Venadaparib 是一种选择性和具有口服活性的PARP抑制剂，对PARP1和PARP2的IC50分别为 1.4 和 1.0 nM。它可防止 DNA 单链断裂 (SSB) 的修复，可研究实体瘤。

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 is insensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSBs) and can be used in solid tumor research.

Venadaparib significantly inhibits PARP1-mediated PAR expression with an EC50?of 0.5 nM In DNA damage-induced Hela cells[1].

Oral administration of Venadaparib significantly inhibits PAR(>90%) in tumor tissues until 24 hr post-dose in the germline BRCA1-mutated ovarian cancer PDX model. Venadaparib also dose-dependently inhibits potent tumor growth compared to the Olaparib treatment group[1].

1681017-83-3

C23H23FN4O2

406.461

NOV140101;IDX-1197

DMSO:90 mg/mL (221.43 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years