AEE788 can potently inhibit EGFR, ErbB2, KDR, and Flt-1with IC50 of 2 nM, 6 nM, 77 nM and 59 nM, respectively.

AEE788 inhibits EGFR and ErbB2 phosphorylation in cells with IC50 of 11 nM and 22 nM, respectively. AEE788 demonstrates antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines (including EGFRvIII-dependent lines) and inhibited the proliferation of epidermal growth factor- and VEGF-stimulated human umbilical vein endothelial cells. AEE788 shows potent antitumor activity in a number of animal models of cancer, including tumors that overexpress EGFR and or ErbB2. AEE788 was able to inhibit the proliferation and induce apoptosis of ATC cell lines in vitro, and anaplastic thyroid carcinoma (ATC) is one of the most aggressive human malignancies.[2]Treatment of cutaneous SCC cells with AEE788 led to dose-dependent inhibition of EGFR and VEGFR-2 phosphorylation, growth inhibition, and induction of apoptosis.[3]

[1] [1] Traxler, P., P. R. Allegrini, et al. (2004). "AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity." Cancer Res 64(14): 4931-4941.
[2] [2] Kim, S., B. A. Schiff, et al. (2005). "Targeted molecular therapy of anaplastic thyroid carcinoma with AEE788." Mol Cancer Ther 4(4): 632-640.
[3] [3]Park, Y. W., M. N. Younes, et al. (2005). "AEE788, a dual tyrosine kinase receptor inhibitor, induces endothelial cell apoptosis in human cutaneous squamous cell carcinoma xenografts in nude mice." Clin Cancer Res 11(5): 1963-1973.
[4] [4] Goudar, R. K., Q. Shi, et al. (2005). "Combination therapy of inhibitors of epidermal growth factor receptor/vascular endothelial growth factor receptor 2 (AEE788) and the mammalian target of rapamycin (RAD001) offers improved glioblastoma tumor growth inhibition." Mol Cancer Ther 4(1): 101-112.