| 货号 | 11423-1mg |
| 描述 | BAY 61-3606 is a cell-permeable, reversible inhibitor of spleen tyrosine kinase (Syk; Ki = 7.5 nM; IC50 = 10 nM). It is 700 to >1,000-fold more selective for Syk over Src, Lyn, Fyn, Itk, and Btk.1,2,3 BAY 61-3606 can inhibit degranulation (IC50 = 5-46 nM) and block cytokine release from mast cells.1 At 3 mg/kg, oral administration of BAY 61-3606 to rats was shown to suppress antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema.1 It can also sensitize MCF-7 breast cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis by inhibiting Cdk9.4 This compound has been used in a pre-clinical model to explore the feasibility of targeting Syk in the treatment of retinoblastoma.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Yamamoto, N.,Takeshita, K.,Shichijo, M., et al. The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents. Journal of Pharmacology and Experimental Therapeutics 306(3), 1174-1181 (2003). 2.Fedorov, O.,Marsden, B.,Pogacic, V., et al. A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proceedings of the National Academy of Sciences of the United States of America 104(51), 20523-20528 (2007). 3.Knight, Z.A., and Shokat, K.M. Features of selective kinase inhibitors. Chemistry & Biology 12(6), 621-637 (2005). 4.Kim, S.Y.,Park, S.E.,Shim, S.M., et al. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells. PLoS One 10(12), (2016). 5.Zhang, J.,Benavente, C.A.,McEvoy, J., et al. A novel retinoblastoma therapy from genomic and epigenetic analyses. Nature 481, 329-334 (2012). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 426.9 |
| 分子式 | C20H18N6O3 • HCl |
| CAS号 | 1615197-10-8 |
| 稳定性 | ≥ 2 years |
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