AEE788 is a potent inhibitor of EGFR and HER2 (IC50=2 nM and 6 nM)
EGFR (epidermal growth factor receptor) is a cell-surface receptor tyrosine kinase. The receptor activation leads to dimerization and tyrosine autophosphorylation. It induces a cascade of downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc.
In HCT 15 colon cancer cells, AEE788 potentiated celecoxib-mediated blockage of proliferation and angiogenesis . In various cell line with EGFR and HER2-overexpressing, AEE788 exhibited antiproliferative activity . AEE788 also inhibited cell proliferation (IC50=1.7-3.8 µM) and prevented epidermal growth factor and neuregulin-induced activation of HER1, HER2, and HER3 in vitro .
Comparing with the control mice, AEE788 treated mice showed 54% inhibited tumor growth in 21 days after the initiation of the treatment . In ZR75.1 A3 xenograft mice, letrozole combined with AEE788 had a prominently greater tumor growth inhibition compared with letrozole treatment alone .
 Venkatesan P, Bhutia SK, Singh AK et al. AEE788 potentiates celecoxib-induced growth inhibition and apoptosis in human colon cancer cells. Life Sci. 2012 Oct 22;91(15-16):789-99.
 Park YW, Younes MN, Jasser SA et al. AEE788, a dual tyrosine kinase receptor inhibitor, induces endothelial cell apoptosis in human cutaneous squamous cell carcinoma xenografts in nude mice. Clin Cancer Res. 2005 Mar 1;11(5):1963-73.
 Traxler P, Allegrini PR, Brandt R et al. 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. 2004 Jul 15;64(14):4931-41.
 Evans AH, Pancholi S, Farmer I et al. EGFR/HER2 inhibitor AEE788 increases ER-mediated transcription in HER2/ER-positive breast cancer cells but functions synergistically with endocrine therapy. Br J Cancer. 2010 Apr 13;102(8):1235-43.
 Meco D, Servidei T, Zannoni GF et al. Dual Inhibitor AEE788 Reduces Tumor Growth in Preclinical Models of Medulloblastoma. Transl Oncol. 2010 Oct 1;3(5):326-35.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥22.05mg/mL in DMSO, ≥14.4 mg/mL in EtOH with ultrasonic, <2.32 mg/mL in H2O|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Description||AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 values of 2 nM and 6 nM, respectively.|
|IC50||2 nM||6 nM||52 nM||59 nM||60 nM|