Filgotinib-d4

Filgotinib-d4 is intended for use as an internal standard for the quantification of filgotinib (Cay-17669) by GC- or LC-MS. 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-a]pyridin-2-yl]-cyclopropane-2,2,3,3-d4-carboxamide. CAS Number: 2041095-50-3. Synonyms: GLPG0634-d4. Molecular Formula: C21H19D4N5O3S. Formula Weight: 429.5. Purity: >99% deuterated forms (d1-d4). Formulation: (Request formulation change), A solid. Solubility: Acetonitrile:Methanol (1:1): soluble, DMSO: soluble. SMILES: O=S1(CCN(CC2=CC=C(C3=CC=CC4=NC(NC(C5C([2H])([2H])C5([2H])[2H])=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)/i8D2,9D2. InChi Key: RIJLVEAXPNLDTC-LZMSFWOYSA-N.