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CAS#: 1206161-97-8

Description: Filgotinib, also known as GLPG0634, is a potent and selective JAK1 inhibitor under investigation for the treatment of rheumatoid arthritis (RA) and Crohn’s disease. It is considered a promising agent as it inhibits JAK1 selectively. Filgotinib displayed a selectivity of 30-fold for JAK1- over JAK2-dependent signaling. GLPG0634 dose-dependently inhibited Th1 and Th2 differentiation and to a lesser extent the differentiation of Th17 cells in vitro.

Synonym: GLPG0634; GLPG 0634; GLPG-0634. Filgotinib; PubChemSID 163643231

IUPAC/Chemical Name: N-(5-(4-((1,1-dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide.


Name: Filgotinib (GLPG0634)
CAS#: 1206161-97-8
Chemical Formula: C21H23N5O3S
Exact Mass: 425.15216
Molecular Weight: 425.5
Elemental Analysis: C, 59.28; H, 5.45; N, 16.46; O, 11.28; S, 7.54


White to off-white-solid powder
>98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition:
Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Soluble in DMSO, not in water
Shelf Life:
>2 years if stored properly
Drug Formulation:
GLPG0634 was formulated in polyethyleneglycol 200/0.9% NaCl (60/40; v/v) for i.v. administration and in 0.5% (v/v) methylcellulose for oral administration for all in vivo studies
Stock Solution Storage:
0 – 4 C for short term (days to weeks), or -20 C for long term (months).


1: Nakayamada S, Kubo S, Iwata S, Tanaka Y. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Aug 31. Review. Erratum in: BioDrugs. 2016 Oct 3;:. PubMed PMID: 27577235.

2: Roskoski R Jr. Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases. Pharmacol Res. 2016 Sep;111:784-803. doi: 10.1016/j.phrs.2016.07.038. Epub 2016 Jul 26. Review. PubMed PMID: 27473820.

3: Liu CY, Li Q, Zhou XD. [Inhibition of suppressor of cytokine signaling 1 on lipopolysaccharide-induced mucin5AC hypersecretion and the mechanism in human bronchial epithelial cells]. Zhonghua Yi Xue Za Zhi. 2016 Mar 29;96(12):966-70. doi: 10.3760/cma.j.issn.0376-2491.2016.12.012. Chinese. PubMed PMID: 27045723.

4: Nielsen OH, Seidelin JB, Ainsworth M, Coskun M. Will novel oral formulations change the management of inflammatory bowel disease? Expert Opin Investig Drugs. 2016 Jun;25(6):709-18. doi: 10.1517/13543784.2016.1165204. Epub 2016 Mar 28. PubMed PMID: 26967267.

5: Namour F, Desrivot J, Van der Aa A, Harrison P, Tasset C, van’t Klooster G. Clinical Confirmation that the Selective JAK1 Inhibitor Filgotinib (GLPG0634) has a Low Liability for Drug-drug Interactions. Drug Metab Lett. 2016;10(1):38-48. PubMed PMID: 26693854.

6: Namour F. Author’s Reply to Srinivas: “Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection”. Clin Pharmacokinet. 2015 Dec;54(12):1297-8. doi: 10.1007/s40262-015-0336-5. PubMed PMID: 26482170; PubMed Central PMCID: PMC4661215.

7: Srinivas NR. Comment on: “Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modelling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection”. Clin Pharmacokinet. 2015 Dec;54(12):1293-5. doi: 10.1007/s40262-015-0335-6. PubMed PMID: 26482169.

8: Namour F, Diderichsen PM, Cox E, Vayssière B, Van der Aa A, Tasset C, Van’t Klooster G. Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection. Clin Pharmacokinet. 2015 Aug;54(8):859-74. doi: 10.1007/s40262-015-0240-z. PubMed PMID: 25681059; PubMed Central PMCID: PMC4513223.

9: Menet CJ, Fletcher SR, Van Lommen G, Geney R, Blanc J, Smits K, Jouannigot N, Deprez P, van der Aar EM, Clement-Lacroix P, Lepescheux L, Galien R, Vayssiere B, Nelles L, Christophe T, Brys R, Uhring M, Ciesielski F, Van Rompaey L. Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. J Med Chem. 2014 Nov 26;57(22):9323-42. doi: 10.1021/jm501262q. Epub 2014 Nov 17. PubMed PMID: 25369270.

10: Norman P. Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77. doi: 10.1517/13543784.2014.918604. Epub 2014 May 12. Review. PubMed PMID: 24818516.