產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
AEE788 (NVP-AEE788) | 10mM (in 1mL DMSO) 5mg 10mg 25mg 50mg | 497839-62-0 | EY-Y0165152 |
Cas No.497839-62-0
別名
化學名 6-[4-[(4-ethylpiperazin-1-yl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
分子式 C27H32N6
分子量 440.58
溶解度 ≥ 22.05mg/mL in DMSO, ≥ 14.4 mg/mL in EtOH with ultrasonic
儲存條件 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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
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.
關鍵字： 497839-62-0;C27H32N6;AEE788 (NVP-AEE788);
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學、分子生物學和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè)，公司自成立以來，秉承""全心全意服務于科研工作者""的企業(yè)理念，立足生物科技領域，運用生物技術和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機構、高等院校、科研院所、企事業(yè)單位提供優(yōu)質的產(chǎn)品，服務生物科技領域的科學研究人員。
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