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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-Decernotinib
Decernotinib

Chemical Structure : Decernotinib

CAS No.: 944842-54-0

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

货号: 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).

规格 价格 库存 数量
2 mg (Free Sample) ￥280 In stock
5 mg ￥780 In stock
10 mg ￥1180 In stock
50 mg ￥2980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 392.3783
分子式 C18H19F3N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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)-

参考文献

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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