Filgotinib (GLPG0634) - 10mM in DMSO, high purity , CAS No.1206161-97-8

Item Number

F420902

• Synonyms: 1206101-20-3 | Filgotinib | GLPG0634 | 1206161-97-8 | N-(5-(4-((1,1-dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide | GLPG-0634 | Filgotinib(GLPG0634) | Filgotinib (GLPG0634) | N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]
• Specifications & Purity: Moligand™, 10mM in DMSO
• Biochemical and Physiological Mechanisms: Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™

Product Description

Information

Filgotinib (GLPG0634) is a selectiveJAK1inhibitor withIC50of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.

Targets

JAK1 (Cell-free assay); JAK2 (Cell-free assay); TYK2 (Cell-free assay); JAK3 (Cell-free assay) 10 nM; 28 nM; 116 nM; 810 nM

In vitro

In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells.

In vivo

Following oral administration, the absolute bioavailability is moderate in rats (45%) and high in mice (∼100%). Filgotinib (30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)) dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice.\xa0 Filgotinib (GLPG0634) in DSS-treated mice demonstrates that inhibition of JAK1 is sufficient for achieving strong efficacy in pre-clinical mouse model, correlated to the inhibition of STAT3 phosphorylation in the inflamed colon.