Filgotinib (GLPG0634)

Catalog No.S7605

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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Filgotinib (GLPG0634) Chemical Structure

Filgotinib (GLPG0634) Chemical Structure
Molecular Weight: 425.50

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

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]
IC50 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(Only for Reference)

Kinase Assay: [1]

Biochemical assays IC50 determination Recombinant JAK1, TYK2, JAK2, and JAK3 are used to develop activity assays in 50 mM HEPES (pH 7.5), 1 mM EGTA, 10 mM MgCl2, 2 mM DTT, and 0.01% Tween 20. The amount of JAK protein is determined per aliquot, maintaining initial velocity and linearity over time. The ATP concentration is equivalent to 4-fold the experimental Km value and the substrate concentration (ULight-conjugated JAK-1(Tyr1023) peptide) corresponded to the experimentally determined Km value. After 90 min incubation at room temperature (RT), the amount of phosphorylated substrate is measured by addition of 2 nM europium-anti-phosphotyrosine Ab and 10 mM EDTA in Lance detection buffer. Compound IC50 values are determined by preincubating the enzyme with compound at RT for 60 min, prior to the addition of ATP.

Animal Study: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Van Rompaey L, et al. J Immunol. 2013, 191(7), 3568-3577.

[2] Merciris D, et al. ECCO. 2014, P072.

Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02162355 Completed Healthy Galapagos NV June 2014 Phase 1
NCT02084199 Completed Renal Impairment Galapagos NV March 2014 Phase 1
NCT02048618 Completed Crohns Disease Galapagos NV February 2014 Phase 2
NCT02065700 Enrolling by invitation Rheumatoid Arthritis Galapagos NV February 2014 Phase 2
NCT01915667 Completed Healthy Galapagos NV July 2013 Phase 1

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Chemical Information

Download Filgotinib (GLPG0634) SDF
Molecular Weight (MW) 425.50


CAS No. 1206161-97-8
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 85 mg/mL (199.76 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name N-[5-[4-[(1,1-Dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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