Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00145
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| PDC Name |
E1-7 doxorubicin
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Medulloblastoma
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| Structure |
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| Peptide Name |
E1-7
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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 |
Glutaric acid
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Linker Info | ||||
| Formula |
C62H85N13O22
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 1364.431 | ||||
| Lipid-water partition coefficient (xlogp) | -3.8227 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 17 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 24 | |||||
| Rotatable Bond Count (rotbonds) | 35 | |||||
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 | Medulloblastoma | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
130 ± 1.27 nM
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| Administration Time | 72 h | ||||
| Description |
This was confirmed with E1-7 doxorubicin conjugate (4) displaying a 5-fold reduction in cytotoxicity compared to E1-3 doxorubicin conjugate (3) (IC50 values of 130 ± 1.27 nM and 25 ± 1.22 nM, respectively) and 14-fold reduction in cytotoxicity compared to free doxorubicin (5) (IC50 values of 130 ± 1.27 nM and 8.8 ± 1.31 nM, respectively) (Figure 7).
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| In Vitro Model | Medulloblastoma | Medulloblastoma cell | Homo sapiens | ||
References