| 词条 | Mocetinostat |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 444509574 | ImageFile=mocetinostat.png | ImageSize=200px | IUPACName= N-(2-Aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl] benzamide | OtherNames= |Section1={{Chembox Identifiers | IUPHAR_ligand = 7008 | CASNo_Ref = {{cascite|correct|??}} | CASNo=726169-73-9 | PubChem=9865515 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 272980 | KEGG = D09641 | SMILES=C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 8041206 | InChI = 1/C23H20N6O/c24-19-5-1-2-6-21(19)28-22(30)17-9-7-16(8-10-17)14-27-23-26-13-11-20(29-23)18-4-3-12-25-15-18/h1-13,15H,14,24H2,(H,28,30)(H,26,27,29) | InChIKey = HRNLUBSXIHFDHP-UHFFFAOYAW | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C23H20N6O/c24-19-5-1-2-6-21(19)28-22(30)17-9-7-16(8-10-17)14-27-23-26-13-11-20(29-23)18-4-3-12-25-15-18/h1-13,15H,14,24H2,(H,28,30)(H,26,27,29) | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = HRNLUBSXIHFDHP-UHFFFAOYSA-N | UNII_Ref = {{fdacite|correct|FDA}} | UNII = A6GWB8T96J |Section2={{Chembox Properties | C=23 | H=20 | N=6 | O=1 | Appearance= | Density= | MeltingPt= | BoilingPt= | Solubility= |Section3={{Chembox Hazards | MainHazards= | FlashPt= | AutoignitionPt = }}Mocetinostat (MGCD0103) is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers including follicular lymphoma, Hodgkin's lymphoma and acute myelogenous leukemia.[1][2][3] One clinical trial (for refractory follicular lymphoma) was temporarily put on hold due to cardiac problems but resumed recruiting in 2009.[4] In 2010 favourable results were announced from the phase II trial for Hodgkin's lymphoma.[5] MGCD0103 has also been used as a research reagent where blockage of members of the HDAC-family of histone deacetylases is required.[6] Mechanism of actionIt works by inhibiting mainly histone deacetylase 1 (HDAC1), but also HDAC2, HDAC3, and HDAC11.[7] References1. ^{{cite press release | url=http://www.biospace.com/news_story.aspx?NewsEntityId=20794 | deadurl=yes | title=Pharmion Corporation (PHRM) Release: Clinical Data On Oncology HDAC Inhibitor MGCD0103, Presented At The American Society of Clinical Oncology 42nd Annual Meeting | date=June 6, 2006 | publisher=BioSpace | location=Colorado, United States | archiveurl=https://web.archive.org/web/20110716091432/http://www.biospace.com/news_story.aspx?NewsEntityId=20794 | archivedate=July 16, 2011 | df= }} {{HDAC inhibitors}}2. ^{{cite conference | title=Phase I trials of the oral histone deacetylase (HDAC) inhibitor MGCD0103 given either daily or 3x weekly for 14 days every 3 weeks in patients (pts) with advanced solid tumors | author=Gelmon, K. | author2=Tolcher, A. | author3=Carducci, M. | author4=Reid, G. K. | author5=Li, Z. | author6=Kalita, A. | author7=Callejas, V. | author8=Longstreth, J. | author9=Besterman, J. M. | author10=Siu, L. L. | conference=2005 ASCO Annual Meeting. | journal=J. Clin. Oncol. | volume=23 | issue=16S | year=2005 | id=3147 | url=http://meeting.ascopubs.org/cgi/content/abstract/23/16_suppl/3147 | archive-url=https://archive.is/20120711180327/http://meeting.ascopubs.org/cgi/content/abstract/23/16_suppl/3147 | dead-url=yes | archive-date=2012-07-11 }} 3. ^MethylGene to Resume Development of its HDAC Inhibitor, MGCD0103 (Mocetinostat), Sept 2009 4. ^{{cite news |url=http://www.lifescience-online.com/METHYLGENE_TO_RESUME_DEVELOPMENT_OF_ITS_HDAC_INHIB,17766.html?portalPage=Lifescience+Today.News |title=METHYLGENE TO RESUME DEVELOPMENT OF ITS HDAC INHIBITOR, MGCD0103 (MOCETINOSTAT) |date=21 Sep 2009 }} 5. ^{{cite news |url=http://www.sys-con.com/node/1637603 |title=Final Phase 2 Clinical Data for Mocetinostat (MGCD0103) in Relapsed/Refractory Hodgkin Lymphoma Patients |date=6 Dec 2010 }} 6. ^{{cite journal | title=Specific NuRD components are required for fin regeneration in zebrafish | first=Catherine | last=Pfefferli | first2=Fritz | last2=Müller | first3=Anna | last3=Jaźwińska | first4=Chantal | last4=Wicky | journal=BMC Biol. | doi=10.1186/1741-7007-12-30 | volume=12 | issue=30 | pages=30 | year=2014 | pmid=24779377 | pmc=4038851 }}{{open access}} 7. ^MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo 4 : Pyrimidines|Pyridines|Benzanilides|Histone deacetylase inhibitors |
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