AZD-26

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抑制剂描述：

产品名称：AZD-26

产品别名：见爱必信官网

英文别名：AZD-26

靶点：Akt

CAS：1357158-81-6

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：AZD-26 is an inhibitor of AKT. AZD-26 inhibits the phosphorylation of Thr308 on AKT in BT474 cells with an IC50 of 422 nM.

溶解性：

体外研究：

AKT-IN-1 (Compound 26) is able to potently inhibit phosphorylation of AKT in cells at both Thr308 and Ser473, with IC50s of 0.422 and 0.322 μM, respectively. AKT-IN-1 inhibits the phosphorylation of ribosomal protein S6, a downstream effector of the PI3K-AKT pathway. AKT-IN-1 potently inhibits the phosphorylation of PRAS40.

体内研究：The effects of AKT-IN-1 (Compound 26) in vivo are characterized by measuring the pharmacodynamic activity of AKT-IN-1 in a BT474c breast adenocarcinoma xenograft model. Following acute doses of 100 and 200 mg/kg, AKT-IN-1 potently inhibits the phosphorylation of its downstream substrate GSK3β as well as the phosphorylation of AKT (Ser473), with a potency consistent with its pharmacokinetic profile. The in vivo activity of AKT-IN-1 is further characterized by measuring the effects on the growth of tumor cell xenografts. Continuous (daily) oral dosing of AKT-IN-1 (100 and 200 mg/kg) to nude mice bearing BT474c breast adenocarcinoma xenografts results in inhibition of tumor growth in a dose-dependent manner. When dosed at 200 mg/kg daily, AKT-IN-1 causes significant tumor growth inhibition.

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