| CAS NO: | 497839-62-0 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 询价 |
| 5mg | 询价 |
| 10mg | 询价 |
| 25mg | 询价 |
| 50mg | 询价 |
| 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 |
| Canonical SMILES | CCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(N3)N=CN=C4NC(C)C5=CC=CC=C5 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
AEE788是EGFR和HER2的有效抑制剂，IC50值分别为2 nM和6 nM。
表皮生长因子受体（EGFR）是一种细胞表面受体酪氨酸激酶。受体活化导致二聚化和酪氨酸自磷酸化。它诱导一系列下游细胞应答级联反应，如基因表达修饰、细胞增殖和细胞骨架重排等。
在HCT 15结肠癌细胞中，AEE788增强塞来昔布（celecoxib）介导的增殖和血管生成的阻断[1]。在EGFR和HER2过表达的各种细胞系中，AEE788表现出抗增殖活性[3]。AEE788还抑制细胞增殖，IC50 为1.7-3.8 μM，抑制表皮生长因子和体外神经调节蛋白诱导的HER1、HER2和HER3的活化[5]。
与对照小鼠相比，AEE788治疗21天后，抑制54％的肿瘤生长[2]。在ZR75.1 A3异种移植小鼠中，与单独来曲唑治疗相比，来曲唑与AEE788结合使用显著抑制肿瘤生长[4]。
参考文献：
[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.
| Description | AEE788（NVP-AEE788）是EGFR和HER2/ErbB2的有效抑制剂，IC50值分别为2 nM和6 nM。 | |||||
| 靶点 | EGFR | HER2/ErbB2 | c-Abl | FLT1 | c-Fms | |
| IC50 | 2 nM | 6 nM | 52 nM | 59 nM | 60 nM | |
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