General Information of This Peptide-drug Conjugate (PDC)
PDC ID
PDC_00146
PDC Name
EETI-2.5Z-amide -gemcitabine
PDC Status
Investigative
Indication
In total 1 Indication(s)
Glioblastoma
Structure
Peptide Name
EETI-2.5Z
 Peptide Info 
Receptor Name
Integrin
 Receptor Info 
Drug Name
Gemcitabine
 Drug Info 
Therapeutic Target
Ribonucleoside-diphosphate reductase subunit M2 (RRM2)
 Target Info 
Linker Name
Alkyne-Triazole
 Linker Info 
Peptide Modified Type
Amino acid modifications; Cyclization modification
Modified Segment
Cyclization modification
Formula
C148H220F2N48O50S6
#Ro5 Violations (Lipinski): 5 Molecular Weight 3702.072
Lipid-water partition coefficient (xlogp) -20.1763
Hydrogen Bond Donor Count (hbonddonor) 44
Hydrogen Bond Acceptor Count (hbondacc) 60
Rotatable Bond Count (rotbonds) 46
Full List of Activity Data of This Peptide-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Glioblastoma
Efficacy Data Half Maximal Effective Concentration (EC50)
8.9 ± 1.2 nM
Evaluation Method CCK-8 assay
Description
Cell proliferation was quantified 4 d after treatment with each compoundusing CCK-8 colorimetric assays and compared to the untreated control.
In Vitro Model Glioblastoma U-87MG cell CVCL_0022
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Glioblastoma
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.8 ± 0.2 nM
Evaluation Method CCK-8 assay
Description
Cell proliferation was quantified 4 d after treatment with each compoundusing CCK-8 colorimetric assays and compared to the untreated control.
In Vitro Model Glioblastoma U-87MG cell CVCL_0022
References
Ref 1 Integrin-Targeting Knottin Peptide-Drug Conjugates Are Potent Inhibitors of Tumor Cell Proliferation. Angew Chem Int Ed Engl. 2016 Aug 16;55(34):9894-7. doi: 10.1002/anie.201603488. Epub 2016 Jun 15.