| 货号 | 9842S |
| 供应商 | CST |
| 背景 | Tyrphostin AG 1478 is a tyrosine kinase inhibitor specifically selective to EGFR (ErbB1), with an IC50 of about 3 nM in vitro (1,2). Treatment of cell with 50-150 nM of AG 1478 can substantially block EGFR activiation in vivo (3). In addition to EGFR, AG 1478 also inhibits ErbB4 activation induced by radiation in cancer cells (4). Testing of AG 1478 alone or in combination with other treatments to assess anti-tumor and anti-fibrotic effectiveness has yielded promising results (5-8). |
| 存放说明 | -20C |
| 参考文献 | Osherov, N. and Levitzki, A. (1994) Eur J Biochem 225, 1047-53. Levitzki, A. and Gazit, A. (1995) Science 267, 1782-8. Fan, Z. et al. (1995) J Cell Biol 131, 235-42. Bowers, G. et al. (2001) Oncogene 20, 1388-97. Nagane, M. et al. (2001) J Neurosurg 95, 472-9. Ishii, Y. et al. (2006) Am J Respir Crit Care Med 174, 550-6. Ellis, A.G. et al. (2006) Biochem Pharmacol 71, 1422-34. Rahman, M. et al. (2009) Breast Cancer Res Treat 113, 217-30. |
Structure of Tyrphostin AG 1478Tyrphostin AG 1478的结构 | |
Western blot analysis of extracts from serum starved A431 cells, untreated or treated with indicated concentrations of Tyrphostin AG1478 for 30 minutes, followed by stimulation with EGF for 10 minutes. The EGFR activation was detected by using Phospho-EGF Receptor (Tyr1173) (53A5) Rabbit mAb #4407 (upper). EGF Receptor Antibody #2232 was used to detect the equal loading of EGFR (lower). Tyrphostin AG1478-mediated inhibition of EGF-induced phosphorylation of EGF Receptor at Tyr1173 is shown.A431细胞经过血清饥饿后，未经处理或经过特定浓度的Tyrphostin AG1478 处理 30分钟, 然后再用EGF 刺激10分钟，最后用细胞提取物进行免疫印迹检测。用Phospho-EGF Receptor (Tyr1173) (53A5) Rabbit mAb #4407检测EGFR 的活化(上)。 用EGF Receptor Antibody #2232 检测同样的EGFR样品 (下)。 如图示Tyrphostin AG1478介导的对EGF引起的EGF受体 Tyr1173位点的磷酸化的抑制作用。 |
