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| | 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride Basic information |
| | 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMF: 20 mg/ml; DMSO: 25 mg/ml; Ethanol: 1 mg/ml; PBS (pH 7.2): 10 mg/ml | | form | A crystalline solid | | color | Light yellow to yellow |
| | 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride Usage And Synthesis |
| Description | Janus kinases (JAKs) are non-receptor tyrosine kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family. A point mutation of JAK2, V617F, activates signaling through STAT5 and drives certain forms of cancer. NVP-BSK805 is a potent inhibitor of JAK2 that also inhibits the JAK2V617F mutant enzyme (IC50s for both enzymes ~ 0.5 nM). It displays at least 20-fold selectivity against other JAK enzymes and a panel of serine/threonine and tyrosine kinases. This ATP-competitive inhibitor is orally bioavailable and has a long half-life in vivo, suppressing leukemic cell spreading and splenomegaly in JAK2V617F cell-driven disease in mice. NVP-BSK805 suppresses recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats. NVP-BSK805 can be used to study the molecular mechanisms involved in JAK2V617F signaling in cells. |
| | 8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline dihydrochloride Preparation Products And Raw materials |
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