Formulation: A solid
Formal Name: 1-[(2S,5R)-2-methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one
Purity: ≥95%
Formula Markup: C15H19N5O
Formula Weight: 285,3
Shelf life (days): 1460
CAS Number: 1792180-81-4
Notes: PF-06651600 is a covalent inhibitor of JAK3 (IC50 = 33.1 nM).{69674} 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.
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