Venadaparib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Venadaparib (IDX-1197) 是一种有效的、选择性的、口服活性的 PARP 抑制剂，对 PARP1 和 PARP2 的 IC50 值分别为 1.4 nM 和 1.0 nM。

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.(In Vitro):Venadaparib significantly inhibits PARP1-mediated PAR expression with an EC50?of 0.5 nM In DNA damage-induced Hela cells.(In Vivo):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.

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

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.

IDX-1197 | NOV140101

Cell Cycle/DNA Damage

PARP

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1681017-83-3

406.461

C23H23FN4O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (246.03 mM)

Fc1ccc(Cc2n[nH]c(=O)c3ccccc23)cc1C(=O)N1CC(CNC2CC2)C1

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(-20℃)

With Ice Pack

≥ 2 years