Decernotinib(VX-509)
Decernotinib(VX-509) may potently inhibits JAK3 in enzyme assays (Ki = 2.5 nM + 0.7 nM) and cellular assays dependent on JAK3 activity (IC50 range, 50-170 nM), with limited or no measurable potency against other JAK isotypes or non-JAK kinases. VX-509 also showed activity in two animal models of aberrant immune function. VX-509 treatment resulted in dose-dependent reduction in ankle swelling and paw weight and improved paw histopathology scores in the rat collagen-induced arthritis model. In a mouse model of oxazolone-induced delayed-type hypersensitivity, VX-509 reduced the T cell-mediated inflammatory response in skin. These findings demonstrate that VX-509 is a selective and potent inhibitor of JAK3 in vitro and modulates proinflammatory response in models of immune-mediated diseases, such as collagen-induced arthritis and delayed-type hypersensitivity. The data support evaluation of VX-509 for treatment of patients with autoimmune and inflammatory diseases such as rheumatoid arthritis.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | Decernotinib(VX-509) |
|---|---|
| Iupac 化学名称 | (R)-2-((2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)-2-methyl-N-(2,2,2-trifluoroethyl)butanamide |
| 同义词 | Decernotinib;VX-509;VX509;VX 509 |
| 英文同义词 | Decernotinib;VX-509;VX509;VX 509 |
| 分子式 | C18H19F3N6O |
| 分子量 | 392.38 |
| Smile | CC[C@@](C)(NC1=NC(C2=CNC3=NC=CC=C32)=NC=C1)C(NCC(F)(F)F)=O |
| InChiKey | ASUGUQWIHMTFJL-QGZVFWFLSA-N |
| InChi | InChI=1S/C18H19F3N6O/c1-3-17(2,16(28)25-10-18(19,20)21)27-13-6-8-23-15(26-13)12-9-24-14-11(12)5-4-7-22-14/h4-9H,3,10H2,1-2H3,(H,22,24)(H,25,28)(H,23,26,27)/t17-/m1/s1 |
| Cas号 | 944842-54-0 |
| 相关CAS号 |
订购信息
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|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
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