AEE-788

A potent, orally bioavailable dual EGFR/VEGFR receptor tyrosine kinase inhibitor with IC50 of 2, 6, 77 and 59 nM for EGFR, ErbB2, KDR and Flt-1, respectively; inhibits growth factor-induced EGFR and ErbB2 phosphorylation in cells with IC50 of 11 and 220 nM, respectively, demonstrates antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines; shows antitumor and antiangiogenic activity in vivo.Brain Cancer Phase 2 Discontinued.