Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00138
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| PDC Name |
DOXKGFRWR
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Hepatocellular carcinoma
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| Structure |
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| Peptide Name |
KGFRWR
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Peptide Info | ||||
| Drug Name |
Doxorubicin
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Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 2-alpha (TOP2A)
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Target Info | ||||
| Linker Name |
Succinic Acid
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Linker Info | ||||
| Peptide Modified Type |
Modification by dosage
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| Modified Segment |
Self-assemble
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| Formula |
C86H101N15O22
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| #Ro5 Violations (Lipinski): 4 | Molecular Weight | 1696.837 | ||||
| Lipid-water partition coefficient (xlogp) | 1.3467 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 19 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 23 | |||||
| Rotatable Bond Count (rotbonds) | 40 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Obtained from the Model Organism Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
5.27 µM
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| Description |
The IC50 values for KGFRWR, DOX, and DOX-KGFRWR against the MMP2 enzyme were 14.19, 8.68, and 5.27 10-6 m, respectively.
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| In Vivo Model | SMMC7721 pulmonary metastatic mouse model. | ||||
| Half life period | 24.52±13.17 h | ||||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Percent survival |
50%
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| Administration Time | 40 days | ||||
| Description |
DOX-KGFRWR has significantly prolonged survival rates.
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| In Vivo Model | SMMC7721 tumorbearing mice. | ||||
| Half life period | 24.52±13.17 h | ||||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Percent survival | > 40 days | |||
| Administration Time | 30 days | ||||
| Description |
DOX-KGFRWR has significantly prolonged survival rates.
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| In Vivo Model | SMMC7721 tumorbearing mice. | ||||
| Half life period | 24.52±13.17 h | ||||
| Experiment 4 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
78.51%
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| Description |
The antitumor efficacy of the DOX-KGFRWR nanofiber was superior to all other treatments, with a final tumor volume of 376 mm3.
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| In Vivo Model | SMMC7721 tumorbearing mice. | ||||
| Half life period | 24.52±13.17 h | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
34.55 µg mL-1
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| Evaluation Method | MTT assay | ||||
| Description |
The IC50 values for DOX-KGFRWR is 34.55 μg mL-1.
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| In Vitro Model | Hepatocellular carcinoma | SMMC-7721 cell | CVCL_0534 | ||
| Half life period | 24.52±13.17 h | ||||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Hepatocellular carcinoma | ||||
| Efficacy Data | Migration rates |
19.90%
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| Description |
Cells treated with DOX and DOX-KGFRWR exhibited markedly decreased migration, with migration rates of 39.4% and 19.9%, respectively, compared with those in the control, indicating that DOX-KGWRFR exerted a stronger inhibiting effect on migration than DOX.
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| In Vitro Model | Hepatocellular carcinoma | SMMC-7721 cell | CVCL_0534 | ||
| Half life period | 24.52±13.17 h | ||||
References