Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00096
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| PDC Name |
CRB-FFE-YSV
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Tumor
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| Structure |
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| Peptide Name |
YSV
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Peptide Info | ||||
| Drug Name |
Chlorambucil
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Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 2-alpha (TOP2A)
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Target Info | ||||
| Linker Name |
FFE
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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 |
C54H67Cl2N7O12
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| #Ro5 Violations (Lipinski): 4 | Molecular Weight | 1077.073 | ||||
| Lipid-water partition coefficient (xlogp) | 3.2335 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 10 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 11 | |||||
| Rotatable Bond Count (rotbonds) | 34 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Relative tumor volume of mice |
356%
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| Administration Time | Day 1, day 4, day 7, and day 10 | ||||
| Administration Dosage | 10 µmol/kg | ||||
| Description |
After treatment for 28 days, the final relative tumor volume of mice treated with PBS, YSV, CRB, YSV + CRB, or CRB-FFE-YSV hydrogel was 927, 728, 491, 514, and 356%, respectively.
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| In Vivo Model | HepG2-tumor-bearing BALB/c nude mice. | ||||
| In Vitro Model | Hepatoblastoma | L-O2 cell line | CVCL_0027 | ||
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) |
25.7 µM
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| Administration Time | 48 h | ||||
| Evaluation Method | MTT assay | ||||
| Description |
The corresponding IC50 values of CRB-FFE-YSV nanofibers against HepG2, MCF-7, and BEL-7402 cells were 28.9, 47.5, and 25.7 um, respectively, which were much lower than that of free YSV (842.9, 999.5, and 719.2 um), free CRB (154.4, 214.6, and 192.5 um), and the mixed drugs (150.0, 190.3, and 180.6 um).
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| In Vitro Model | Hepatoma | Bel-7402 cell | CVCL_5492 | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
28.9 µM
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| Administration Time | 48 h | ||||
| Evaluation Method | MTT assay | ||||
| Description |
The corresponding IC50 values of CRB-FFE-YSV nanofibers against HepG2, MCF-7, and BEL-7402 cells were 28.9, 47.5, and 25.7 um, respectively, which were much lower than that of free YSV (842.9, 999.5, and 719.2 um), free CRB (154.4, 214.6, and 192.5 um), and the mixed drugs (150.0, 190.3, and 180.6 um).
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| In Vitro Model | Hepatoblastoma | Hep-G2 cell | CVCL_0027 | ||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
47.5 µM
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| Administration Time | 48 h | ||||
| Evaluation Method | MTT assay | ||||
| Description |
The corresponding IC50 values of CRB-FFE-YSV nanofibers against HepG2, MCF-7, and BEL-7402 cells were 28.9, 47.5, and 25.7 um, respectively, which were much lower than that of free YSV (842.9, 999.5, and 719.2 um), free CRB (154.4, 214.6, and 192.5 um), and the mixed drugs (150.0, 190.3, and 180.6 um).
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cell | CVCL_0031 | ||
References