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Filgotinib

SKU: orb1307080
FeaturedFeatured Product

Description

Filgotinib (GLPG0634) is a potent and selective Janus kinase 1 (JAK1) inhibitor, exhibiting IC50 values of 10 nM, 28 nM, 810 nM, and 116 nM against JAK1, JAK2, JAK3, and TYK2, respectively. This small molecule is a valuable research tool for investigating JAK-STAT signaling in inflammatory and autoimmune disease models, both in vitro and in vivo.

Research Area

Stem Cell & Developmental Biology

Images & Validation

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Filgotinib

Key Properties

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CAS Number1206161-97-8
MW425.5
Purity>98%
FormulaC21H23N5O3S
SMILESO=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1
TargetKinase
SolubilitySoluble in DMSO (15 mg/ml, warm)

Bioactivity

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Target IC50
TYK2:116 nM|JAK1:10 nM|JAK2:28 nM|JAK3:810 nM
In Vivo
In cell lines, GLPG0634 inhibits the signaling of JAK1/JAK3/γc induced by IL-2/4 and the signaling of JAK1/TYK2 Type II receptor induced by IFN-αB2, with an IC50 of 150-760 nM. Compared to JAK1 kinase in the JAK/STAT signaling pathway, GLPG0634 exhibits higher selectivity for JAK2 kinase at the cellular level. Additionally, GLPG0634 inhibits the differentiation of Th1/2/17 cells.
In Vitro
In vivo studies on mice treated with DSS demonstrate that Filgotinib (GLPG0634), through the inhibition of JAK1, exhibits potent efficacy in preclinical mouse models, which is associated with the inhibition of STAT3 phosphorylation in inflamed colonic tissues. Oral administration of Filgotinib shows moderate absolute bioavailability in rats (45%) and high bioavailability in mice (~100%). In both rat and mouse CIA models, Filgotinib (30 mg/kg/day in rats; 50 mg/kg, twice per day in mice) demonstrates a dose-dependent reduction in cartilage damage, inflammation, and bone degeneration phenomena.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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GLPG0634; GS-6034

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Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
49831257 ↗

Key Properties

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No computed properties available.

Protocol Information

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5 mg
$ 200.00
25 mg
$ 380.00
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