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Chemical Structure : Decernotinib
CAS No.: 944842-54-0
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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|---|---|---|---|
| 5 mg | $95 | In stock | |
| 25 mg | $265 | In stock | |
| 100 mg | $725 | In stock | |
| 250 mg | Get quote |
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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); also inhibits JAK1, JAK2 and TYK2 (Ki=11, 13 and 11 nM) in biochemical assay and shows >400-fold selectivity over a broad kinases; 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; modulates proinflammatory response in models of immune-mediated diseases, such as collagen-induced arthritis and delayed-type hypersensitivity.
Rheumatoid Arthritis
Phase 2 Discontinued
| M.Wt | 392.3783 | |
| Formula | C18H19F3N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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)- |
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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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