AEE788

AEE788 is an inhibitor of both epidermal growth factor (EGF) and vascular endothelial growth factor (VEGF) receptor tyrosine kinase family members. It can inhibit EGFR and VEGFR tyrosine kinases with IC₅₀ values of 2, 6, 77, and 59 nM for EGFR, ErbB2, KDR, and FLT1, respectively. AEE788 demonstrates antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines and can inhibit the proliferation of EGF- and VEGF-stimulated human umbilical vein endothelial cells. It also has been shown to have antitumor and anti-angiogenic activity in numerous animal models of cancer.

AEE788 is a novel multitargeted human epidermal receptor (HER) 1/2 and vascular endothelial growth factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1.