Afuresertib (GSK2110183),1047634-63-8

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YZ剂描述：

产品名称：Afuresertib (GSK2110183)

产品别名：GSK2110183; GSK 2110183; GSK-2110183

英文别名：GSK2110183;GSK 2110183;GSK-2110183

靶点：Akt

CAS：1047634-63-8

纯度：98% min

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

GSK2110183是一个口服性的，选择性，ATP竞争性的GXAktYZ剂，对Akt1/Akt2 /Akt3的IC50值分别为0.08/2/2.6 nM。

溶解性：10 mM in DMSO

体外研究：

GSK2110183 is an ATP competitive, time dependant and fully reversible inhibitors of the Akt kinase family. GSK2110183 has a K_i of 0.08, 2 and 2.6 nM against Akt1, Akt2 and Akt3, respectively. GSK2110183 inhibits the kinase activity of the E17K Akt 1 mutant protein in a standard kinase assay with EC₅₀ of 0.2 nM.

体内研究：

Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts.

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