . Ovarian serous cystadenocarcinoma SK-OV-3 cell . REF100405 DRG00011 Doxorubicin Half Maximal Effective Dosage (ED50) = 90 ng/mL . . . Colon adenocarcinoma HCT 15 cell . REF100404 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 ng/mL . . . Lymphoma P388 cell . REF100279 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 ng/mL . . . Lymphoblastic leukemia L1210 cell . REF100252 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Endocervical adenocarcinoma HeLa cell . REF101454 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Colon carcinoma HCT 116 cell . REF101339 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Colon cancer HT29 cell . REF100650 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 90 nM . . . Prostate carcinoma PC-3 cell . REF100622 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Prostate carcinoma DU145 cell . REF102265 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF101939 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 90 nM . . . Astrocytoma SF268 cell . REF101917 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 90 nM . . . Prostate carcinoma PC-3 cell . REF101906 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Lung adenocarcinoma A-549 cell . REF101894 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 90 nM . . . Lung adenocarcinoma NCI-H23 cell . REF101551 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101496 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 90 nM . . . Colon adenocarcinoma SW620 cell . REF101480 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 90 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101182 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . T acute lymphoblastic leukemia Jurkat cell . REF100534 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Melanoma G-361 cell . REF100506 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Colon cancer HT29 cell . REF100430 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Astrocytoma U-251MG cell . REF100359 DRG00012 Paclitaxel Half Maximal Effective Dosage (ED50) = 90 nM . . . Mouse reticulum cell sarcoma J774 cell . REF101920 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Colon adenocarcinoma DLD-1 cell . REF100500 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 90 nM . . . Cervical squamous cell carcinoma SiHa cell . REF101568 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 90 pM . . . Lymphoblastic leukemia L1210 cell . REF100368 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 90 uM . . . Normal COLO205 cell . REF102228 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 90 uM . . . Lung adenocarcinoma A-549 cell . REF101845 DRG00013 Gemcitabine Half Maximal Inhibitory Concentration (IC50) = 90.7 nM . . . Osteosarcoma U2OS cell . REF102166 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Invasive breast carcinoma MCF-7 cell . REF101389 DRG00011 Doxorubicin Half Maximal Effective Concentration (EC50) = 900 nM . . . Lung adenocarcinoma A-549 cell . REF102139 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Lymphoblastic leukemia L1210 cell . REF101925 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Lung adenocarcinoma A-549 cell . REF101901 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101635 DRG00011 Doxorubicin Tumor Growth Inhibition value (TGI) = 900 nM . . . Colon cancer HT29 cell . REF101567 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Hepatoblastoma Hep-G2 cell . REF101535 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Invasive breast carcinoma MCF-7 cell . REF101475 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Endocervical adenocarcinoma HeLa cell . REF101273 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Acute myeloid leukemia HL-60 cell . REF101142 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Stomach adenocarcinoma BGC-823 cell . REF101085 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101040 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Hepatoma Bel-7402 cell . REF100878 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Gastric carcinoma SGC-7901 cell . REF100748 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101849 DRG00019 Methotrexate Half Maximal Effective Concentration (EC50) = 900 nM . . . Invasive breast carcinoma MCF-7 cell . REF100850 DRG00059 Sunitinib Half Maximal Effective Concentration (EC50) = 900 nM . . . Invasive breast carcinoma BT-474 cell . REF102459 DRG00065 Irinotecan Half Maximal Inhibitory Concentration (IC50) = 900 nM . . . Invasive breast carcinoma MCF-7 cell . REF101389 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 91 nM . . . Lung adenocarcinoma A-549 cell . REF100991 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 91 uM . . . Colon adenocarcinoma LoVo cell . REF100290 DRG00008 Dexamethasone Half Maximal Cytotoxicity Concentration (CC50) = 91.1 uM . . . Mouse reticulum cell sarcoma J774 cell . REF101616 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 91.2 nM . . . Astrocytoma SF268 cell . REF100589 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 910 nM . . . Breast adenocarcinoma MDA-MB-231 cell . REF101361 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 910 nM . . . Human papillomavirus-related endocervical adenocarcinoma KB cell . REF101296 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 912 nM . . . Prostate carcinoma PC-3 cell . REF100814 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 92 nM . . . Lung adenocarcinoma A-549 cell . REF101816 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 92 nM . . . Colon cancer HT29 cell . REF100882 DRG00011 Doxorubicin Half Maximal Lethal Concentration (IC50) = 92.68 uM . . . Colon adenocarcinoma KM12 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 920 nM . . . Acute myeloid leukemia HL-60 cell . REF101496 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 920 nM . . . Normal Vero cell . REF101325 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 93 nM . . . Astrocytoma SF268 cell . REF100604 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 93.33 nM . . . Ovarian endometrioid adenocarcinoma A2780 cell . REF100596 DRG00296 Zidovudine Half Maximal Cytotoxicity Concentration (CC50) = 93.55 uM . . . Normal MT4 cell . REF100846 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 930 nM . . . Chronic myeloid leukemia K562 cell . REF101510 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 930 nM . . . Colon cancer HT29 cell . REF101357 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 930 nM . . . Acute monocytic leukemia U-937 cell . REF100946 DRG00012 Paclitaxel Half Maximal Inhibitory Concentration (IC50) = 930 nM . . . Hepatoma Bel-7402 cell . REF100631 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 933.25 nM . . . Colon adenocarcinoma SW620 cell . REF100123 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 94 nM . . . Astrocytoma SF268 cell . REF100731 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 94 nM . . . Lung large cell carcinoma NCI-H460 cell . REF100585 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 94 nM . . . Melanoma UACC-62 cell . REF100577 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 94 nM . . . Colon cancer HT29 cell . REF101014 DRG00407 Combretastatin A4 Half Maximal Inhibitory Concentration (IC50) = 94.3 nM . . . Lung adenocarcinoma A-549 cell . REF102427 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 940 nM . . . Normal WI-38 cell . REF101572 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 940 nM . . . Endocervical adenocarcinoma HeLa cell . REF100816 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 940 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101547 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 940 nM . . . Chronic myeloid leukemia K562 cell . REF101431 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 95.6 nM . . . Colon adenocarcinoma LoVo cell . REF101244 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 950 nM . . . Prostate carcinoma DU145 cell . REF101250 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 950 nM . . . Clear cell renal cell carcinoma Caki-1 cell . REF101566 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 950 nM . . . Prostate carcinoma DU145 cell . REF101362 DRG00011 Doxorubicin Half Maximal Growth Inhibition (GI50) = 950 nM . . . Prostate carcinoma DU145 cell . REF101335 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 950 nM . . . Lung adenocarcinoma A-549 cell . REF100980 DRG00020 Docetaxel Half Maximal Inhibitory Concentration (IC50) = 950 nM . . . Pancreatic ductal adenocarcinoma Capan-1 cell . REF101710 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 950 nM . . . Endocervical adenocarcinoma HeLa cell . REF102422 DRG00122 Vinblastine Half Maximal Inhibitory Concentration (IC50) = 96 nM . . . High grade ovarian serous adenocarcinoma NCI-ADR-RES cell . REF102435 DRG00296 Zidovudine Half Maximal Inhibitory Concentration (IC50) = 96 uM . . . Acute myeloid leukemia HL-60 cell . REF102011 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 96.37 uM . . . High grade ovarian serous adenocarcinoma OVCAR-8 cell . REF102166 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 960 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF101008 DRG00081 Cytarabine Half Maximal Inhibitory Concentration (IC50) = 97 ng/mL . . . Lymphoblastic leukemia L1210 cell . REF102028 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 97 nM . . . Melanoma SK-MEL-2 cell . REF100512 DRG00107 Betulinic acid Half Maximal Inhibitory Concentration (IC50) = 97.51 uM . . . Lung adenocarcinoma A-549 cell . REF102133 DRG00003 Fluorouracil Half Maximal Inhibitory Concentration (IC50) = 970 nM . . . Lymphoblastic leukemia L1210 cell . REF102232 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 970 nM . . . Lung adenocarcinoma A-549 cell . REF100594 DRG00010 Daunorubicin Half Maximal Inhibitory Concentration (IC50) = 977 nM . . . Amelanotic melanoma MDA-MB-435 cell . REF100521 DRG00003 Fluorouracil Half Maximal Growth Inhibition (GI50) = 977.24 nM . . . Melanoma M14 cell . REF100123 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 98 nM . . . Gastric carcinoma SNU-638 cell . REF100899 DRG00012 Paclitaxel Half Maximal Effective Concentration (EC50) = 98 nM . . . Lung large cell carcinoma NCI-H1299 cell . REF100740 DRG00011 Doxorubicin Half Maximal Inhibitory Concentration (IC50) = 98.32 uM . . . Invasive breast carcinoma Hs 578T cell . REF101043 DRG00009 Camptothecin Half Maximal Inhibitory Concentration (IC50) = 980 nM . . . Normal CNE-2 cell . REF101670 DRG00019 Methotrexate Half Maximal Inhibitory Concentration (IC50) = 980 nM . . . Ovarian serous adenocarcinoma OVCAR-5 cell . REF100270 DRG00009 Camptothecin Half Maximal Growth Inhibition (GI50) = 99 nM . . . Lung adenocarcinoma A-549 cell . REF101736 DRG00081 Cytarabine Half Maximal Growth Inhibition (GI50) = 99.8 nM . . . T acute lymphoblastic leukemia CCRF-CEM cell . REF102094