Afuresertib HCl (GSK2110183),1047645-82-8

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产品名称：Afuresertib HCl (GSK2110183)

产品别名：Afuresertib,GSK 2110183,GSK2110183,GSK 2110183 hydrochloride, GSK2110183 hydrochloride, GSK-2110183 hydrochloride

英文别名：Afuresertib;GSK 2110183;GSK2110183;GSK 2110183 hydrochloride;GSK2110183 hydrochloride;GSK-2110183 hydrochloride

靶点：Akt

CAS：1047645-82-8

纯度：>98%

外观：Powder

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

溶解性：DMSO: ≥ 52 mg/mL

体外研究：

Afuresertib (GSK 2110183B) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G₁ phase. Western blotting analysis shows that Afuresertib increases the expression of p21^WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G₁ phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response.

体内研究：

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