Filgotinib
JAK1 inhibitor / Potent and selective JAK1 inhibitor (IC50s=10, 28, 810 and 116 nM for JAK1, JAK2, JAK3 and TYK2 respectively.2 Displays potent anti-inflammatory activity in various models.1,2 Effective as a monotherapy in patients with active rheumatoid arthritis.3 Reverses oncostatin M-mediated inhibition of rat stem Leydig cell differentiation.4
Biochemicals & reagents
1206161-97-8
GLPG0634; GS-6034
1) Menet et al. (2014), Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634; J. Med. Chem., 57 9323 2) Rompaey et al. (2013), Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases; J. Immunol., 191 3568 3) Kavanaugh et al. (2017), Filgotinib (GLPG0634/GS-6034), an oral selective JAK1 inhibitor, is effective as monotherapy in patients with active rheumatoid arthritis: results from a randomized dose-finding study (DARWIN 2); Ann. Rheum. Dis., 76 1009 4) Wang et al. (2019), Oncostatin M inhibits differentiation of rat stem Leydig cells in vivo and in vitro; J. Cell. Mol. Med., 23 426
-20°C
TARGET: Kinase -- PATHWAY: JAK/STAT; Cytokine -- RESEARCH AREA: Stem cells -- DISEASE AREA: Inflammation