| 货号 | 18404-1mg |
| 描述 | The receptor tyrosine kinase HER2 (ErbB2) is a key component of epidermal growth factor receptor complexes that are known to have central roles in cell proliferation and cancer.1,2 Neratinib is an orally active, irreversible inhibitor of the HER2 kinase (IC50 = 59 nM).3 It also potently inhibits several mutants of HER2 and shows 10-fold or greater selectivity over a wide variety of other kinases.3,4,5 As an irreversible inhibitor, neratinib may circumvent acquired resistance developed against reversible inhibitors, including gefitinib (Item No. 13166).6 Neratinib has been evaluated in clinical trials against cancers characterized by HER2 overexpression or HER2 activating mutations.7,8 |
| 别名 | HKI-272; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ono, M., and Kuwano, M. Molecular mechanisms of epidermal growth factor receptor (EGFR) activation and response to gefitinib and other EGFR-targeting drugs. Clinical Cancer Research 12, 7242-7251 (2006). 2.Arkin, M., and Moasser, M.M. HER2 directed small molecule antagonists. Curr.Opin.Investig.Drugs 9(12), 1264-1276 (2008). 3.Rabindran, S.K.,Discafani, C.M.,Rosfjord, E.C., et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Research 64(11), 3958-3965 (2004). 4.Ji, H.,Zhao, X.,Yuza, Y., et al. Epidermal growth factor receptor variant III mutations in lung tumorigenesis and sensitivity to tyrosine kinase inhibitors. Proceedings of the National Academy of Sciences of the United States of America 103(20), 7817-7822 (2006). 5.Davis, M.I.,Hunt, J.P.,Herrgard, S., et al. Comprehensive analysis of kinase inhibitor selectivity. Nat.Biotechnol. 29(11), 1046-1051 (2011). 6.Kwak, E.L.,Sordella, R.,Bell, D.W., et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proceedings of the National Academy of Sciences of the United States of America 102(21), 7665-7670 (2005). 7.Kavuri, S.M.,Jain, N.,Galimi, F., et al. HER2 activating mutations are targets for colorectal cancer treatment. Cancer Discov. 5(8), 832-841 (2015). 8.Segovia-Mendoza, M.,González-González, M.E.,Barrera, D., et al. Efficacy and mechanism of action of the tyrosine kinase inhibitors gefitinib, lapatinib and neratinib in the treatment of HER2-positive breast cancer: Preclinical and clinical evidence. Am.J.Cancer Res. 5(9), 2531-2561 (2015). | |
| 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 | 557 |
| 分子式 | C30H29ClN6O3 |
| CAS号 | 698387-09-6 |
| 稳定性 | ≥ 2 years |
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