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Saruparib

CAS No. : 2589531⁻⁷6-8

MCE 国际站：Saruparib

产品活性：Saruparib (AZD5305) 是一种口服有效的，具有选择性的多聚 ADP 核糖聚合酶抑制剂和捕集剂，对 PARP1 和 PARP2 的 IC₅₀ 值分别为 3 nM 和 1400 nM。Saruparib 具有抗增殖活性，并抑制 DNA 修复缺陷细胞的生长。

研究领域：Cell Cycle/DNA Damage | Epigenetics

作用靶点：PARP

In Vitro: Saruparib (AZD5305) (0.1 nM-100 µM) inhibits PARylation in A549 WT cells by selectively blocking PARP1 enzymatic activity with an IC₅₀ value of 2.3 nM.
AZD5305 (0.1 nM-100 µM; A549 WT cells) is a potent ａnd selective trapper of PARP1 in a dose-dependent manner by single digit nanomolar concentrations.
AZD5305 (0.1 nM-100 µM; 48 h; DLD1 WT ａnd DLD1 BRCA2^-/-) has anti-proliferative activity ａnd targets cancer cells with HRR-deficiency, inducing DNA damage accumulation ａnd cell-cycle arrest.

In Vivo: Saruparib (AZD5305) (0.01-0.3 mg/kg; p.o.; daily, for 35 d; female Han Wistar rats) demonstrates sustained antitumor activity in BRCAm xenograft ａnd PDX models in vivo.

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