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AEE788 (NVP-AEE788)EGFR/HER-2/VEGFR inhibitor

AEE788 (NVP-AEE788)

Catalog No. A5455
Size Price Stock Qty
10mM (in 1mL DMSO) $132.00 In stock
5mg $90.00 In stock
10mg $170.00 In stock
25mg $360.00 In stock
50mg $600.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AEE788 (NVP-AEE788)

Biological Activity

Description AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 values of 2 nM and 6 nM, respectively.
Targets EGFR HER2/ErbB2 c-Abl FLT1 c-Fms  
IC50 2 nM 6 nM 52 nM 59 nM 60 nM  

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Chemical Properties

Cas No. 497839-62-0 SDF Download SDF
Chemical Name 6-[4-[(4-ethylpiperazin-1-yl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Canonical SMILES CCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(N3)N=CN=C4NC(C)C5=CC=CC=C5
Formula C27H32N6 M.Wt 440.58
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

AEE788 is a potent inhibitor of EGFR and HER2 (IC50=2 nM and 6 nM)

EGFR (epidermal growth factor receptor) is a cell-surface receptor tyrosine kinase. The receptor activation leads to dimerization and tyrosine autophosphorylation. It induces a cascade of downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc.

In HCT 15 colon cancer cells, AEE788 potentiated celecoxib-mediated blockage of proliferation and angiogenesis [1]. In various cell line with EGFR and HER2-overexpressing, AEE788 exhibited antiproliferative activity [3]. AEE788 also inhibited cell proliferation (IC50=1.7-3.8 µM) and prevented epidermal growth factor and neuregulin-induced activation of HER1, HER2, and HER3 in vitro [5].

Comparing with the control mice, AEE788 treated mice showed 54% inhibited tumor growth in 21 days after the initiation of the treatment [2]. In ZR75.1 A3 xenograft mice, letrozole combined with AEE788 had a prominently greater tumor growth inhibition compared with letrozole treatment alone [4].

References:
[1] Venkatesan P, Bhutia SK, Singh AK et al.  AEE788 potentiates celecoxib-induced growth inhibition and apoptosis in human colon cancer cells. Life Sci. 2012 Oct 22;91(15-16):789-99.
[2] Park YW, Younes MN, Jasser SA et al.  AEE788, a dual tyrosine kinase receptor inhibitor, induces endothelial cell apoptosis in human cutaneous squamous cell carcinoma xenografts in nude mice. Clin Cancer Res. 2005 Mar 1;11(5):1963-73.
[3] Traxler P, Allegrini PR, Brandt R et al.  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 Jul 15;64(14):4931-41.
[4] Evans AH, Pancholi S, Farmer I et al.  EGFR/HER2 inhibitor AEE788 increases ER-mediated transcription in HER2/ER-positive breast cancer cells but functions synergistically with endocrine therapy.  Br J Cancer. 2010 Apr 13;102(8):1235-43.
[5] Meco D, Servidei T, Zannoni GF et al.  Dual Inhibitor AEE788 Reduces Tumor Growth in Preclinical Models of Medulloblastoma. Transl Oncol. 2010 Oct 1;3(5):326-35.