| 货号 | 10483-250mg |
| 描述 | Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity (IC50 = 2.5 µM).1,2 This inhibits tumor growth in human head and neck carcinoma (HN5) tumor xenografts in mice with an ED50 value of 9 mg/kg.1 Erlotinib also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC50 = 4.6 µM) and JAK2 mutant JAK2V617F(IC50 = 5 µM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia.3,4 The drug form of Erlotinib, Tarceva™, is used to treat certain forms of cancer, including non-small cell lung cancer.5,6 |
| 别名 | NSC 718781; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Pollack, V.A.,Savage, D.M.,Baker, D.A., et al. Inhibition of epidermal growth factor receptor-associated tyrosine phosphorylation in human carcinomas with CP-358,774: Dynamics of receptor inhibition in situ and antitumor effects in athymic mice. Journal of Pharmacology and Experimental Therapeutics 291, 739-748 (1999). 2.Greulich, H.,Chen, T.H.,Feng, W., et al. Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants. PLoS Med. 2(11), (2005). 3.Yamasaki, F.,Zhang, D.,Bartholomeusz, C., et al. Sensitivity of breast cancer cells to erlotinib depends on cyclin-dependent kinase 2 activity. Mol. Cancer Ther. 6(8), 2168-2177 (2007). 4.Li, Z.,Xu, M.,Xing, S., et al. Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth. J. Biol. Chem. 282(6), 3428-3432 (2007). 5.Herbst, R.S. and Bunn, P.A., Jr. Targeting the epidermal growth factor receptor in non-small cell lung cancer. Clin. Cancer Res. 9(16), 5813-5824 (2003). 6.Gerber, D.E. EGFR inhibition in the treatment of non-small cell lung cancer. Drug Dev. Res. 69(6), 359-372 (2008). | |
| 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 | 393.4 |
| 分子式 | C22H23N3O4 |
| CAS号 | 183321-74-6 |
| 稳定性 | ≥ 2 years |
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