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产品价格:电议      采购度:1594      原产地:美洲
发布时间:2021/7/27 8:30:40 所属地区:上海 上海市
简要描述:
AKT-IN-1 是一种变构 AKT 抑制剂,IC50 为 μM。
标签:aktin1
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CAS No. : 1357158-81-6
MCE 站:AKT-IN-1
产品活性:AKT-IN-1 是一种变构 AKT 抑制剂,IC50 为 1.042 μM。
研究领域:PI3K/Akt/mTOR
作用靶点:Akt
In Vitro: AKT-IN-1 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.
In Vivo: 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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更新时间:2024/1/2 10:16:38
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