Description
A JAK1 inhibitor (IC50 = 10 nM); selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and Tyk2 (IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3 and -4, FMS, Mer, and TBK1 activity by >35% in a panel of 177 tyrosine kinases at 1 µM; inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells (IC50 = 629 nM in isolated human whole blood); reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis at 0.1-30 mg/kg per day for 15 days