AEE 788

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Cat.No. 5318 - AEE 788 | C27H32N6 | CAS No. 497839-62-0
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)
Datasheet
Citations (1)
Literature

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.

Compound Libraries

AEE 788 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.06 100

Preparing Stock Solutions

The following data is based on the product molecular weight 440.58. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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View Related Products by Product Action

View all EGFR Inhibitors

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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? If so please let us know.

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Literature in this Area

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Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
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Pathways for AEE 788

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