Venadaparib (IDX-1197) 是一种有效、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 nM 和 1.0 nM。Venadaparib 对 PARP-5 不敏感。Venadaparib 可防止 DNA 单链断裂 (SSB) 的修复，可用于实体瘤研究。
货号:ajcx33110
CAS:1681017-83-3
分子式:C23H23FN4O2
分子量：406.45
溶解度:DMSO : 100 mg/mL (246.03 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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 DNA damage-induced Hela cells, Venadaparib (IDX-1197) significantly inhibits PARP1-mediated PAR expression (EC50 of 0.5 nM)[1].

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].

[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.