BAY-1082439 is an oral, highly selective and balanced PI3Kα/β inhibitor, with IC50 values of 4.9 nM and 15 nM for PI3Kα and PI3Kβ isoforms respectively, and >1000-fold selectivity against mTOR kinase. BAY-1082439 demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN. In vivo, it also showed clear advantages over the strong PI3Kα inhibitor BAY80-6946 (Copanlisib) in PTEN/PI3Kβ-driven tumor models. BAY-1082439 represents a new type of PI3K inhibitor with unique pharmacological and pharmacodynamic properties to be further explored.

KEYWORDS: BAY-1082439 | Supplier | PI3Kα/β inhibitor | BAY1082439 | BAY-1082439 | CT-BAY108 | CAS [1375469-38-7] | Phosphatidylinositol | PI3K | inhibitor | Enzymes