Filgotinib maleate

Names

[ Name ]:
Filgotinib maleate

Biological Activity

[Description]:

Filgotinib (maleate) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research[1][2].

[Related Catalog]:

Signaling Pathways >> JAK/STAT Signaling >> JAK

Signaling Pathways >> Epigenetics >> JAK

Signaling Pathways >> Stem Cell/Wnt >> JAK

Research Areas >> Inflammation/Immunology

[Target]

JAK1:10 nM (IC50)

JAK2:28 nM (IC50)

JAK3:810 nM (IC50)

Tyk2:116 nM (IC50)

[In Vitro]

Filgotinib (maleate) (1-10 μM) inhibits Th1 and Th2 differentiation in a dose-dependent manner[1].

[References]

[1]. Van Rompaey L, et, al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013 Oct 1;191(7):3568-77.

[2]. Labetoulle R, et al. Filgotinib for the treatment of Crohn's disease. Expert Opin Investig Drugs. 2018 Mar;27(3):295-300.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₇N₅O₇S

[ Molecular Weight ]:
541.58

Related Compounds

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