Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00054
|
|||||
|---|---|---|---|---|---|---|
| PDC Name |
ABD-RPARPAR-DOXO
|
|||||
| PDC Status |
Investigative
|
|||||
| Indication |
In total 1 Indication(s)
Tumor
|
|||||
| Structure |
|
|||||
| Peptide Name |
ABD-RPARPAR
|
Peptide Info | ||||
| Drug Name |
Doxorubicin
|
Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 2-alpha (TOP2A)
|
Target Info | ||||
| Linker Name |
(6-maleimidocaproyl) hydrazone derivative
|
Linker Info | ||||
| Peptide Modified Type |
The modification of binding with chemical macromolecules
|
|||||
| Modified Segment |
ABD
|
|||||
| Ternimal Modification |
N-terminal modification
|
|||||
| Formula |
C350H562N100O108S2
|
|||||
| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 7963.072 | ||||
| Lipid-water partition coefficient (xlogp) | -36.9415 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 110 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 118 | |||||
| Rotatable Bond Count (rotbonds) | 275 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Obtained from the Model Organism Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Retarded the tumor growth rate |
47.09%
|
|||
| Administration Time | 20 days | ||||
| Administration Dosage | 3.0 mg/kg doxorubicin equivalent | ||||
| Description |
The doxorubicin, DOXO-EMCH, ABD-RGDK-DOXO, and ABD-RPARPAR-DOXO retarded the tumor growth rate by 24.28, 25.67, 47.78, and 47.09% on day 20, respectively.
|
||||
| In Vivo Model | Tumor-bearing BALB/c nude mice. | ||||
| Half life period | 23.88 ± 0.94 h | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
11.21 ± 4.54 µM
|
|||
| Evaluation Method | CCK-8 assay | ||||
| Description |
Whereas conjugation of a peptide would hinder the passive diffusion route, resulting in higher IC50 values for the peptide-DOX-conjugates (9.27 ± 3.56 uM for ABD-RGDK-DOXO and 11.21 ± 4.54 uM for ABD-RPARPAR-DOXO, respectively).
|
||||
| In Vitro Model | Lung adenocarcinoma | A-549 cell | CVCL_0023 | ||
| Half life period | 23.88 ± 0.94 h | ||||
References