Filgotinib

SKU: orb1307080

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Description

Filgotinib (GLPG0634) is a potent and selective Janus kinase 1 (JAK1) inhibitor, exhibiting IC50 values of 10 nM, 28 nM, 810 nM, and 116 nM against JAK1, JAK2, JAK3, and TYK2, respectively. This small molecule is a valuable research tool for investigating JAK-STAT signaling in inflammatory and autoimmune disease models, both in vitro and in vivo.

Research Area

Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	1206161-97-8
MW	425.5
Purity	>98%
Formula	C₂₁H₂₃N₅O₃S
SMILES	O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1
Target	Kinase
Solubility	Soluble in DMSO (15 mg/ml, warm)

Bioactivity

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Target IC50	TYK2:116 nM\|JAK1:10 nM\|JAK2:28 nM\|JAK3:810 nM
In Vivo	In cell lines, GLPG0634 inhibits the signaling of JAK1/JAK3/γc induced by IL-2/4 and the signaling of JAK1/TYK2 Type II receptor induced by IFN-αB2, with an IC50 of 150-760 nM. Compared to JAK1 kinase in the JAK/STAT signaling pathway, GLPG0634 exhibits higher selectivity for JAK2 kinase at the cellular level. Additionally, GLPG0634 inhibits the differentiation of Th1/2/17 cells. Read more...
In Vitro	In vivo studies on mice treated with DSS demonstrate that Filgotinib (GLPG0634), through the inhibition of JAK1, exhibits potent efficacy in preclinical mouse models, which is associated with the inhibition of STAT3 phosphorylation in inflamed colonic tissues. Oral administration of Filgotinib shows moderate absolute bioavailability in rats (45%) and high bioavailability in mice (~100%). In both rat and mouse CIA models, Filgotinib (30 mg/kg/day in rats; 50 mg/kg, twice per day in mice) demonstrates a dose-dependent reduction in cartilage damage, inflammation, and bone degeneration phenomena. Read more...

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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GLPG0634; GS-6034

Quality Guarantee

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Compound Identifiers

PubChem CID

49831257 ↗

Key Properties

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No computed properties available.

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Filgotinib (orb1307080)

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CAS Number:	1802998-75-9
MW:	541.58
Formula:	C₂₅H₂₇N₅O₇S

Purity:	97.87% (May vary between batches)
CAS Number:	3067170-12-8
MW:	371.39
Formula:	C₂₁H₁₇N₅O₂

CAS Number:	1540859-07-1
MW:	516.01
Formula:	C₂₁H₃₀ClN₅O₆S

Purity:	99.78% (May vary between batches)
CAS Number:	1257705-09-1
MW:	357.43
Formula:	C₁₇H₁₉N₅O₂S

Purity:	>98% (HPLC)
CAS Number:	1206101-20-3
MW:	425.5
Formula:	C₂₁H₂₃N₅O₃S

Filgotinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Key Properties

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Filgotinib (orb1307080)

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