A-966492,934162-61-5

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抑制剂描述：

产品名称：A-966492

产品别名：见爱必信官网

英文别名：A-966492

靶点：PARP

CAS：934162-61-5

纯度：>98%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：

A-966492是一种新型有效的PARP1和PARP2抑制剂，K_i分别为1 nM和1.5 nM。A-966492是最有效的PARP抑制剂之一。在所有细胞实验中，A-966492有效抑制PARP-1，EC50为1nM，K_i值为1 nM，作用于PARP-2时，K_i值为1.5 nM。A-966492作用于PARP酶具有极好的药效,尤其作用于C41细胞。

溶解性：DMSO ：64 mg/mL warmed (197.31 mM)

体外研究：

A-966492 is one of the most potent PARP inhibitors. A-966492 displays excellent potency against the PARP-1 enzyme with a Kiof 1 nM and an EC50 of 1 nM in a whole cell assay. A-966492 significantly enhances the efficacy of TMZ in a dose-dependent manner. In addition, A-966492 is orally bioavailable across multiple species, crosses the blood−brain barrier, and appears to distribute into tumor tissue. A-966492 represents a promising, structurally diverse benzimidazole analogue and is being further characterized preclinically.

体内研究：A-966492 also demonstrates good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in combination with carboplatin. In addition, A-966492 has excellent pharmaceutical properties and has demonstrated in vivo efficacy in preclinical mouse tumor models in combination with TMZ and carboplatin, as well as single agent activity in a BRCA1-deficient MX-1 tumor model. A-966492 is further characterized in Sprague−Dawley rats, beagle dogs, and cynomolgus monkeys, with A-966492 demonstrating oral bioavailabilities of 34−72% and half-lives of 1.7−1.9 hours. In vivo, A-966492 demonstrates significant enhancement of the efficacy of TMZ in a murine B16F10 syngeneic melanoma model, with the A-966492 combination groups showing superior efficacy.

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