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Filgotinib

Catalog No. T1929 CAS 1206161-97-8

Synonyms: GLPG0634

Filgotinib (GLPG0634) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.

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Filgotinib, CAS 1206161-97-8

Pack Size	Availability	Price/USD
2 mg	In stock	$ 50.00
5 mg	In stock	$ 71.00
10 mg	In stock	$ 112.00
25 mg	In stock	$ 166.00
50 mg	In stock	$ 313.00
100 mg	In stock	$ 513.00
1 mL * 10 mM (in DMSO)	In stock	$ 71.00

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Purity: 99.42%

Purity: 98.03%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Filgotinib (GLPG0634) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.
Targets&IC50	JAK2:28 nM, JAK1:10 nM, TYK2:116 nM, JAK3:810 nM
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.
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.
Kinase Assay	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.

Synonyms	GLPG0634
Molecular Weight	425.5
Formula	C21H23N5O3S
CAS No.	1206161-97-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 79 mg/mL (185.7 mM)

References and Literature

1. Van Rompaey L, et al. J Immunol. 2013, 191(7), 3568-3577.

Citations

1. Vogel A, Martin K, Soukup K, et al. JAK1 signaling in dendritic cells promotes peripheral tolerance in autoimmunity through PD-L1-mediated regulatory T cell induction. Cell Reports. 2022, 38(8): 110420. 2. Si H, Wang J, He R, et al. Identification of U937JAK3-M511I Acute Myeloid Leukemia Cells as a Sensitive Model to JAK3 Inhibitor. Frontiers in oncology. 2021, 11: 807200-807200.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Inhibitor Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library FDA-Approved Kinase Inhibitor Library Anti-Liver Cancer Compound Library

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Related compounds with same targets

Vidarabine Ruxolitinib SAR-20347 Beta-Hydroxyisovalerylshikonin RO495 BMS-911543 BMS-066 Gefitinib

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Keywords

Filgotinib 1206161-97-8 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors JAK Tyrosine Kinases inhibit Janus kinase GLPG 0634 GLPG0634 Inhibitor GLPG-0634 inhibitor

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