Synonyms: 2-[4-(1-Aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide; BAY-1125976; BAY1125976
Molecular Formula: C23H21N5O
Molecular Weight: 383.45
Linear Structural Formula: C23H21N5O
MDL Number: MFCD30481340
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: BAY 1125976 is an orally active, potent and highly selective AKT1/2 allosteric inhibitor (IC50 = 5.2/18 nM with 10 muM ATP, IC50 = 44/36 nM with 2 mM ATP; AKT3 IC50 = 427 nM with 10 muM ATP) that targets a pocket formed by the kinase & PH domain. BAY 1125976 reduces basal AKT T308/S473 phosphorylation (IC50 = 0.9/1.1; KPL-4 cells) and exhibits anti-cancer efficacy in cultures (IC50 = 0.02-10 muM, 23 human cancer lines) and in xenograft models in vivo (25, 50 mg/kg/day or 5, 15, 25 mg/kg bid. po.; mice), including breast cancers (KPL4 PIK3CAH1074R mutant, MCF7, HBCx-2), AKTE17K-driven prostate cancer LAPC-4, and anal cancer AXF 984.