产品信息
抗原名称
Akt1,Akt2,Akt3,Akt1 E17K mutant,PKG1α,PKA,PKG1β,ROCK,PKCη,P70S6K,RSK1,PKCβ1,PKCθ
商品描述
GSK2110183 hydrochloride is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.
分子量
481.77
纯度
98%
可溶性
DMSO : ≥ 36 mg/mL (74.72 mM)
In vitro(体外研究)
GSK2110183 is an ATP competitive, time dependant and fully reversible inhibitors of the Akt kinase family. GSK2110183 has a Ki 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.
In vivo(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.
背景
分子式
C18H17Cl3F2N4OS
CAS号
2070009-64-0
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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