Filgotinib

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].

Product Specifications

CAS Number

[1206161-97-8]

Product Name Alternative

GLPG0634

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

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 Formula

C21H23N5O3S

Molecular Weight

425.50

Precautions

H302, H315, H319, H335

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.