Filgotinib (GLPG0634) 1206161-97-8

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight:

425.50 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.


Biological Activity


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.


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. 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.


Biochemical assays IC50 determination


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-fold the experimental Km value and
the substrate concentration (ULight-conjugated JAK-1(Tyr1023) peptide)
corresponded 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.

Contact us if you need more details on 1206161-97-8. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Filgotinib 1206161-97-8、GLPG0634 1206161-97-8. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Epigenetics > JAK Inhibitor