6-[4-[(4-乙基-1-哌嗪)甲基]苯基]-N-[(1R)-1-苯基乙基]-7H-吡咯并[2,3-d]嘧啶-4-胺

溶解度:DMSO

储存条件:at -20℃2years

生物活性

AEE788 is a novel dual inhibitor of EGFR/ErbB2 and VEGFR tyrosine kinases (IC50s: EGFR=2 nM, ErbB2=6 nM, KDR=77 nM, and Flt-1=59 nM). In cells, growth factor-induced EGFR and ErbB2 phosphorylation was also efficiently inhibited (IC50s: 11 and 220 nM, respectively). [1] AEE788 demonstrated antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines and inhibited the proliferation of EGF- and VEGF-stimulated human umbilical vein endothelial cells. Oral administration of AEE788 to tumor-bearing mice resulted in high and persistent compound levels in tumor tissue. [2, 3]

参考文献

[1] Traxler P et al. Cancer Res. 2004 Jul 15; 64(14):4931-41 [2] Park YW et al. Clin Cancer Res. 2005 Mar 1; 11(5):1963-73 [3] Yokoi K et al. Cancer Res. 2005 May 1; 65(9):3716-25