AEE 788

Cat. No. 5318

AEE 788 C27H32N6 [497839-62-0]

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Chemical Name: 6-[4-[(4-Ethyl-1-piperazinyl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Biological Activity

Potent 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.

Technical Data

M.Wt:
440.58
Formula:
C27H32N6
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
497839-62-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Yokoi et al (2005) 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. Cancer Res. 65 3716. PMID: 15867367.

Traxler et al (2004) 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. 64 4931. PMID: 15256466.

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Citations are publications that use Tocris products. Selected citations for AEE 788 include:

Bill et al (2015) ANO1 interacts with EGFR and correlates with sensitivity to EGFR-targeting therapy in head and neck cancer. Int J Mol Sci 6 9173. PMID: 25823819.

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Keywords: AEE 788, supplier, AEE788, potent, epidermal, vascular, endothelial, growth, factors, EGFR, VEGFR, ErbB2, antiangiogenic, antitumor, orally, active, Tocris Bioscience, EGFR Inhibitor products

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