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Filgotinib

Chemical Structure : Filgotinib

CAS No.: 1206161-97-8

Filgotinib (GLPG0634, GLPG-0634)

Catalog No.: PC-45448Not For Human Use, Lab Use Only.

Filgotinib (GLPG 0634) is a potent JAK1/JAK2 inhibitor with IC50 of 10 nM/28 nM in biochemical assays, less potent for JAK3 and TYK2.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Filgotinib (GLPG 0634) is a potent JAK1/JAK2 inhibitor with IC50 of 10 nM/28 nM in biochemical assays, less potent for JAK3 and TYK2.
Filgotinib (GLPG 0634) shows a selectivity of 30-fold for JAK1- over JAK2-dependent signaling in cellular and whole blood assays.
Filgotinib (GLPG 0634) inhibits Th1 and Th2 differentiation and to a lesser extent the differentiation of Th17 cells in vitro。
Filgotinib (GLPG 0634) shows efficacy in the collagen-induced arthritis models and is orally active.

Physicochemical Properties

M.Wt 425.504
Formula C21H23N5O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: 6.8 mg/mL

Chemical Name/SMILES

Cyclopropanecarboxamide, N-[5-[4-[(1,1-dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-

References

1. Menet CJ, et al. J Med Chem. 2014 Nov 26;57(22):9323-42.

2. Van Rompaey L, et al. J Immunol. 2013 Oct 1;191(7):3568-77.

3. Chen H, et al. Sci Rep. 2016 Jul 26;6:30459.

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