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.
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纯度 |
>98%
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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.
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基本信息 | |
别名 |
AZD-8186,AZD 8186
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外观 |
Powder
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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
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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
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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.
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分子结构图