AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.
IC50&Target
EGFR
2 nM (IC50)
ErbB2
6 nM (IC50)
体外研究
AEE788 inhibits EGFR and VEGF receptor tyrosine kinases in the nM range (IC50:EGFR 2 nm, ErbB2 6 nm, KDR 77 nm, and Flt-1 59 nm). In cells, growth factor-induced EGFR and ErbB2 phosphorylation is also efficiently inhibited (IC50:11 and 220 nm, respectively). AEE788 demonstrates antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines (including EGFRvIII-dependent lines) and inhibits the proliferation of epidermal growth factor- and VEGF-stimulated human umbilical vein endothelial cells. Treatment of cutaneous SCC cells with AEE788 leads to dose-dependent inhibition of EGFR and VEGFR-2 phosphorylation, growth inhibition, and induction of apoptosis.
体内研究
AEE788 efficiently inhibits growth factor-induced EGFR and ErbB2 phosphorylation in tumors for >72 h. AEE788 also inhibits VEGF-induced angiogenesis in a murine implant model. In mice treated with AEE788, tumor growth is inhibited by 54% at 21 days after the start of treatment compared with control mice.
分子式
C27H32N6
分子量
440.58
CAS号
497839-62-0
运输条件
Room temperature in continental US; may vary elsewhere.