生物活性

• 靶点

  VEGFR2 IC50:77nM

  Src IC50:61nM

  VEGFR1 IC50:59nM

  Abl IC50:52nM

  EGFR IC50:2nM

  更多

• 描述AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1.
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  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 ... more >> 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 Collapse <<
  NCT00118456	Cancer	Phase 1	Completed	-	United States, Connecticut ... more >> 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 Collapse <<
  NCT00107237	Brain and Central Nervous Syst... more >>em Tumors Collapse <<	Phase 1 Phase 2	Completed	-	United States, California ... more >> 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 Collapse <<

• 参考文献

• [1] Park YW, Younes MN, 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.

  [2] Traxler P, Allegrini PR, 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.