Peptide-drug Conjugate Information
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)
|
|||||
| 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
| 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
