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LY2784544 is a potent, ATP-competitive inhibitor of janus kinase 2 (JAK2) that less effectively inhibits JAK3 (IC50s = 3 and 48 nM, respectively). It also inhibits JAK2 containing the V617F mutation (IC50 = 20 nM), blocking STAT5 phosphorylation and proliferation of Ba/F3 pro-B-cells expressing this constitutively active JAK2 mutant form. When given by oral gavage, LY2784544 significantly reduces the growth of Ba/F3 pro-B-cells in SCID mice without affecting erythroid progenitors, reticulocytes, or platelets. JAK inhibitors, including LY2784544, may be useful in hematological malignancies.Formal Name: 3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)-imidazo[1,2-b]pyridazin-6-amine. CAS Number: 1229236-86-5. Molecular Formula: C23H25ClFN7O. Formula Weight: 470.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml, Ethanol: 10 mg/ml. lambdamax: 225, 255, 345 nm. SMILES: CC1=CC(NC2=NN3C(C(CN4CCOCC4)=C2)=NC(C)=C3CC5=C(F)C=C(Cl)C=C5)=NN1. InChi Code: InChI=1S/C23H25ClFN7O/c1-14-9-21(29-28-14)27-22-11-17(13-31-5-7-33-8-6-31)23-26-15(2)20(32(23)30-22)10-16-3-4-18(24)12-19(16)25/h3-4,9,11-12H,5-8,10,13H2,1-2H3,(H2,27,28,29,30). InChi Key: SQSZANZGUXWJEA-UHFFFAOYSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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