Filgotinib

SKU: orb1307080

Description

Filgotinib

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Infectious Disease & Virology, Protein Biochemistry, Signal Transduction, 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	99.76%
Formula	C₂₁H₂₃N₅O₃S
SMILES	O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1
Target	JAK,Tyrosine Kinases,HIV Protease
Solubility	Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.7 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:50 mg/mL (117.51 mM)

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 inhibit the signaling of JAK1/JAK3/γc induced by IL-2/4 an 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 a the cellular level. Additionally, GLPG0634 inhibit the differentiation of Th1/2/17 cells. Read more...
In Vitro	in vivo studies on mice treated with DSS demonstrate that Filgotinib (GLPG0634), throug the Inhibition of JAK1, exhibits potent efficacy in preclinical mouse models, which is associated wit 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	keep away from direct sunlight,keep away from moisture,store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Tyrosine Kinases, TyrosineKinases, Tyk2, Inhibitor, GLPG 0634, GLPG0634, GLPG-0634, Filgotinib, JAK3, Janus kinase, JAK, JAK1, JAK2, inhibit

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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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Filgotinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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