Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00359
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| PDC Name |
TH1904
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| PDC Status |
Preclinical
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| Indication |
In total 1 Indication(s)
Ovarian cancer
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| Structure |
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| Peptide Name |
TH19P01
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Peptide Info | ||||
| Receptor Name |
Sortilin (SORT1)
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Receptor 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 |
3,3-Dimethylglutaric acid
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Linker Info | ||||
| Formula |
C153H212N28O51
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 3259.524 | ||||
| Lipid-water partition coefficient (xlogp) | -6.5223 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 39 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 53 | |||||
| Rotatable Bond Count (rotbonds) | 91 | |||||
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 | Ovarian cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
54 nM
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| Administration Time | 12 h | ||||
| MOA of PDC |
Overall, these results indicate that both conjugates alter cell migration in either TNBC or ovarian cancer cell models through a SORT1-dependent mechanism. The effects of TH1902 and TH1904 on cell migration further support the molecular rationale that inhibition of VM activity may result, in part, from the reduction of cancer cell invasive phenotype.
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| Description |
TH1904 IC50 value was 54 nM for the number of loops inhibition (Figure 5B).
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| In Vitro Model | Ovarian clear cell adenocarcinoma | ES-2 cell | CVCL_3509 | ||
References