NVP-BSK805 (hydrochloride)

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.Formal Name: 4-(2,6-difluoro-4-(3-(1-(pip4-(2,6-difluoro-4-(3-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)quinoxalin-5-yl)benzyl)morpholine, dihydrochloride. CAS Number: 1942919-79-0. Molecular Formula: C27H28F2N6O . 2HCl. Formula Weight: 563.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 25 mg/ml, Ethanol: 1 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 244, 275, 350 nm. SMILES: FC1=C(CN2CCOCC2)C(F)=CC(C3=CC=CC4=C3N=C(C5=CN(C6CCNCC6)N=C5)C=N4)=C1.Cl.Cl. InChi Code: InChI=1S/C27H28F2N6O.2ClH/c28-23-12-18(13-24(29)22(23)17-34-8-10-36-11-9-34)21-2-1-3-25-27(21)33-26(15-31-25)19-14-32-35(16-19)20-4-6-30-7-5-20,,/h1-3,12-16,20,30H,4-11,17H2,2*1H. InChi Key: NUOCAPALWRHKCU-UHFFFAOYSA-N.