[CAS NO. 1206161-97-8] Filgotinib (GLPG0634)

Name: Filgotinib (GLPG0634)
Brand: Arctom Scientific
SKU: SLK-S7605

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PRODUCTS SPECIFICATIONS [1206161-97-8]

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Catalog

SLK-S7605

Brand

Selleck

CAS

1206161-97-8

DESCRIPTION [1206161-97-8]

Overview

MDL	MFCD20527867
Molecular Weight	425.50
Molecular Formula	C21H23N5O3S
SMILES	N(C(=O)C1CC1)C2=NN3C(=CC=CC3=N2)C4=CC=C(CN5CCS(=O)(=O)CC5)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3502 mL	11.7509 mL	23.5018 mL
5 mM	0.4700 mL	2.3502 mL	4.7004 mL
10 mM	0.2350 mL	1.1751 mL	2.3502 mL
50 mM	0.0470 mL	0.2350 mL	0.4700 mL

Description

Filgotinib (GLPG0634) is a selective inhibitor with of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.

Targets

JAK1 ^[1] (Cell-free assay)	JAK2 ^[1] (Cell-free assay)	TYK2 ^[1] (Cell-free assay)	JAK3 ^[1] (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. 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.

References

[1] Van Rompaey L, et al. J Immunol. 2013, 191(7), 3568-3577.
[2] Merciris D, et al. ECCO. 2014, P072.

Synonyms

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

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

Filgotinib

G 146034

GLPG 0634

GLP0634