Filgotinib (GLPG0634)

Catalog No.S7605

Filgotinib (GLPG0634) Chemical Structure

Molecular Weight(MW): 425.50

Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.

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Biological Activity

Description Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
Targets
JAK1 [1] JAK2 [1] TYK2 [1] JAK3 [1]
10 nM 28 nM 116 nM 810 nM
In vitro

In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells. [1]

In vivo Following oral administration, the absolute bioavailability is moderate in rats (45%) and high in mice (∼100%). Filgotinib (30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)) dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice. [1] Filgotinib (GLPG0634) in DSS-treated mice demonstrates that inhibition of JAK1 is sufficient for achieving strong efficacy in pre-clinical mouse model, correlated to the inhibition of STAT3 phosphorylation in the inflamed colon. [2]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Rat CIA model and mouse CIA model
  • Formulation: 0.5% (v/v) methylcellulose
  • Dosages: 30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 85 mg/mL (199.76 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+ddH2O 3mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 425.50
Formula

C21H23N5O3S

CAS No. 1206161-97-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02914535 Recruiting Ulcerative Colitis Gilead Sciences|Galapagos NV January 24, 2017 Phase 3
NCT02914600 Recruiting Crohns Disease Gilead Sciences|Galapagos NV January 23, 2017 Phase 3
NCT03025308 Not yet recruiting RheumatoId Arthritis Gilead Sciences|Galapagos NV February 2017 Phase 3
NCT03046056 Not yet recruiting Small Bowel Crohns Disease Gilead Sciences|Galapagos NV February 2017 Phase 2
NCT02914561 Recruiting Crohns Disease Gilead Sciences|Galapagos NV October 2016 Phase 3
NCT02885181 Recruiting Rheumatoid Arthritis Gilead Sciences September 2016 Phase 2

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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID