Peptide Information
General Information of This Peptide
| Peptide ID |
PEP00127
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|---|---|---|---|---|---|---|
| Peptide Name |
c(RPQfK)
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| Structure |
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| Sequence |
RPQFK
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| Peptide Type |
Cyclic
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| Receptor Name |
Integrin alpha-V; Integrin beta-3 (ITGAV; ITGB3)
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Receptor Info | ||||
| PDC Transmembrane Types | Cell targeting peptides (CTPs) | |||||
| Formula |
C30H45N9O7
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| Isosmiles |
[H]N/C(N)=N/CCC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)C2CCCN2C1=O
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| InChI |
InChI=1S/C30H45N9O7/c31-13-5-4-10-19-25(42)36-20(11-6-14-34-30(32)33)29(46)39-15-7-12-23(39)28(45)38-22(17-24(40)41)27(44)37-21(26(43)35-19)16-18-8-2-1-3-9-18/h1-3,8-9,19-23H,4-7,10-17,31H2,(H,35,43)(H,36,42)(H,37,44)(H,38,45)(H,40,41)(H4,32,33,34)/t19-,20-,21+,22-,23?/m0/s1
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| InChIKey |
ISXOIHSKTMJRON-DRSFHUHJSA-N
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| Pharmaceutical Properties |
Molecule Weight
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643.746
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Polar area
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264.43
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Complexity
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643.3441948
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xlogp Value
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-2.1698
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Heavy Count
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46
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Rot Bonds
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12
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Hbond acc
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8
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Hbond Donor
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8
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Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
cRPQ-SMCC-DM1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Tumer volume |
2400 mm3
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| Administration Time | Given every other day for a total of five times | ||||
| Administration Dosage | 400 µg/kg (calculated by free DM1) | ||||
| Description |
It was demonstrated here, RCCD@NPs and RSSD@NPs exhibited significantly better tumor-growth inhibition compared with that of the free DM1, QCCD@NPs or QSSD@NPs (Figure (Figure4A).4A). RSSD@NPs showed the most suppression on B16 tumor up to 25 days, and resulted in a tumor volume 4 times smaller than the saline group at the end of the experiment. The final tumor volumes in various nano-DDS groups ranked from the greatest to the least: QCCD@NPs, QSSD@NPs>DM1>RCCD@NPs>RSSD@NPs. Almost the same trends were found in terms of tumor weight and tumor size (Figures (Figures4B,4B, C).
Click to Show/Hide
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Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
67.61 ± 13.67 nM
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| Administration Time | 48 h | ||||
| Description |
The IC50 of QCCD@NPs and QSSD@NPs (389.05±75.25 nM and 245.47±37.54 nM) on B16 cells seemed much higher than the values of RCCD@NPs and RSSD@NPs (102.33±38.92 nM and 21.38±4.32 nM). The cytotoxicity of APDC@NPs on HUVEC showed a similar pattern.
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| In Vitro Model | Normal | Human umbilical vein endothelial cell | Homo sapiens | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
331.13 ± 85.56 nM
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| Administration Time | 48 h | ||||
| Description |
The IC50 of QCCD@NPs and QSSD@NPs (389.05±75.25 nM and 245.47±37.54 nM) on B16 cells seemed much higher than the values of RCCD@NPs and RSSD@NPs (102.33±38.92 nM and 21.38±4.32 nM). The cytotoxicity of APDC@NPs on HUVEC showed a similar pattern.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cell | CVCL_0031 | ||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
389.05 ± 75.25 nM
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| Administration Time | 48 h | ||||
| Description |
The IC50 of QCCD@NPs and QSSD@NPs (389.05±75.25 nM and 245.47±37.54 nM) on B16 cells seemed much higher than the values of RCCD@NPs and RSSD@NPs (102.33±38.92 nM and 21.38±4.32 nM). The cytotoxicity of APDC@NPs on HUVEC showed a similar pattern.
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| In Vitro Model | Melanoma | B16 cell | CVCL_F936 | ||
cRPQ-SS-DM1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Tumer volume |
5200 mm3
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| Administration Time | Given every other day for a total of five times | ||||
| Administration Dosage | 400 µg/kg (calculated by free DM1) | ||||
| Description |
It was demonstrated here, RCCD@NPs and RSSD@NPs exhibited significantly better tumor-growth inhibition compared with that of the free DM1, QCCD@NPs or QSSD@NPs (Figure (Figure4A).4A). RSSD@NPs showed the most suppression on B16 tumor up to 25 days, and resulted in a tumor volume 4 times smaller than the saline group at the end of the experiment. The final tumor volumes in various nano-DDS groups ranked from the greatest to the least: QCCD@NPs, QSSD@NPs>DM1>RCCD@NPs>RSSD@NPs. Almost the same trends were found in terms of tumor weight and tumor size (Figures (Figures4B,4B, C).
Click to Show/Hide
|
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Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
154.88 ± 31.85 nM
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| Administration Time | 48 h | ||||
| Description |
The IC50 of QCCD@NPs and QSSD@NPs (389.05±75.25 nM and 245.47±37.54 nM) on B16 cells seemed much higher than the values of RCCD@NPs and RSSD@NPs (102.33±38.92 nM and 21.38±4.32 nM). The cytotoxicity of APDC@NPs on HUVEC showed a similar pattern.
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| In Vitro Model | Normal | Human umbilical vein endothelial cell | Homo sapiens | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
245.47 ± 37.54 nM
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| Administration Time | 48 h | ||||
| Description |
The IC50 of QCCD@NPs and QSSD@NPs (389.05±75.25 nM and 245.47±37.54 nM) on B16 cells seemed much higher than the values of RCCD@NPs and RSSD@NPs (102.33±38.92 nM and 21.38±4.32 nM). The cytotoxicity of APDC@NPs on HUVEC showed a similar pattern.
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| In Vitro Model | Melanoma | B16 cell | CVCL_F936 | ||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
371.53 ± 94.49 nM
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| Administration Time | 48 h | ||||
| Description |
The IC50 of QCCD@NPs and QSSD@NPs (389.05±75.25 nM and 245.47±37.54 nM) on B16 cells seemed much higher than the values of RCCD@NPs and RSSD@NPs (102.33±38.92 nM and 21.38±4.32 nM). The cytotoxicity of APDC@NPs on HUVEC showed a similar pattern.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cell | CVCL_0031 | ||
References