CAS NO: | 1357158-81-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | AKT-IN-1 is an allostericAKTinhibitor with anIC50of 1.042 μM. | ||||||||||||||||
IC50& Target | IC50: 1.042 μM (AKT)[1] | ||||||||||||||||
体外研究 (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[1]. | ||||||||||||||||
体内研究 (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[1]. | ||||||||||||||||
分子量 | 343.42 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C22H21N3O | ||||||||||||||||
CAS 号 | 1357158-81-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 75 mg/mL(218.39 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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