生物活性

• 靶点

  HDAC1 IC50:0.15μM

  HDAC2 IC50:0.29Μm

  HDAC3 IC50:1.66μM

• 描述Mocetinostat is a potent HDAC inhibitor with IC50 of 0.15, 0.29 and 1.66 μM for HDAC 1, HDAC 2 and HDAC 3, respectively.
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  ANBL6	1 μM	Function Assay	24 h	enhances 5-AC-induced MAGE-A3 gene expression	21171821
  AsPC-1	-	Growth Inhibition Assay	-	EC50=3.9 μM	21375679
  BT549	-	Growth Inhibition Assay	48 h	IC50=4.38 μM	26378038

• 更多
• 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
  NCT00543582	Hodgkin Lymphoma ... more >> Non-Hodgkin Lymphoma (Follicular or Large Diffuse B-cell Lymphoma or Mantle Cell Lymphoma) Collapse <<	Phase 2	Terminated(Celgene terminated ... more >>its collaboration agreement with MethylGene for the development of MGCD0103. All Celgene-sponsored trials with MGCD0103 will be closed.) Collapse <<	-	United States, Indiana ... more >> St. Francis Cancer Research Foundation Beech Grove, Indiana, United States, 46107 United States, Nevada Nevada Cancer Institute Las Vegas, Nevada, United States, 89135 United States, New York Weill Medical College of Cornell University New York, New York, United States United States, Texas University of Texas, MD Anderson Houston, Texas, United States, 77030 Collapse <<
  NCT00372437	Tumors	Phase 1 Phase 2	Completed	-	United States, Indiana ... more >> Indiana University Cancer Center Indianapolis, Indiana, United States, 46202 United States, Kansas Veterans Affairs Medical Center Kansas City, Kansas, United States, 64128 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio Gabrail Cancer Center Canton, Ohio, United States, 44718 United States, Pennsylvania Pennsylvania Presbyterian Medical Center Philadelphia, Pennsylvania, United States, 19104-4283 United States, Tennessee Vanderbilt University Medical Center Nashville, Tennessee, United States, 37232-6307 Canada, Quebec McGill University/Dept Oncology Montreal, Quebec, Canada, H2W 1S6 CHUS Hopital Fleurimont Sherbrooke, Quebec, Canada, J1H 5N4 Collapse <<
  NCT02993991	Squamous Cell Carcinoma, Head ... more >>And Neck Squamous Cell Carcinoma Mouth Resectable Squamous Cell Carcinoma of Oral Cavity Collapse <<	Phase 1	Withdrawn(The study has been t... more >>erminated due to a change in internal prioritization and not due to any safety concerns.) Collapse <<	-	Canada, Ontario ... more >> Princess Margaret Cancer Centre Toronto, Ontario, Canada, M5G 2M9 Collapse <<

• 更多
• 参考文献

• [1] Cavasin MA, Demos-Davies K, et al. Selective class I histone deacetylase inhibition suppresses hypoxia-induced cardiopulmonary remodeling through an antiproliferative mechanism. Circ Res. 2012 Mar 2;110(5):739-48.

  [2] Fournel M, Bonfils C, et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008 Apr;7(4):759-68.