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GLPG3667

Chemical Structure : GLPG3667

CAS No.: 2308520-97-8

GLPG3667 (GLPG 3667, GLPG-3667)

Catalog No.: PC-22404Not For Human Use, Lab Use Only.

GLPG3667 is a potent, reversible and selective, ATP-competitive TYK2 inhibitor with IC50 of 2.3 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GLPG3667 is a potent, reversible and selective, ATP-competitive TYK2 inhibitor with IC50 of 2.3 nM.
GLPG3667 is a selective TYK2 inhibitor in human PBMC and whole blood assays.
GLPG3667 shows dose-dependent inhibition of IFNα-induced STAT1 phosphorylation (JAK1/TYK2-dependent, IC50=70 nM), IL-2-induced STAT5 phosphorylation (JAK1/JAK3-dependent) and granulocyte macrophage colony-stimulating factor (GM-CSF)-induced STAT5 phosphorylation (JAK2-dependent).
GLPG3667 displays general kinase selectivity against a panel of 365 kinases.
GLPG3667 reduced dermal ear inflammation in an IL-23-induced in vivo mouse model of psoriasis.

Physicochemical Properties

M.Wt 443.47
Formula C22H21N9O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO

Chemical Name/SMILES

4-methyl-5-((3-methyl-7-((6-morpholinopyridazin-3-yl)amino)-3H-imidazo[4,5-b]pyridin-5-yl)oxy)picolinonitrile

References

1. Mammoliti O, et al. J Med Chem. 2024 May 28. doi: 10.1021/acs.jmedchem.4c00769.

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