AEE788 (NVP-AEE788)
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 440.58 |
| Cas No. | 497839-62-0 |
| Formula | C27H32N6 |
| Solubility | ≥22.05 mg/mL in DMSO; insoluble in H2O; ≥14.4 mg/mL in EtOH with ultrasonic |
| Chemical Name | 6-[4-[(4-ethylpiperazin-1-yl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine |
| SDF | Download SDF |
| Canonical SMILES | CCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(N3)N=CN=C4NC(C)C5=CC=CC=C5 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| 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 | |
Quality Control & MSDS
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Chemical structure
