BAY-1125976

BAY-1125976 is an allosteric inhibitor of Akt1 and -2 (IC50s = 5.2 and 18 nM, respectively, in a time-resolved FRET assay). It is selective for Akt1 and -2 over Akt3 (IC50 = 427 nM in the same assay) but does inhibit the activity of the receptor tyrosine kinases FLT1, -3, -4, and Mer by greater than 50% in a panel of 227 kinases at 1 µM. BAY-1125976 inhibits the proliferation of 23 cancer cell lines (IC50s = 0.02-10 µM) and reduces tumor growth in KPL-4, MCF-7, and patient-derived xenograft (PDX) mouse models when administered at a dose of 50 mg/kg per day.Formal Name: 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-imidazo[1,2-b]pyridazine-6-carboxamide. CAS Number: 1402608-02-9. Molecular Formula: C23H21N5O. Formula Weight: 383.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5mg/mL, DMF:PBS (pH 7.2) (1:3): 0.25mg/mL, DMSO: 3mg/mL. lambdamax: 241, 379 nm. SMILES: NC(C(C=C1)=NN2C1=NC(C3=CC=C(C4(N)CCC4)C=C3)=C2C5=CC=CC=C5)=O. InChi Code: InChI=1S/C23H21N5O/c24-22(29)18-11-12-19-26-20(21(28(19)27-18)16-5-2-1-3-6-16)15-7-9-17(10-8-15)23(25)13-4-14-23/h1-3,5-12H,4,13-14,25H2,(H2,24,29). InChi Key: JBGYKRAZYDNCNV-UHFFFAOYSA-N.