货号 | 11493-5mg |
描述 | The epidermal growth factor (EGF) receptors EGFR (ErbB1) and human EGFR2 (HER2, ErbB2) are receptor tyrosine kinases that are often over-expressed in cancer.1,2 Lapatinib is a potent and selective dual inhibitor of EGFR and HER2 (IC50s = 19 and 3 nM, respectively).3,4,5 It is effective in vivo and is used in combination therapy to prevent or suppress cancers where these kinases are over-expressed, including breast cancer.6,7 |
别名 | GSK572016;GW 572016;Tyverb; |
供应商 | Cayman |
应用文献 | |
1.Gerber, D.E. EGFR inhibition in the treatment of non-small cell lung cancer. Drug Dev. Res. 69(6), 359-372 (2008). 2.Ciardiello, F. and Tortora, G. A novel approach in the treatment of cancer: Targeting the epidermal growth factor receptor. Clin. Cancer Res. 7(10), 2958-2970 (2001). 3.Rheault, T.R.,Caferro, T.R.,Dickerson, S.H., et al. Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors. Bioorganic & Medicinal Chemistry Letters 19(3), 817-820 (2009). 4.Cho, T.P.,Jun, F.,Li, H., et al. Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 19(22), 6437-6440 (2009). 5.Suzuki, N.,Shiota, T.,Watanabe, F., et al. Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors. Bioorganic & Medicinal Chemistry Letters 21(6), 1601-1606 (2011). 6.den Hollander, P.,Savage, M.I. and Brown, P.H. Targeted therapy for breast cancer prevention. Front.Oncol. 3, 250 (2013). 7.Botrel, T.E.A.,Paladini, L. and Clark, O.A. Lapatinib plus chemotherapy or endocrine therapy (CET) versus CET alone in the treatment of HER-2-overexpressing locally advanced or metastatic breast cancer: Systematic review and meta-analysis. Core Evid. 8, 69-78 (2013). | |
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 | 581.1 |
分子式 | C29H26ClFN4O4S |
CAS号 | 231277-92-2 |
稳定性 | ≥ 2 years |
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