Mocetinostat(MGCD0103)isapotentandisotype-selectiveinhibitorofhistonedeacetylases(HDACs).Incell-freeassays,Mocetinostat(MGCD0103)exhibitedmostpotentinhibitionagainsthumanHDAC1(IC50=0.15?M)andalsohasinhibitoryactivityagainstHDAC2,HDAC3,andHDAC11,withIC50valuesranged0.3to1.7?M.NoactivitywasshowedonHDACs4-8.[1]Mocetinostat(MGCD0103)exhibitedpotentinhibitionactivityinproliferationofhumancancercelllines,bothincell-basedassayandinhumantumorxenograftsinnudemice.[1]
Mocetinostat(MGCD0103)hasbeenevaluatedinPhaseIIclinicaltrialsinpatientswithmetastaticleiomyosarcoma[2]andHodgkinslymphoma[3]."
Technicalinformation:
| ChemicalFormula: | C23H20N6O | |
| CAS#: | 726169-73-9 | |
| MolecularWeight: | 396.44 | |
| Purity: | >98% | |
| Appearance: | Off-white | |
| ChemicalName: | N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide | |
| Solubility: | Upto10mMinDMSO | |
| Synonyms: | Mocetinostat,MGCD0103,MG0103 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderorDMSOsolutionat-20oCdesiccated.
Reference:
| 1. | FournelM,etal.MGCD0103,anovelisotype-selectivehistonedeacetylaseinhibitor,hasbroadspectrumantitumoractivityinvitroandinvivo.MolCancerTher.2008;7(4):759-68PubmedID:18413790 |
| 2. | SARC018:AStudyofMocetinostatandGemcitABIneinPatientsWithMetastaticLeiomyosarcoma.clinicaltrials.gov/NCT02303262 |
| 3. | Mocetinostat(MGCD0103)PlusBrentuximabVedotin(SGN-35)inPatientsWithRelapsedorRefractoryHodgkinLymphoma.clinicaltrials.gov/NCT02429375 |
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