| Identification | Back Directory | [Name]
BAY-1125976. | [CAS]
1402608-02-9 | [Synonyms]
CS-2913
BAY1125976
BAY 1125976
BAY-1125976.
BAY-1125976; BAY 1125976
2-[4-(1-Aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide
Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl- | [Molecular Formula]
C23H21N5O | [MDL Number]
MFCD30481340 | [MOL File]
1402608-02-9.mol | [Molecular Weight]
383.45 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:13.0(Max Conc. mg/mL);33.9(Max Conc. mM)
DMF:5.0(Max Conc. mg/mL);13.04(Max Conc. mM)
DMF:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.65(Max Conc. mM) | [form ]
A crystalline solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
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. |
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