| 货号 | 11422-25mg |
| 描述 | R406 is a potent ATP-competitive inhibitor of spleen tyrosine kinase (Syk, Ki = 30 nM).1 Through this action, R406 blocks FcεRI-dependent mast cell activation (EC50 = 43 nM) and, at 3 μM, reduces the release of IL-10, -12, and -13 by immune complex-pulsed dendritic cells.1,2 R406 is orally available and can reduce immune complex-mediated inflammation.3 In cancers characterized by over-expression of Syk, R406 can prevent signaling downstream of Syk and induce apoptosis.4,5 R406 also inhibits Syk-dependent signaling through c-Jun N-terminal kinase in rheumatoid arthritis synoviocytes, suggesting a therapeutic intervention in this autoimmune disease.6,7 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Matsubara, S.,Li, G.,Takeda, K., et al. Inhibition of spleen tyrosine kinase prevents mast cell activation and airway hyperresponsiveness. American Journal of Respiration and Critical Care Medicine 173(1), 56-63 (2006). 2.Matsubara, S.,Koya, T.,Takeda, K., et al. Syk activation in dendritic cells is essential for airway hyperresponsiveness and inflammation. American Journal of Respiration, Cell, and Molecular Biology 34(4), 426-433 (2006). 3.Braselmann, S.,Taylor, V.,Zhao, H., et al. R406, an orally available spleen tyrosine kinase inhibitor blocks Fc receptor signaling and reduces immune complex-mediated inflammation. Journal of Pharmacology and Experimental Therapeutics 319(3), 998-1008 (2006). 4.Buchner, M.,Fuchs, S.,Prinz, G., et al. Spleen tyrosine kinase is overexpressed and represents a potential therapeutic target in chronic lymphocytic leukemia. Cancer Research 69(13), 5424-5432 (2009). 5.Zhang, J.,Benavente, C.A.,McEvoy, J., et al. A novel retinoblastoma therapy from genomic and epigenetic analyses. Nature 481, 329-334 (2012). 6.Cha, H.S.,Boyle, D.L.,Inoue, T., et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. Journal of Pharmacology and Experimental Therapeutics 317(2), 571-578 (2006). 7.Singh, R.,Masuda, E.S. and Payan, D.G. Discovery and development of spleen tyrosine kinase (SYK) inhibitors. Journal of Medicinal Chemistry 55(8), 3614-3643 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 470.5 |
| 分子式 | C22H23FN6O5 |
| CAS号 | 841290-80-0 |
| 稳定性 | ≥ 2 years |
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