AZD8186

AZD8186CAS号: 1627494-13-6分子式: C24H25F2N3O4分子量: 457.47描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
AZD8186 is an inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity.
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
AZD-8186,AZD 8186
外观
Powder
可溶性/溶解性
DMSO 91 mg/mL warmed (198.92 mM)

Ethanol 35 mg/mL warmed (76.5 mM)

生物活性
靶点
PI3Kβ ,PI3Kδ ,PI3Kα
In vitro(体外研究)
AZD8186 potently inhibits p-Akt in MDA-MB-468 cells sensitive to PI3Kβ inhibition and Jeko B cells sensitive to PI3Kδ inhibition with IC50 of 3 nM and 4 nM, respectively. AZD8186 shows preferred growth inhibition activity in most PTEN deficient cell lines with GI50 of
In vivo(体内研究)
In nude mice bearing PTEN-deficient PC3 prostate tumor xenografts, AZD8186 (100 mg/kg, p.o.) strongly inhibits Akt phosphorylation levels, and causes significant tumor growth inhibition. When used in combination with ABT, AZD8186 (60 mg/kg, p.o.) results in complete inhibition of tumor growth. In the mouse PTEN-null TNBC models HCC70 and MDA-MB-468, and the prostate models HID28, AZD8186 (50 mg/kg, p.o.) also inhibits the growth of tumors. Combination therapy using AZD8186 with androgen deprivation results in long-lasting tumor regression, which persisted after treatment cessation.

分子结构图

AZD8186