货号 | 19280-1mg |
描述 | Nilotinib-d6 contains three deuterium atoms located on the phenyl group and three deuterium atoms located on the methyl group. It is intended for use as an internal standard for the quantification of nilotinib (Item No. 10010422) by GC- or LC-MS. Nilotinib is a second generation tyrosine kinase inhibitor that 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; Item Nos. 13139|18257).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 |
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). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥99% deuterated forms (d1-d6) |
计算分子量 | 535.6 |
分子式 | C28H16D6F3N7O |
CAS号 | 1268356-17-7 |
稳定性 | ≥ 2 years |
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