ChemicalBook--->CAS DataBase List--->1681017-83-3

1681017-83-3

1681017-83-3 Structure

1681017-83-3 Structure
IdentificationBack Directory
[Name]

Venadaparib
[CAS]

1681017-83-3
[Synonyms]

IDX-1197
NOV140101
Venadaparib
IDX-1197/Venadaparib
Venadaparib(IDX-1197)
inhibit,PARP,Venadaparib,IDX1197,Inhibitor,solid,IDX 1197,tumors,anticancer,poly ADP ribose polymerase
1(2H)-Phthalazinone, 4-[[3-[[3-[(cyclopropylamino)methyl]-1-azetidinyl]carbonyl]-4-fluorophenyl]methyl]-
[Molecular Formula]

C23H23FN4O2
[MDL Number]

MFCD34470861
[MOL File]

1681017-83-3.mol
[Molecular Weight]

406.45
Chemical PropertiesBack Directory
[density ]

1.43±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : 100 mg/mL (246.03 mM; Need ultrasonic)
[form ]

Solid
[pka]

12.06±0.40(Predicted)
[color ]

White to yellow
Hazard InformationBack Directory
[Uses]

Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research[1][2].
[in vivo]

In the germline BRCA1-mutated ovarian cancer PDX model, oral administration of Venadaparib (IDX-1197) exhibits significant PAR inhibition (>90%) in tumor tissues until 24 hr post dose. Venadaparib also dose-dependently led to potent tumor growth inhibition compared to Olaparib treatment group[1].

[IC 50]

PARP1: 1.4 nM (IC50); PARP2: 1 nM (IC50)
[References]

[1] Myongjae Lee, et al. Abstract A106: Development of IDX-1197, a novel, selective, and highly potent PARP inhibitor. American Association for Cancer Research, 2018.
[2] Yong Man Kim, et al. First-in-human dose-finding study of venadaparib (IDX-1197), a potent and selective PARP inhibitor, in patients with advanced solid tumors. Journal of Clinical Oncology. 39, no. 15_suppl (May 20, 2021) 3107-3107.
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