| 货号 | 12121S |
| 供应商 | CST |
| 背景 | Lapatinib is a dual inhibitor of EGFR and HER2 tyrosine kinases (1-4). Researchers have shown that lapatinib inhibits purified EGFR and HER2 tyrosine kinase domains in cell-free kinase assays with IC50 values of 10.8 nM and 9.2 nM, respectively, and HER4 with an IC50 of 367 nM. Lapatinib was greater than 300-fold more selective for HER2 and EGFR than many other kinases, including c-src, MEK, Erk, and p38 in these assays (1). Studies have shown that lapatinib effectively inhibits both EGFR and HER2 autophosphorylation in cell types over expressing these kinases, and cell growth inhibition is correlated with HER2 overexpression (2-4). |
| 存放说明 | -20C |
| 参考文献 | 1 . Rusnak, D.W. et al. (2001) Mol Cancer Ther 1, 85-94. 2 . Konecny, G.E. et al. (2006) Cancer Res 66, 1630-9. 3 . Zhang, D. et al. (2008) Mol Cancer Ther 7, 1846-50. 4 . Hegde, P.S. et al. (2007) Mol Cancer Ther 6, 1629-40. |
Chemical structure of lapatinib.拉帕替尼的化学结构。 | |
Western blot analysis of extracts from SK-BR-3 cells, untreated or treated with Lapatinib (6 hr) at the indicated concentrations, using Phospho-HER2/ErbB2 (Tyr1248)/EGFR (Tyr1173) Antibody #2244 (upper) or HER2/ErbB2 (D8F12) XP® Rabbit mAb #4290 (lower).Western blot方法检测SK-BR-3细胞提取物，细胞未处理或用拉帕替尼在指定的浓度处理(6 hr)，使用的抗体为Phospho-HER2/ErbB2 (Tyr1248)/EGFR (Tyr1173) Antibody #2244 (上图)或HER2/ErbB2 (D8F12) XP® Rabbit mAb #4290 (下图). |
