Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00002
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| PDC Name |
(123B9)2L2PTX
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
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| Structure |
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| Peptide Name |
123B9
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Peptide Info | ||||
| Receptor Name |
Ephrin type-A receptor 2 (EPHA2)
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Receptor Info | ||||
| Drug Name |
Paclitaxel
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Drug Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Antitriazole
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Linker Info | ||||
| Peptide Modified Type |
The modification of binding with chemical macromolecules
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| Modified Segment |
Lys-Gly-Lys-Gly
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| Ternimal Modification |
N-terminal modification
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| Formula |
C195H262Cl2F2N34O63
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 4199.318 | ||||
| Lipid-water partition coefficient (xlogp) | -6.7164 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 42 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 63 | |||||
| Rotatable Bond Count (rotbonds) | 123 | |||||
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 | Breast cancer | ||||
| Efficacy Data | Number of Lung metastases nodules |
5
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| Administration Time | 2 weeks | ||||
| Administration Dosage | 24.5 mg/kg | ||||
| Description |
We observed the clear and significant (p < 0.0001) beneficial effects of the dimer drug on lung metastasis (Figure5A,B), with a reduction of the gross lung-metastasis count by more than 75% compared with those in the control and Abraxane groups.
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| In Vivo Model | BALB/c mice syngeneic breast-cancer metastasis model. | ||||
References
