BAY 1082439|BAY1082439|PI3Kα/β inhibitor

BAY 1082439|BAY1082439|PI3Kα/β inhibitor

BAY 1082439 is a highly selective and balanced PI3Kα/β inhibitor demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN.

Product Name: BAY 1082439|Cat No: DC9939|cas: 1375469-38-7|Other Names: BAY10-82439; BAY 10-82439; BAY-10-82439; BAY1082439; BAY 1082439; BAY-1082439

BAY 1082439 has an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase. The balanced PI3Kα and PI3Kα activity of BAY 1082439 is also reflected in cellular mechanistic (p-AKT473) and proliferation assays in PI3Kα- (KPL4, BT474) vs. PI3Kα-driven (PC3, LNCaP) tumor cells. In vivo, BAY 1082439 showed clear advantages over the strong PI3Kα inhibitor BAY 80-6946 in PTEN/PI3Kα-driven tumor models (e.g., PC3 and HEC-1B), when the two compounds were compared at their MTDs. Furthermore, BAY 1082439 has unique pharmacokinetic (PK) properties with very high plasma free fractions across all species tested (33-50%), large Vss, high clearance and intermediate T1/2.

For the research and scientific use only, not for human use!