Filgotinib(GLPG0634) chemical structure
Chemical structureResearch use only
CAT. NO. DC7137Featured

Filgotinib(GLPG0634)

Pack Sizes & Prices

TotalUS$300
We match the best price and quality on market.
Product overview

Description & Application

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.

ParameterValue
Chemical NameFilgotinib
CAS No.1206161-97-8
SynonymsFilgotinib;Filgotinib (GLPG0634);GLPG0634;GLPG-0634 (Filgotinib);GPLG0634;GPLG-0634;N-(5-(4-((1,1-Dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide;N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide;cyclopropanecarboxylic acid {5-[ 4-(1,1-dioxo-thiomorpholin-4-ylmethyl)-phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-amide;cyclopropanecarboxylic acid {5-[4-((1,1-dioxo-1-thimorpholin-4-yl)methyl)-phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-amide;GLPG-0634;N-[5-[4-[(1,1-Dioxido-4-thiomorpholinyl)methyl]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide;SYN1158;UNII-3XVL385Q0M;GLPG0634 （Filgotinib）;3XVL385Q0M;AK171369;Filgotinib [USAN:INN];GLPG 0634;N-(5-{4-[;Filgotinib(GLPG0634);G146034;N-(5-(4-((1,1-dioxido
FormulaC21H23N5O3S
M.Wt425.5
SMILESS1(C([H])([H])C([H])([H])N(C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])C2=C([H])C([H])=C([H])C3=NC(=NN23)N([H])C(C2([H])C([H])([H])C2([H])[H])=O)C([H])([H])C1([H])[H])(=O)=O
Purity98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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.

In Vitro

GLPG0634 dose-dependently inhibits the differentiation of Th2 cells mediated by IL-4, a cytokine that signals through JAK1 and JAK3. GLPG0634 also inhibits Th1 differentiation with similar potencies of 1 μM or lower[1]. GLPG0634 does not inhibit JAK2 homodimer-mediated signaling induced by EPO or PRL (IC50 > 10 μM)[2].

In Vivo

GLPG0634 (3, 10, 30 mg/kg, p.o.) dose-dependently prevents disease progression in the therapeutic rat CIA model. GLPG0634 (50 mg/kg, o.p.) protects bone and cartilage from degradation, effectively reduces infiltration of T cells (CD3+ cells) and macrophages (F4/80+ cells) in the paw, and decreases the serum levels of all cytokines and chemokines measured, including IL-6, IP-10, XCL1, and MCP-1[1]. GLPG0634 (0.1 and 0.3 mg/kg) shows efficacy in the rat CIA model[2].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

View online datasheetRequest COA / MSDS

Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Solution calculator

Related research products

AZD1480 chemical structureDC5032

AZD1480

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. IC50 value: 0.26 nM Target: JAK2 in vitro: AZD1480 demonstrated…

View activity & prices
BMS-911543 chemical structureDC4175

BMS-911543

BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively).

View activity & prices
JAK2 Inhibitor V,Z3 chemical structureDC7436

JAK2 Inhibitor V,Z3

JAK2 Inhibitor V, Z3 is a cell-permeable pyridinylbutanone compound that inhibits both JAK2 and the active V167F mutant cellular autophosphorylation. JAK2 Inhibitor V, Z3 displays no effect against cellular Tyk 2…

View activity & prices
TG101209 chemical structureDC7317

TG101209

TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.

View activity & prices

Cart

Request quotation