生物活性

• 描述CI-1040 is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM, being 100-fold selective for MEK1/2 than MEK5.
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  23132-87	-	Growth Inhibition Assay	-	IC50=5.16872 μM	SANGER
  639-V	-	Growth Inhibition Assay	-	IC50=9.64388 μM	SANGER
  647-V	-	Growth Inhibition Assay	-	IC50=49.3414 μM	SANGER

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• 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
  NCT00034827	Colorectal Neoplasms ... more >> Breast Neoplasms Carcinoma, Non-Small-Cell Lung Pancreatic Neoplasms Collapse <<	Phase 2	Completed	-	United States, Alabama ... more >> Pfizer Investigational Site Birmingham, Alabama, United States, 35205 Pfizer Investigational Site Birmingham, Alabama, United States, 35233 United States, California Pfizer Investigational Site Blendora, California, United States, 91740 Pfizer Investigational Site Glendale, California, United States, 91204 Pfizer Investigational Site Huntington Beach, California, United States, 92648 Pfizer Investigational Site Long Beach, California, United States, 90813 Pfizer Investigational Site Los Alamitos, California, United States, 90720 Pfizer Investigational Site Los Angeles, California, United States, 90048 Pfizer Investigational Site Los Angeles, California, United States, 90095 Pfizer Investigational Site Mission Hills, California, United States, 91345 Pfizer Investigational Site Northridge, California, United States, 91328 Pfizer Investigational Site Oxnard, California, United States, 93030 Pfizer Investigational Site Pasadena, California, United States, 91105 Pfizer Investigational Site Pomona, California, United States, 91767 Pfizer Investigational Site Rancho Cucamonga, California, United States, 91730 Pfizer Investigational Site Redondo Beach, California, United States, 90277 Pfizer Investigational Site Santa Monica, California, United States, 90404 Pfizer Investigational Site Torrance, California, United States, 90505 Pfizer Investigational Site Ventura, California, United States, 93003 Pfizer Investigational Site West Covina, California, United States, 91790 United States, Georgia Pfizer Investigational Site Atlanta, Georgia, United States, 30342 Pfizer Investigational Site Decatur, Georgia, United States, 30033 Pfizer Investigational Site Macon, Georgia, United States, 30342 United States, Kentucky Pfizer Investigational Site Crestview Hills, Kentucky, United States, 41017 United States, Michigan Pfizer Investigational Site Detroit, Michigan, United States, 48201 United States, Minnesota Pfizer Investigational Site Rochester, Minnesota, United States, 55905 United States, Ohio Pfizer Investigational Site Cincinnait, Ohio, United States, 45236 Pfizer Investigational Site Cincinnati, Ohio, United States, 45219 Pfizer Investigational Site Cincinnati, Ohio, United States, 45230 Pfizer Investigational Site Cincinnati, Ohio, United States, 45242 Collapse <<
  NCT00033384	Breast Cancer ... more >> Colorectal Cancer Lung Cancer Pancreatic Cancer Collapse <<	Phase 2	Completed	-	United States, Alabama ... more >> University of Alabama at Birmingham Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3300 Collapse <<

• 参考文献

• [1] Wei CR, Ge XF, et al. MEK inhibitor CI-1040 induces apoptosis in acute myeloid leukemia cells in vitro. Eur Rev Med Pharmacol Sci. 2016 May;20(10):1961-8.

  [2] Allen LF, Sebolt-Leopold J, et al. CI-1040 (PD184352), a targeted signal transduction inhibitor of MEK (MAPKK). Semin Oncol. 2003 Oct;30(5 Suppl 16):105-16.