Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00209
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| PDC Name |
HCPTMDP26-PEG
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Breast cancer
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| Structure |
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| Peptide Name |
MDP26
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Peptide Info | ||||
| Drug Name |
Hydroxycamptothecin
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Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
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Target Info | ||||
| Linker Name |
Glycylglycylglycine
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Linker Info | ||||
| Peptide Modified Type |
Amino acid modifications
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| Ternimal Modification |
N-terminal modification
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| Formula |
C158H265N33O50
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 3427.039 | ||||
| Lipid-water partition coefficient (xlogp) | -6.619 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 33 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 55 | |||||
| Rotatable Bond Count (rotbonds) | 145 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Breast cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.27 µM
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| Description |
Peptides and drug-peptide conjugates were incubated with HepG2 cells for 48 hours followed by a CCK8 cytotoxicity assay. Despite the large population of the positive charges, supramolecular peptides alone demonstrated negligible cytotoxicity (Fig. S8, ESI). The drug conjugate, HCPT-MDP26-PEG showed a dose-dependent cytotoxicity with an IC50of 1.27 uM, comparable to the IC50of free HCPT at ˜1.3 uM (Fig. 3a). At a high drug dosage, the drug conjugate is much more potent than free HCPT.
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| In Vitro Model | Hepatoblastoma | L-O2 cell line | CVCL_0027 | ||
References