Home JAK/STAT JAK inhibitor Filgotinib (GLPG0634) For research use only.

Filgotinib (GLPG0634)

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.

Filgotinib (GLPG0634) Chemical Structure

Filgotinib (GLPG0634) Chemical Structure

CAS No. 1206161-97-8

Purity & Quality Control

Filgotinib (GLPG0634) Related Products

Signaling Pathway

JAK Signaling Pathways

JAK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CD34+ cells Function assay 45 mins Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis 24417533
NK92 Function assay Inhibition of JAK1/JAK3 in IL2-induced human NK92 cells assessed as pSTAT5, =0.148μM. 25369270
THP1 Function assay Inhibition of JAK1/JAK3 in IL4-induced human THP1 cells assessed as pSTAT6, =0.154μM. 25369270
U2OS Function assay Inhibition of JAK1/TYK2 in IFN-alphaB2-induced human U2OS cells assessed as pSTAT1, =0.436μM. 25369270
HeLa Function assay Inhibition of JAK1/JAK2 in OSM-induced human HeLa cells assessed as STAT1 reporter, =1.045μM. 25369270
THP1 Function assay Inhibition of JAK1/JAK2 in IFNgamma-induced human THP1 cells assessed as pSTAT1, =3.364μM. 25369270
TF1 Function assay Inhibition of JAK2 in IL3-induced human TF1 cells assessed as pSTAT5, =3.524μM. 25369270
BaF3 Function assay Inhibition of JAK2 in IL3-induced human BaF3 cells assessed as cell proliferation, =4.546μM. 25369270
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
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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]
(Cell-free assay)		 JAK2 [1]
(Cell-free assay)		 TYK2 [1]
(Cell-free assay)		 JAK3 [1]
(Cell-free assay)
10 nM 28 nM 116 nM 810 nM
In vitro
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-STAT3 / STAT3 28191885
In Vivo
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]
Animal Research Animal Models Rat CIA model and mouse CIA model
Dosages 30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06222034 Recruiting
Juvenile Idiopathic Arthritis
Galapagos NV
 April 2024 Phase 1
NCT06043739 Completed
Bioavailability
Galapagos NV
 September 22 2023 Phase 1
NCT05697159 Recruiting
Rheumatoid Arthritis|Sickness Behavior|Inflammatory Disease|Autoimmune|Pain Chronic
NHS Greater Glasgow and Clyde|Galapagos NV
 August 22 2023 --
NCT05653791 Active not recruiting
Ulcerative Colitis
Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Galapagos NV
 October 1 2022 --
NCT03417778 Completed
Rheumatoid Arthritis
Gilead Sciences|Galapagos NV
 April 3 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 425.50 Formula

C21H23N5O3S
CAS No. 1206161-97-8 SDF Download Filgotinib (GLPG0634) SDF
Smiles C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 21 mg/mL ( (49.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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Frequently Asked Questions

Question 1:
Could you recommemd a vehicle for oral gavage for S7605?

Answer:
It can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension for oral gavage.

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