LY2784544

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.