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Filgotinib

Product Specifications

UNSPSC Description

Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease[1][2][3].

Target Antigen

HIV; JAK

Type

Reference compound

Related Pathways

Anti-infection;Epigenetics;JAK/STAT Signaling;Protein Tyrosine Kinase/RTK;Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GLPG0634.html

Purity

99.44

Solubility

DMSO : 25 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL

Smiles

O=C(C1CC1)NC2=NN3C(C4=CC=C(CN5CCS(CC5)(=O)=O)C=C4)=CC=CC3=N2

Molecular Weight

425.50

References & Citations

[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.|[3]Yeh, et al. "Filgotinib suppresses HIV-1–driven gene transcription by inhibiting HIV-1 splicing and T cell activation." The Journal of Clinical Investigation 130.9 (2020): 4969-4984.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-18300/Filgotinib-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-18300/Filgotinib-SDS-MedChemExpress.pdf

Clinical Information

Launched

CAS Number

1206161-97-8

Available Sizes

Curated Selection

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