AEE 788

Tocris Bioscience, part of Bio-Techne | Catalog # 5318

(2)

Citations (2)

COA / SDS

Potent EGFR and VEGFR inhibitor

Key Product Details

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)
Molecular Weight:	440.58

View Full Technical Details for AEE 788

Technical Data
Citations / Reviews (2)

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 for AEE 788

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	22.70 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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References for AEE 788

References are publications that support the biological activity of the product.

Yokoi 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. 2005 PMID: 15867367
Traxler 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 PMID: 15256466