| 货号 | 13166-5g |
| 描述 | Overactivity of the epidermal growth factor receptor-associated tyrosine kinase (EGFR-TK) has been associated with a number of cancers and thus TK inhibitors could be potential therapeutic agents to prevent malignant growth.1 Gefitinib is a selective EGFR-TK inhibitor that blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50s ranging between 0.2-0.4 µM.2 By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Gefitinib has been used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval for this compound (Iressa™) when a phase III trial failed to demonstrate an overall survival benefit.3 Gefitinib appears to be most efficacious in treating certain EGFR gene mutations that are prevalent in Asian populations.4,5 |
| 别名 | ZD 1839; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Sausville, E.A.,Elsayed, Y.,Monga, M., et al. Signal transduction-directed cancer treatments. Annual Reviews of Pharmacology and Toxicology 43, 199-231 (2003). 2.Ciardiello, F.,Caputo, R.,Bianco, R., et al. Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor. Clinical Cancer Research 6(5), 2053-2063 (2000). 3.Gerber, D.E. EGFR inhibition in the treatment of non-small cell lung cancer. Drug Dev. Res. 69(6), 359-372 (2008). 4.Yang, C.T.,Hung, J.Y.,Lai, C.L., et al. Gefitinib as first-line therapy for advanced or metastatic non-small cell lung cancer patients in southern Taiwan. Kaohsiung Journal of Medical Sciences 26(1), 1-7 (2010). 5.Uruga, H.,Kishi, K.,Fujii, T., et al. Efficacy of gefitinib for elderly patients with advanced non-small cell lung cancer harboring epidermal growth factor receptor gene mutations: A retrospective analysis. Internal Medicine 49, 103-107 (2010). | |
| 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 | 446.9 |
| 分子式 | C22H24ClFN4O3 |
| CAS号 | 184475-35-2 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |