| 货号 | 17259-1mg |
| 描述 | Tyrphostins are tyrosine phosphorylation inhibitors that act by inhibiting tyrosine kinases.1 AG957 is a tyrphostin that targets transforming Bcr-Abl fusion proteins (p185Bcr-Abl, p210Bcr-Abl), as well as normal c-Abl (IC50s = 4.3, 1, and 7.1 µM, respectively, for human proteins).2 It also inhibits epidermal growth factor receptor (IC50 = 0.25 µM).2 As the constitutively-active 210 kDa Bcr-Abl fusion protein commonly occurs in chronic myelogenous leukemia (CML) cells, AG957 is commonly used to study Bcr-Abl signaling in the CML K562 cell line.3,4 AG957 is also used to study signaling through c-Abl.5 |
| 别名 | NSC 654705;Tyrphostin AG957; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Levitzki, A., and Gazit, A. Tyrosine kinase inhibition: An approach to drug development. Science 267(5205), 1782-1788 (1995). 2.Anafi, M.,Gazit, A.,Gilon, C., et al. Selective interactions of transforming and normal abl proteins with ATP, tyrosine-copolymer substrates, and tyrphostins. The Journal of Biological Chemisty 267(8), 4518-4523 (1992). 3.Kaur, G.,Gazit, A.,Levitzki, A., et al. Tyrphostin induced growth inhibition: correlation with effect on p210bcr-abl autokinase activity in K562 chronic myelogenous leukemia. Anti-Cancer Drugs 5, 213-222 (1994). 4.Jamieson, L.,Carpenter, L.,Biden, T.J., et al. Protein kinase Cι activity is necessary for Bcr-Abl-mediated resistance to drug-induced apoptosis. The Journal of Biological Chemisty 274(7), 3927-3930 (1999). 5.Fu, P.,Usatyuk, P.V.,Lele, A., et al. c-Abl mediated tyrosine phosphorylation of paxillin regulates LPS-induced endothelial dysfunction and lung injury. American Journal of Physiology.Regulatory, Integrative and Comparative Physiology 308, L1025-L1038 (2015). | |
| 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 | 273.3 |
| 分子式 | C15H15NO4 |
| CAS号 | 140674-76-6 |
| 稳定性 | ≥ 2 years |
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