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抑制剂描述:

产品名称:GSK2110183

产品别名:见爱必信官网

英文别名:GSK2110183

靶点:Akt

CAS:1047644-62-1

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:

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

溶解性:DMSO : ≥ 40 mg/mL (93.61 mM)

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

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.

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