Description: OSI-027 (ASP4786) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kalpha, PI3Kbeta, PI3Kgamma or DNA-PK. Phase 1. Target: Autophagy, PI3K, mTOR, DNA-PK. Smiles:...

The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin (Cay-13346)) and regulate different pathways. OSI-027 is an inhibitor of the catalytic site of...

OSI-027 is an inhibitor of mTORC1/2 that exhibits anticancer chemotherapeutic activity. In vitro, OSI0027 inhibits phosphorylation of downstream target Akt, inhibiting cell proliferation in breast cancer cells. OSI-027 also induces apoptosis in several lymphoid cell lines including mantle cell lymphoma, acute...