PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC₅₀ of 7 nM for PI3Kα in a cell assay, and K_is 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)^[1]
Ki: 10.6 nM (mTOR), 12.5 nM (Mouse PI3Kα)^[1] In Vitro: PI3Kα/mTOR-IN-1 exhibits potent activity against PI3Kα and mTOR, high LipE, good kinase selectivity and robust ADMET properties^[1]. 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 V_dss, T_1/2 of 0.9 h, and good oral bioavailability^[1].