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BAY-1082439 (BAY1082439) is an orally bioavailable and highly selective PI3Kα/β-balanced inhibitor, binding to PI3Kα/β isoforms with a ratio of 1:3 in enzymatic assays (PI3Kα (4.9 nM) vs. PI3Kβ (15.0 nM)), and >1000-fold selectivity against mTOR kinase. By specifically targeting class I PI3K alpha (α) and beta (β) isoform, BAY 1082439 may be more efficacious and less toxic than pan PI3K inhibitors. The balanced PI3Kα and PI3Kβ activity of BAY 1082439 is also reflected in cellular mechanistic (p-AKT473) and proliferation assays in PI3Kα- (KPL4, BT474) vs. PI3Kβ-driven (PC3, LNCaP) tumor cells. In vivo, BAY 1082439 showed clear advantages over the strong PI3Kα inhibitor BAY80-6946 (Copanlisib) in PTEN/PI3Kβ-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. BAY 1082439 showed strong p-AKT inhibition at 2 and 5 hours post-treatment while p-AKT returned to levels comparable to the vehicle group at 24 hours in all 4 tumor models tested. BAY 1082439 could induce tumor regression in KPL4 (PIK3CAmut and HER2+), and tumor stasis in HEC-1B (PTENdel) and in HEC-1A (PIK3CAmut) tumor models. (Ref. 1)
Catalog NO: CT-BAY108
Synonym: BAY1082439
CAS NO: 1375469-38-7
Mol. Formula: C25H30N6O5∙0.2H2O
MW: 498.2
** in vivo grade material. A snow-white, recrystallized powder (pic attached), >99% pure by chiral and achiral HPLCs, coming with a spot-on quantitative elemental analysis. Bulk Stock!! Ship within 1 day.