PI3Kα/mTOR-IN-1

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.

Research Areas >> Cancer

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.

Rapamycin (Sirolimus) | 3-Methyladenine | LY294002 | Wortmannin | Alpelisib (BYL719) | Torin 1 | BKM120 | Eganelisib(IPI-549) | MHY1485 | Sapanisertib (MLN0128) | AZD8055 | BAY 80-6946 (Copanlisib) | Idelalisib (CAL-101) | Dactolisib (BEZ235) | Quercetin