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| | BAY-1125976. Basic information |
| Product Name: | BAY-1125976. | | Synonyms: | BAY 1125976;BAY1125976;BAY-1125976.;2-[4-(1-Aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide;BAY-1125976; BAY 1125976;CS-2913;Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-;inhibit,Inhibitor,Protein kinase B,Akt,BAY 1125976,BAY1125976,PKB,BAY-1125976 | | CAS: | 1402608-02-9 | | MF: | C23H21N5O | | MW: | 383.45 | | EINECS: | | | Product Categories: | | | Mol File: | 1402608-02-9.mol |  |
| | BAY-1125976. Chemical Properties |
| 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 |
| | BAY-1125976. Usage And Synthesis |
| 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. |
| | BAY-1125976. Preparation Products And Raw materials |
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