Peficitinib

Peficitinib is an inhibitor of JAK (IC50s = 3.9, 5, and 0.71 nM for JAK1-3, respectively). It is 14-fold selective for JAK1 and JAK3 over JAK2 in erythropoietin-induced leukemia cell proliferation assays. Peficitinib inhibits IL-2-induced proliferation of rat splenocytes (IC50 = 10 nM) and phosphorylation of STAT5 in rat and human whole blood (IC50s = 124 and 127 nM, respectively). In vivo, peficitinib reduces paw swelling (ED50 = 5.6 mg/kg) and bone destruction in a rat model of adjuvant-induced arthritis when administered at a dose of 30 mg/kg.Formal Name: 4-[(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, stereoisomer. CAS Number: 944118-01-8. Synonyms: ASP015K, JNJ-54781532. Molecular Formula: C18H22N4O2. Formula Weight: 326.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 246, 294 nm. SMILES: NC(C1=CN=C2C(C=CN2)=C1N[C@@H]3[C@H](C4)C[C@@]5(O)C[C@@H]3C[C@@H]4C5)=O. InChi Code: InChI=1S/C18H22N4O2/c19-16(23)13-8-21-17-12(1-2-20-17)15(13)22-14-10-3-9-4-11(14)7-18(24,5-9)6-10/h1-2,8-11,14,24H,3-7H2,(H2,19,23)(H2,20,21,22)/t9-,10-,11+,14-,18-. InChi Key: DREIJXJRTLTGJC-ZKVNVPQCSA-N.