Filgotinib

Filgotinib is a JAK1 inhibitor (IC50 = 10 nM). It is selective for JAK1 over JAK3 (IC50 = 810 nM) but also inhibits JAK2 and tyrosine kinase 2 (Tyk2, IC50s = 28 and 116 nM, respectively), as well as Abl, FLT1, -3, and -4, FMS, Mer, and TBK1 activity by greater than 35% in a panel of 177 tyrosine kinases at 1 µM. Filgotinib inhibits IL-6-induced phosphorylation of STAT1 in CD4+ T cells with an IC50 value of 629 nM in isolated human whole blood. It reduces hind paw macrophage and T cell infiltration and bone erosion in a rat model of collagen-induced arthritis when administered at doses ranging from 0.1 to 30 mg/kg per day for 15 days.Formal Name: N-[5-[4-[(1,1-dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-alpha]pyridin-2-yl]-cyclopropanecarboxamide. CAS Number: 1206161-97-8. Synonyms: GLPG0634. Molecular Formula: C21H23N5O3S. Formula Weight: 425.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.15 mg/ml, DMSO: 15 mg/ml. lambdamax: 233, 300 nm. SMILES: O=S1(CCN(CC2=CC=C(C3=CC=CC4=NC(NC(C5CC5)=O)=NN43)C=C2)CC1)=O. InChi Code: InChI=1S/C21H23N5O3S/c27-20(17-8-9-17)23-21-22-19-3-1-2-18(26(19)24-21)16-6-4-15(5-7-16)14-25-10-12-30(28,29)13-11-25/h1-7,17H,8-14H2,(H,23,24,27). InChi Key: RIJLVEAXPNLDTC-UHFFFAOYSA-N.