BIIB-057
货号：
17652-500ug 基本售价：
546.0 元 规格：
500 ug
产品信息
概述| 货号 | 17652-500ug |
| 描述 | BIIB-057 is a potent inhibitor of the non-receptor tyrosine kinase Syk (IC50 = 1 nM).1 It displays at least 80-fold selectivity for Syk over other kinases. BIIB-057 blocks B cell receptor-mediated cell signaling and activation in whole blood (IC50s = 0.27 and 0.28 µM, respectively), as well as Fcɛ receptor 1-mediated basophil degranulation (IC50 = 0.15 µM).1 It antagonizes chemokine production, cell migration, and survival of chronic lymphocytic leukemia (CLL) cells after B cell receptor activation and synergistically enhances the action of fludarabine (Item No. 14128) in killing CLL cells.2,3 BIIB-057 is orally bioavailable, as it produces dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis.1 It also prevents splenomegaly and inhibits non-Hodgkin lymphoma tumor growth in a xenograft model.3 |
| 别名 | P505-15;PRT062607;PRT2607; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Coffey, G.,DeGuzman, F.,Inagaki, M., et al. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. Journal of Pharmacology and Experimental Therapeutics 340(2), 350-359 (2012).
2.Hoellenriegel, J.,Coffey, G.P.,Sinha, U., et al. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia 26(7), 1576-1583 (2012).
3.Spurgeon, S.E.,Coffey, G.,Fletcher, L.B., et al. The selective Syk inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. Journal of Pharmacology and Experimental Therapeutics 344, 378-387 (2015).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 393.5 |
| 分子式 | C19H23N9O |
| CAS号 | 1370261-96-3 |
| 稳定性 | ≥ 2 years |
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