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PI3Kα/mTOR-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PI3Kα/mTOR-IN-1图片
CAS NO:1013098-90-2
规格:98%
分子量:310.35
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
PI3Kα/mTOR-IN-1 是一种有效的 PI3Kα/mTOR 双重抑制剂,在细胞实验中对 PI3Kα 的 IC50 值为 7 nM,在体外酶实验中对 mTOR 和 PI3Kα 的 Ki 值分别为 10.6 nM 和 12.5 nM。
CAS:1013098-90-2
分子式:C16H18N6O
分子量:310.35
纯度:98%
存储:Store at -20°C

Background:

PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively. PI3Kα|7 nM (IC50, Cell Assay)|PI3Kα|12.5 nM (Ki)|mTOR|10.6 nM (Ki)


PI3Kα/mTOR-IN-1 exhibits potent activity against PI3Kα and mTOR, high LipE, good kinase selectivity and robust ADMET properties[1].


PI3Kα/mTOR-IN-1 exhibits low HLM ER, but it is highly cleared in rat liver microsome (RLM) with ER of 0.88. PI3Kα/mTOR-IN-1 exhibits moderate clearance, moderate Vdss, T1/2 of 0.9 h, and good oral bioavailability[1].


[1]. Le PT, et al. Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR. Bioorg Med Chem Lett. 2012 Aug 1;22(15):5098-103.