Ruxolitinib (phosphate)

Ruxolitinib is a potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively, and is relatively less selective for JAK3 (IC50 = 322 nM). It blocks interleukin-6 (IL-6) signaling (IC50 = 281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50 = 127 nM). In primary cultures, ruxolitinib preferentially suppresses erythroid progenitor colony formation from JAK2V617F+ polycythemia vera patients (IC50 = 67 nM) versus healthy donors (IC50 > 400 nM). In a mouse model of JAK2V617F+ myeloproliferative neoplasms (MPN), 90 mg/kg ruxolitinib reduces splenomegaly, decreases circulating levels of IL-6 and TNF-alpha, eliminates neoplastic cells, and prolongs survival.Formal Name: betaR-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile, monophosphate. CAS Number: 1092939-17-7. Synonyms: INC 424 (phosphate), INCB 018424 (phosphate). Molecular Formula: C17H18N6 . H3PO4. Formula Weight: 404.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMSO: 33 mg/ml, Ethanol: 1 mg/ml. lambdamax: 217, 224, 254, 311 nm. SMILES: N#CC[C@H](C1CCCC1)N(N=C2)C=C2C3=C4C(NC=C4)=NC=N3.O=P(O)(O)O. InChi Code: InChI=1S/C17H18N6.H3O4P/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16,1-5(2,3)4/h6,8-12,15H,1-5H2,(H,19,20,21),(H3,1,2,3,4)/t15-,/m1./s1. InChi Key: JFMWPOCYMYGEDM-XFULWGLBSA-N.