PF-06700841 (tosylate)

PF-06700841 is an inhibitor of JAK1 and tyrosine kinase 2 (TYK2, IC50s = 17 and 23 nM, respectively). It is selective for JAK1 and TYK2 over JAK2 and JAK3 (IC50s = 77 and 6,494 nM, respectively). PF-06700841 selectively inhibits IFN-alpha/STAT3 signaling over erythropoietin/STAT5 signaling in human whole blood (IC50s = 30 and 577 nM, respectively). It reduces increases in hind paw volume in a rat model of adjuvant-induced arthritis in a dose-dependent manner.Formal Name: [(1S)-2,2-difluorocyclopropyl][3-[2-[(1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-3,8-diazabicyclo[3.2.1]oct-8-yl]-methanone, 4-methylbenzenesulfonate. CAS Number: 2140301-96-6. Molecular Formula: C18H21F2N7O . C7H8O3S. Formula Weight: 561.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:20): 50µg/ml, Ethanol: slightly soluble. lambdamax: 224 nm. SMILES: CN1N=CC(NC2=NC=CC(N3CC4CCC(N4C([C@H]5C(F)(F)C5)=O)C3)=N2)=C1.CC6=CC=C(S(O)(=O)=O)C=C6. InChi Code: InChI=1S/C18H21F2N7O.C7H8O3S/c1-25-8-11(7-22-25)23-17-21-5-4-15(24-17)26-9-12-2-3-13(10-26)27(12)16(28)14-6-18(14,19)20,1-6-2-4-7(5-3-6)11(8,9)10/h4-5,7-8,12-14H,2-3,6,9-10H2,1H3,(H,21,23,24),2-5H,1H3,(H,8,9,10)/t12?,13?,14-,/m0./s1. InChi Key: FAKGOYNHHHOTEN-WTMFEIAXSA-N.