General Information of This Peptide-drug Conjugate (PDC)
PDC ID
PDC_00236
PDC Name
M1-PTX
PDC Status
Investigative
Indication
In total 1 Indication(s)
Glioma
Structure
Peptide Name
M1
 Peptide Info 
Drug Name
Paclitaxel
 Drug Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Succinic Acid
 Linker Info 
Formula
C194H252N34O54
#Ro5 Violations (Lipinski): 4 Molecular Weight 3924.334
Lipid-water partition coefficient (xlogp) -1.9678
Hydrogen Bond Donor Count (hbonddonor) 36
Hydrogen Bond Acceptor Count (hbondacc) 57
Rotatable Bond Count (rotbonds) 99
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 Glioma
Efficacy Data Percent survival
0%
Administration Time 25 days
Administration Dosage Normalized to 17.3 mg/kg PTX
Description
The survival of the PTX group was markedly lower than that of the Vehicle group. M1-PTX did not improve survival, whereas the survival of the M1-RGD-PTX group was increased.
In Vivo Model U87MG-Luc-bearing xenograft model.
In Vitro Model Glioblastoma U87MG-Luc cell CVCL_5J15
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Glioma
Efficacy Data Cell viability
60%
Administration Time 24 h
Administration Dosage 100 nM
Evaluation Method MTS assay
Description
Both PDCs showed higher in vitro cytotoxicity than free PTX.
In Vitro Model Glioblastoma U-87MG cell CVCL_0022
References
Ref 1 Blood-Brain Barrier- and Blood-Brain Tumor Barrier-Penetrating Peptide-Derived Targeted Therapeutics for Glioma and Malignant Tumor Brain Metastases. ACS Appl Mater Interfaces. 2019 Nov 13;11(45):41889-41897. doi: 10.1021/acsami.9b14046. Epub 2019 Oct 29.