GSK2110183

GSK2110183CAS号: 1047644-62-1分子式: C18H17Cl2FN4OS分子量: 427.32描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

GSK2110183 is a potent pan-AKT inhibitor that demonstrated synergy with bortezomib in preclinical models of multiple myeloma (MM).

纯度
98%
储存/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.
基本信息
别名
Afuresertib;GSK-2110183C
可溶性/溶解性
DMSO : ≥ 40 mg/mL (93.61 mM)
生物活性
靶点
Akt1,Akt2,Akt3
In vitro(体外研究)
Afuresertib inhibits the kinase activity of the E17K AKT1 mutant protein with EC50 of 0.2 nM. Afuresertib shows a concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3b, PRAS40, FOXO and Caspase 9. Overall 65% of the hematological cell lines are sensitive to afuresertib (EC50
In vivo(体内研究)
Mice bearing BT474 breast tumor xenografts are dosed with afuresertib (p.o.) at 10, 30 or 100 mg/kg daily which results in 8, 37 and 61% TGI, respectively. Mice bearing SKOV3 ovarian tumor xenografts are treated with 10, 30 and 100 mg/kg afuresertib which results in 23, 37 and 97% TGI, respectively.

分子结构图

GSK2110183