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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Cited by 4 Publications

2 Customer Reviews

  • Confocal microscopy showing BAFF in ductal epithelial structures within SG organoids from patients with sicca (Sc) or primary Sjögren's syndrome (SS). Nuclei were stained with DAPI (blue). Original magnification × 100.

    Arthritis Rheumatol, 2018, 70(12):2057-2066. Filgotinib (GLPG0634) purchased from Selleck.

    Treatment of IL-6 (10 ng/ml) with or without S3I-201 (a STAT3 antagonist, 5 μM) or filgotinib (a JAK1 inhibitor, 10 nM). Mean ± SEM, n = 6. *, **,*** indicate significant difference between two groups when compared to the control at P < 0.05, 0.01, 0.001, respectively.

    Mol Cell Endocrinol, 2018, 472:26-39. Filgotinib (GLPG0634) purchased from Selleck.

Purity & Quality Control

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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 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CD34+ cells M3nDb2Z2dmO2aX;uJIF{e2G7 NGf3S4g1PSCvaX7z NFrQ[4tKdmirYnn0bY9vKG:oIFrBT|IhcG:vb3TpcYVzKGmwIHj1cYFvKEOGM{SrJINmdGy|IIPwbYtm\CCrboTvJIh2dWGwIIfoc4xmKGKub3;kJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSXBQNWmwZIXj[YQhW1SDVD21JJBpd3OyaH;yfYxifGmxbjDwdoVqdmO3YnH0[YQh\m:{IES1JI1qdnNiZn;scI94\WRiYomgSXBQKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFE2KG2rboOgZpkhTkGFUzDhcoFtgXOrcx?= MWqyOFQyPzV|Mx?=

... Click to View More Cell Line Experimental Data

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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
3mg/mL

* 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
NCT03417778 Completed Rheumatoid Arthritis|Ulcerative Colitis|Crohn''s Disease Gilead Sciences|Galapagos NV April 3 2018 Phase 1
NCT03417778 Completed Rheumatoid Arthritis|Ulcerative Colitis|Crohn''s Disease Gilead Sciences|Galapagos NV April 3 2018 Phase 1
NCT03285711 Active not recruiting Lupus Membranous Nephropathy Gilead Sciences October 6 2017 Phase 2
NCT03285711 Active not recruiting Lupus Membranous Nephropathy Gilead Sciences October 6 2017 Phase 2
NCT03320876 Active not recruiting Psoriatic Arthritis Galapagos NV July 26 2017 Phase 2
NCT03207815 Recruiting Noninfectious Uveitis Gilead Sciences July 26 2017 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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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.

JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID