PF-06651600

PF-06651600 is a covalent inhibitor of JAK3 (IC50 = 33.1 nM). It is selective for JAK3 over JAK1, JAK2, and tyrosine kinase 2 (TYK2, IC50s = >10,000 for all) and a panel of 304 other kinases at 1 µM. PF-06651600 inhibits STAT5, STAT6, and STAT3 phosphorylation induced by IL-2, IL-4, or IL-21, respectively, in isolated human lymphocytes (IC50s = 244, 340, and 350 nM, respectively). It inhibits T cell differentiation into the T helper cells Th1 and Th17 in a T cell differentiation assay (IC50s = 30 and 167 nM, respectively). PF-06651600 (3, 10, or 30 mg/kg) reduces paw swelling in a rat model of adjuvant-induced arthritis. It also decreases disease severity in a mouse model of experimental autoimmune encephalomyelitis (EAE) when administered at doses of 30 or 100 mg/kg. Formulations containing PF-06651600 have been used in the treatment of severe alopecia in adults and adolescents.Formal Name: 1-[(2S,5R)-2-methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one. CAS Number: 1792180-81-4. Synonyms: Ritlecitinib. Molecular Formula: C15H19N5O. Formula Weight: 285.3. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble. SMILES: O=C(C=C)N(C1)[C@@H](C)CC[C@@H]1NC2=C3C(NC=C3)=NC=N2. InChi Code: InChI=1S/C15H19N5O/c1-3-13(21)20-8-11(5-4-10(20)2)19-15-12-6-7-16-14(12)17-9-18-15/h3,6-7,9-11H,1,4-5,8H2,2H3,(H2,16,17,18,19)/t10-,11-/m0/s1. InChi Key: CBRJPFGIXUFMTM-QWRGUYRKSA-N.