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Introduction of 1013098-90-2 :
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. IC50 & Target: IC50: 7 nM (PI3Kα, cell) Ki: 10.6 nM (mTOR), 12.5 nM (Mouse PI3Kα)In Vitro: PI3Kα/mTOR-IN-1 exhibits potent activity against PI3Kα and mTOR, high LipE, good kinase selectivity and robust ADMET properties. In Vivo: 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.