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Submit ReviewAEE 788
Description: Potent EGFR and VEGFR inhibitor
Chemical Name: 6-[4-[(4-Ethyl-1-piperazinyl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Purity: ≥98% (HPLC)
Biological Activity for AEE 788
AEE 788 is a 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 for AEE 788
| M. Wt | 440.58 |
| Formula | C27H32N6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 497839-62-0 |
| PubChem ID | 10297043 |
| InChI Key | OONFNUWBHFSNBT-HXUWFJFHSA-N |
| Smiles | C[C@@H](NC2=C(C=C(C4=CC=C(CN5CCN(CC)CC5)C=C4)N3)C3=NC=N2)C1=CC=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AEE 788
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.06 | 100 |
Preparing Stock Solutions for AEE 788
The following data is based on the product molecular weight 440.58. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.27 mL | 11.35 mL | 22.7 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.27 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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Product Datasheets for AEE 788
References for AEE 788
References are publications that support the biological activity of the product.
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
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
If you know of a relevant reference for AEE 788, please let us know.
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Keywords: AEE 788, AEE 788 supplier, AEE788, potent, epidermal, vascular, endothelial, growth, factors, EGFR, VEGFR, ErbB2, antiangiogenic, antitumor, orally, active, 5318, Tocris Bioscience
1 Citation for AEE 788
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
Do you know of a great paper that uses AEE 788 from Tocris? Please let us know.
Reviews for AEE 788
Average Rating: 5 (Based on 2 Reviews.)
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Inhibits proliferation.
By
Anonymous on 09/17/2022
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: EGFR-hi cells
Used this to inhibit proliferation, looks great!
In vitro culture.
By
Anonymous on 08/05/2018
Assay Type: In Vitro
Species: Mouse
Used in vitro to investigate ERG pathway in connection with VGEF
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.