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.