1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK

GLPG0634 (Synonyms: Filgotinib)

Cat. No.: HY-18300 Purity: 99.64%
Data Sheet SDS Handling Instructions

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.

For research use only. We do not sell to patients.
GLPG0634 Chemical Structure

GLPG0634 Chemical Structure

CAS No. : 1206161-97-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $77 In-stock
5 mg $70 In-stock
10 mg $110 In-stock
25 mg $180 In-stock
50 mg $280 In-stock
100 mg $480 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of GLPG0634:

    GLPG0634 purchased from MCE. Usage Cited in: J Immunol. 2016 May 15;196(10):4322-30.

    HEK293T (IRF3-BiLC) cells are pretreated with TPCA-1 for 1 h, stimulated with TNF-α for 12 h, and then transfected with poly(I:C) for 12 h, after which IRF3-BiLC luciferase activity is measured.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    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.

    IC50 & Target

    IC50: 10 nM (JAK1), 28 nM (JAK2), 810 nM (JAK3), 116 nM (Tyk2)

    In Vitro

    GLPG0634 dose-dependently inhibits the differentiation of Th2 cells mediated by IL-4, a cytokine that signals through JAK1 and JAK3. GLPG0634 also inhibits Th1 differentiation with similar potencies of 1 μM or lower[1]. GLPG0634 does not inhibit JAK2 homodimer-mediated signaling induced by EPO or PRL (IC50 > 10 μM)[2].

    In Vivo

    GLPG0634 (3, 10, 30 mg/kg, p.o.) dose-dependently prevents disease progression in the therapeutic rat CIA model. GLPG0634 (50 mg/kg, o.p.) protects bone and cartilage from degradation, effectively reduces infiltration of T cells (CD3+ cells) and macrophages (F4/80+ cells) in the paw, and decreases the serum levels of all cytokines and chemokines measured, including IL-6, IP-10, XCL1, and MCP-1[1]. GLPG0634 (0.1 and 0.3 mg/kg) shows efficacy in the rat CIA model[2].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT03117270 Galapagos NV Ankylosing Spondylitis March 7, 2017 Phase 2
    NCT03025308 Gilead Sciences|Galapagos NV RheumatoId Arthritis February 28, 2017 Phase 3
    NCT02914600 Gilead Sciences|Galapagos NV Crohn's Disease March 17, 2017 Phase 3
    NCT02914535 Gilead Sciences|Galapagos NV Ulcerative Colitis February 23, 2017 Phase 3
    NCT03077412 Gilead Sciences|Galapagos NV Fistulizing Crohn's Disease April 6, 2017 Phase 2
    NCT03046056 Gilead Sciences|Galapagos NV Small Bowel Crohn's Disease April 11, 2017 Phase 2
    NCT03207815 Gilead Sciences Non-infectious Uveitis August 2017 Phase 2
    NCT03101670 Galapagos NV Psoriatic Arthritis March 9, 2017 Phase 2
    NCT02914561 Gilead Sciences|Galapagos NV Crohn's Disease October 2016 Phase 3
    NCT02914522 Gilead Sciences|Galapagos NV Ulcerative Colitis November 14, 2016 Phase 3
    NCT02873936 Gilead Sciences|Galapagos NV Rheumatoid Arthritis July 2016 Phase 3
    NCT02886728 Gilead Sciences|Galapagos NV Rheumatoid Arthritis August 2016 Phase 3
    NCT03201445 Gilead Sciences|Galapagos NV Ulcerative Colitis July 11, 2017 Phase 2
    NCT03134222 Gilead Sciences|Galapagos NV Cutaneous Lupus Erythematosus May 24, 2017 Phase 2
    NCT02889796 Gilead Sciences|Galapagos NV Rheumatoid Arthritis August 2016 Phase 3
    NCT02065700 Gilead Sciences|Galapagos NV Rheumatoid Arthritis February 2014 Phase 2
    NCT03100942 Gilead Sciences|Galapagos NV Sjogren's Syndrome May 1, 2017 Phase 2
    NCT02885181 Gilead Sciences Rheumatoid Arthritis September 21, 2016 Phase 2
    NCT02048618 Galapagos NV Crohn's Disease February 2014 Phase 2
    NCT01915667 Galapagos NV Healthy July 2013 Phase 1
    NCT01798979 Galapagos NV Healthy February 2013 Phase 1
    NCT01820806 Galapagos NV Healthy March 2013 Phase 1
    NCT02084199 Galapagos NV Renal Impairment March 2014 Phase 1
    NCT02162355 Galapagos NV Healthy June 2014 Phase 1
    NCT01665924 Galapagos NV Healthy July 2012 Phase 1
    NCT01419990 Galapagos NV Healthy August 2011 Phase 1
    NCT01894516 Galapagos NV Rheumatoid Arthritis July 2013 Phase 2
    NCT01668641 Galapagos NV Rheumatoid Arthritis May 2012 Phase 2
    NCT01888874 Galapagos NV Rheumatoid Arthritis July 2013 Phase 2
    NCT01384422 Galapagos NV Rheumatoid Arthritis June 2011 Phase 2
    NCT01179581 Galapagos NV Healthy August 2010 Phase 1
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.3502 mL 11.7509 mL 23.5018 mL
    5 mM 0.4700 mL 2.3502 mL 4.7004 mL
    10 mM 0.2350 mL 1.1751 mL 2.3502 mL
    Kinase Assay
    [1]

    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× the experimental Km value and the substrate concentration (ULight-conjugated JAK-1(Tyr1023) peptide) corresponds 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    GLPG0634 is formulated in polyethyleneglycol 200/0.9% NaCl (60/40; v/v) for i.v. administration and in 0.5% (v/v) methylcellulose for oral administration.

    GLPG0634 is orally dosed as a single esophageal gavage at 5 mg/kg (dosing volume of 5 mL/kg) and i.v. dosed as a bolus via the caudal vein at 1 mg/kg (dosing volume of 5 mL/kg). In the rat study, each group consists of three rats and blood samples are collected via the jugular vein. In the mouse study, each group consists of 21 mice (n=3/time point) and blood samples are collected by intracardiac puncture under isoflurane anesthesia. Lithium heparin is used as anticoagulant and blood is taken at 0.05, 0.25, 0.5, 1, 3, 5, and 8 h (i.v. route) and 0.25, 0.5, 1, 3, 5, 8, and 24 h (by mouth). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    425.5

    Formula

    C₂₁H₂₃N₅O₃S

    CAS No.

    1206161-97-8

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 6.8 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.64%

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    Product Name:
    GLPG0634
    Cat. No.:
    HY-18300
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