General Information of This Peptide-drug Conjugate (PDC)
PDC ID
PDC_00002
PDC Name
(123B9)2L2PTX
PDC Status
Investigative
Indication
In total 1 Indication(s)
Breast cancer
Structure
Peptide Name
123B9
 Peptide Info 
Receptor Name
Ephrin type-A receptor 2 (EPHA2)
 Receptor Info 
Drug Name
Paclitaxel
 Drug Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Antitriazole
 Linker Info 
Peptide Modified Type
The modification of binding with chemical macromolecules
Modified Segment
Lys-Gly-Lys-Gly
Ternimal Modification
N-terminal modification
Formula
C195H262Cl2F2N34O63
#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
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Breast cancer
Efficacy Data Number of Lung metastases nodules
5
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.
In Vivo Model BALB/c mice syngeneic breast-cancer metastasis model.
References
Ref 1 Reduction of Circulating Cancer Cells and Metastases in Breast-Cancer Models by a Potent EphA2-Agonistic Peptide-Drug Conjugate. J Med Chem. 2018 Mar 8;61(5):2052-2061. doi: 10.1021/acs.jmedchem.7b01837. Epub 2018 Feb 27.