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AEE788

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Chemical Structure| 497839-62-0 同义名 : NVP-AEE 788
CAS号 : 497839-62-0
货号 : A176210
分子式 : C27H32N6
纯度 : 98+%
分子量 : 440.583
MDL号 : MFCD11100351
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(113.49 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% PEG400+0.5% Tween80+5% propylene glycol+water 30 mg/mL suspension

生物活性
靶点

  • EGFR/ErbB1

    EGFR, IC50:2 nM

  • HER2/ErbB2

    HER2/ErbB2, IC50:6 nM

  • ErbB4

    HER4/ErbB4, IC50:160 nM

  • VEGFR1

    FLT1, IC50:59 nM
描述 AEE788 effectively inhibits EGFR and VEGF receptor tyrosine kinases within the nanomolar range, with IC50 values for EGFR at 2 nm, ErbB2 at 6 nm, KDR at 77 nm, and Flt-1 at 59 nm. It also efficiently blocks growth factor-induced phosphorylation of EGFR and ErbB2 in cells, with IC50 values of 11 nm and 220 nm, respectively. AEE788 exhibits antiproliferative effects on various cell lines that overexpress EGFR and ErbB2, including those dependent on EGFRvIII, and it hinders the proliferation of human umbilical vein endothelial cells stimulated by epidermal growth factor and VEGF[1]. Administering AEE788 to cutaneous SCC cells results in a dose-dependent reduction of EGFR and VEGFR-2 phosphorylation, inhibits cell growth, and triggers apoptosis[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
Huh7 Cytotoxicity assay Cytotoxicity against human hepatocellular carcinoma cell line (Huh7), CC50=27.83 Μm 18579783
Jeko B cells Function assay 2 h Inhibition of PI3Kdelta in human Jeko B cells assessed as inhibition of Akt phosphorylation after 2 hrs, IC50=0.017 μM 25514658
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00116376 Glioblastoma Multiforme Phase 1 Phase 2 Completed - United States, California ... 展开 >> University of California at Los Angeles Los Angeles, California, United States, 90095 University of California, San Francisco San Francisco, California, United States, 94143 United States, North Carolina The Brain Tumor Center at Duke, Duke University Medical Center Box 3624 DUMC, Trent Drive, Durham, North Carolina, United States, 27710 United States, Texas University of Texas, MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT00118456 Cancer Phase 1 Completed - United States, Connecticut ... 展开 >> Yale Cancer Center New Haven, Connecticut, United States, 06520 United States, Nevada Nevada Cancer Institute Las Vegas, Nevada, United States, 89125 United States, Tennessee Sarah Cannon Research Institute Nashville, Tennessee, United States, 37203 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77054 Institute of Drug Development/Cancer Therapy and Research Center San Antonio, Texas, United States, 78229 收起 <<
NCT00107237 Brain and Central Nervous Syst... 展开 >>em Tumors 收起 << Phase 1 Phase 2 Completed - United States, California ... 展开 >> Jonsson Comprehensive Cancer Center at UCLA Los Angeles, California, United States, 90095-1781 United States, North Carolina Duke Univaersity Medical Center Durham, North Carolina, United States, 27710 United States, Texas MD Anderson Cancer Center/University of Texas Houston, Texas, United States, 77030 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.35mL

2.27mL

1.13mL

22.70mL

4.54mL

2.27mL
参考文献

[1]Traxler P, 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):4931-4941.

[2]Park 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):1963-1973.