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Decernotinib

Chemical Structure : Decernotinib

CAS No.: 944842-54-0

Decernotinib (VX-509, VRT-831509, VX509, VRT831509)

Catalog No.: PC-43049Not For Human Use, Lab Use Only.

Decernotinib (VX-509, VRT-831509) is a potent, selective, orally available JAK3 inhibitor with Ki of 2.5 nM and cellular IC50 of 50-170 nM, demonstrates limited inhibition of JAK1/JAK2/TYK2 in cell-based assays (25-100 fold).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Decernotinib (VX-509, VRT-831509) is a potent, selective, orally available JAK3 inhibitor with Ki of 2.5 nM and cellular IC50 of 50-170 nM, demonstrates limited inhibition of JAK1/JAK2/TYK2 in cell-based assays (25-100 fold).
Decernotinib also inhibits JAK1, JAK2 and TYK2 (Ki=11, 13 and 11 nM) in biochemical assay and shows >400-fold selectivity over a broad kinases.
Decernotinib inhibits IL-2–induced STAT-5 phosphorylation in IL-2–dependent T-cell line with IC50 of 99 nM, potently suppresses T-cell proliferation with IC50 of 170 nM.
Decernotinib modulates proinflammatory response in models of immune-mediated diseases, such as collagen-induced arthritis and delayed-type hypersensitivity.

Physicochemical Properties

M.Wt 392.3783
Formula C18H19F3N6O
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
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Butanamide, 2-methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)-4-pyrimidinyl]amino]-N-(2,2,2-trifluoroethyl)-, (2R)-

References

1. Farmer LJ, et al. J Med Chem. 2015 Sep 24;58(18):7195-216.

2. Mahajan S, et al. J Pharmacol Exp Ther. 2015 May;353(2):405-14.

3. Genovese MC, et al. Arthritis Rheumatol. 2016 Jan;68(1):46-55.

4. Genovese MC, et al. Ann Rheum Dis. 2016 Nov;75(11):1979-1983.

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