Chemical Name: 6-[4-[(4-Ethyl-1-piperazinyl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Biological ActivityPotent EGFR and VEGFR inhibitor (IC50 values are 2, 6, 59, 77, 160 and 330 nM for EGFR, ErbB2, VEGFR-1, VEGFR-2, ErbB4 and VEGFR-3 respectively). Also inhibits c-Abl, c-Fms and c-Src (IC50 values are 52, 60 and 61 nM respectively). Inhibits proliferation of EGFR and ErbB2 overexpressing cancer cell lines in vitro. Inhibits tumor xenograft growth and VEGF-induced angiogenesis in mice. Orally active.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity.
Traxler et al.
Cancer Res., 2004;64:4931
Dual inhibition of epidermal growth factor receptor and vascular endothelial growth factor receptor phosphorylation by AEE788 reduces growth and metastasis of human colon carcinoma in an orthotopic nude mouse model.
Yokoi et al.
Cancer Res., 2005;65:3716
Citation for AEE 788
The citations listed below are publications that use Tocris products. Selected citations for AEE 788 include:
1 Citation: Showing 1 - 1
ANO1 interacts with EGFR and correlates with sensitivity to EGFR-targeting therapy in head and neck cancer.
Authors: Bill Et al.
Int J Mol Sci 2015;6:9173
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Used in vitro to investigate ERG pathway in connection with VGEF