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Purity: ≥98%
Filgotinib (also known as GLPG0634; GLPG-0634; Jyseleca) is a novel, potent and selective JAK1 (Janus kinase) inhibitor with potential anti-inflammatory activity. As of 2020, it was approved as a medication for the treatment of rheumatoid arthritis. Filgotinib inhibits JAK1, JAK2, JAK3, and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM, and 116 nM, respectively. It is currently being investigated for the treatment of rheumatoid arthritis (RA) and Crohn's disease. It is considered to be a promising drug candidate for treating autoimmune diseases by selectively inhibiting JAK1. In cellular assays, GLPG0634 is most potent in inhibiting the JAK1/JAK3/γc signaling induced by IL-2– and IL-4 as well as the JAK1/TYK2 type II receptor signaling induced by IFN-αB2. However, it shows lower potent to inhibit JAK2 homodimer–mediated signaling induced by EPO or PRL. In addition, GLPG0634 is found to inhibit the phosphorylation of STAT1 and STAT5 induced by cytokines.
| ln Vitro |
Th2 cell differentiation mediated by IL-4, a cytokine that signals through JAK1 and JAK3, is dose-dependently inhibited by filgotinib (GLPG0634). Moreover, filgotinib also inhibits Th1 differentiation at 1 μM or less in potency [1]. JAK2 homodimer-mediated signaling generated by PRL or EPO (IC50 > 10 μM) is not inhibited by filgotinib (GLPG0634) [2].
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| ln Vivo |
In a rat CIA model that has been modified, filgotinib (GLPG0634; 3, 10, 30 mg/kg, po) dose-dependently inhibits the course of the disease. Filgotinib (50 mg/kg, op) inhibits the deterioration of bone and cartilage, effectively decreases the infiltration of T cells (CD3+ cells) and macrophages (F4/80+ cells) in the paw, and lowers blood levels of cytokines and chemokines, such as IL-6, IP-10, XCL1, and MCP-1[1]. In a rat model of CIA, filgotinib (GLPG0634; 0.1 and 0.3 mg/kg) demonstrated effectiveness [2].
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| References |
[1]. Van Rompaey L, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013, 191(7), 3568-3577.
[2]. Menet CJ, et al. Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634. J Med Chem. 2014 Nov 17 |
| Molecular Formula |
C21H23N5O3S
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|---|---|
| Molecular Weight |
425.50
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| CAS # |
1206161-97-8
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| Related CAS # |
GLPG0634 analog;1206101-20-3;Filgotinib maleate;1802998-75-9;Filgotinib-d4;2041095-50-3
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| SMILES |
O=C(C1CC1)NC2=NN3C(C4=CC=C(CN5CCS(CC5)(=O)=O)C=C4)=CC=CC3=N2
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| Chemical Name |
N-(5-(4-((1,1-dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide.
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| Synonyms |
GLPG-0634; PubChemSID 163643231; GLPG0634; GLPG 0634; Filgotinib
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05817942 | Recruiting | Drug: Filgotinib | Ulcerative Colitis | Galapagos NV | June 12, 2023 | |
| NCT05323591 | Recruiting | Drug: Filgotinib | Rheumatoid Arthritis | Galapagos NV | May 3, 2022 | |
| NCT04871919 | Recruiting | Drug: Filgotinib | Rheumatoid Arthritis | Galapagos NV | May 11, 2021 | |
| NCT05785611 | Recruiting | Drug: Filgotinib Drug: Placebo |
Axial Spondyloarthritis | Galapagos NV | April 5, 2023 | Phase 3 |
GLPG0634 inhibits the differentiation of Th1, Th2, and Th17 cells.J Immunol.2013 Oct 1;191(7):3568-77. |
GLPG0634 dose-dependently prevents disease progression in the therapeutic rat CIA model.J Immunol.2013 Oct 1;191(7):3568-77. |
GLPG0634 is efficacious in a mouse therapeutic CIA model.J Immunol.2013 Oct 1;191(7):3568-77. |
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