| 货号 | 10010422-5mg |
| 描述 | Nilotinib is a second generation tyrosine kinase inhibitor that is reported to have been used in targeted therapy for cancer. Specifically, it potently inhibits Bcr/Abl tyrosine kinase and is effective in the treatment of chronic myeloid leukemia (MLL) or Philadelphia chromosome acute lymphoblastic leukemia (Ph+ ALL), even in patients who are resistant to the first generation drug, imatinib (Gleevec).1,2,3,4 Nilotinib is ~20-fold more potent than imatinib in inhibiting both wild-type and mutant Bcr/Abl (e.g.,IC50 = 15 versus 280 nM, respectively, for wild-type Bcr/Abl).5 Also, nilotinib regulates the gene expression for DNA helicase complex, cyclins, and cyclin-dependent kinases, inhibiting cell proliferation and decreasing progression through S phase, while imatinib does not.6 |
| 别名 | AMN107; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Golemovic, M.,Verstovsek, S.,Giles, F., et al. AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl, has in vitro activity against imatinib-resistant chronic myeloid leukemia. Clinical Cancer Research 11(13), 4941-4947 (2005). 2.Weisberg, E.,Manley, P.,Mestan, J., et al. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL. British Journal of Cancer 94, 1765-1769 (2006). 3.McFarland, K.L., and Wetzstein, G.A. Chronic myeloid leukemia therapy: Focus on second-generation tyrosine kinase inhibitors. Cancer Control 16(2), 132-140 (2009). 4.Kantarjian, H.,Giles, F.,Wunderle, L., et al. Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL. New England Journal of Medicine 354(24), 2542-2551 (2006). 5.OHare, T.,Walters, D.K.,Stoffregen, E.P., et al. In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Research 65(11), 4500-4505 (2005). 6.Ji, R.R.,de Silva, H.,Jin, Y., et al. Transcriptional profiling of the dose response: A more powerful approach for characterizing drug activities. PLoS Computational Biology 5(9), (2009). | |
| 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 | 529.5 |
| 分子式 | C28H22F3N7O |
| CAS号 | 641571-10-0 |
| 稳定性 | ≥ 2 years |
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