Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECitarinostatCat.No.:HY-15994CASNo.:1316215-12-9Synonyms:ACY241分?式:C??H??ClN?O?分?量:467.95作?靶點:HDAC作?通路:CellCycle/DNADamage;Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥30mg/mL(64.11mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1370mL10.6849mL21.3698mL5mM0.4274mL2.1370mL4.2740mL10mM0.2137mL1.0685mL2.1370mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.34mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.34mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.34mM);ClearsolutionBIOLOGICALACTIVITY?物活性Citarinostat(ACY241)第?代有效的，?服活性，?選擇性的HDAC6抑制劑，IC50為2.6nM(HDAC1，HDAC2，HDAC3和HDAC8的IC50分別為35nM，45nM，46nM和137nM)。Citarinostat具有抗癌作?。IC50&TargetHDAC6HDAC1HDAC2HDAC32.6nM(IC50)35nM(IC50)45nM(IC50)46nM(IC50)HDAC8HDAC7137nM(IC50)7300nM(IC50)體外研究Citarinostat(ACY241;0-3μM;24hours;A2780cells)treatmentwith300nMresultsinincreasedhyperacetylationofα-tubulin,consistentwithinhibitionofthetubulindeacetylaseHDAC6.Incontrast,hyperacetylationofhistoneH3,atargetofClassIHDACs,isonlyobservedatdosesabove1μM.LowexposuresofCitarinostatresultinselectiveinhibitionofHDAC6,whilehigherexposuresleadtoinhibitionofClassIHDACisozymes[1].ThesingleagentviabilityIC50ofCitarinostat(ACY241)rangedfrom4.6-6.1μMinA2780andTOV-21GovariancancerandMDA-MD-231breastcancercells.Consistentwiththeviabilityassay,singleagentCitarinostatmodestlyreducesproliferationatdosesupto3μMwithoutinducingapoptosis,while10μMofCitarinostatcausessignificantinductionofapoptosisandcompletelysuppressesproliferation[1].WesternBlotAnalysis[1]CellLine:A2780cellsConcentration:0μM,0.1μM,0.3μM,0.5μM,1μM,3μMIncubationTime:24hoursResult:Resultedinincreasedhyperacetylationofα-tubulin,consistentwithinhibitionofthetubulindeacetylaseHDAC6.Incontrast,hyperacetylationofhistoneH3,atargetofClassIHDACs,wasonlyobservedatdosesabove1μM.體內(nèi)研究Citarinostat(ACY241;50mg/kg;intraperitonealinjection;oncedailyforfivedays,followedbytwodaysoff;for3weeks;femaleathymicnudemice)significantlysuppressestumorgrowthincombinationwithNSC125973[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:Femaleathymicnudemice(7-week-old)injectedwithTOV-21Gcells[1]Dosage:50mg/kgAdministration:Intraperitonealinjection;oncedailyforfivedays,followedbytwodaysoff;for3weeksResult:CombinationtreatmentwithNSC125973resultedinsignificantlysuppressionoftumorgrowth.戶使?本產(chǎn)品發(fā)表的科研?獻?Oncogene.2021Apr;40(15):2711-2724.?ActaPharmacolSin.2021Apr13.?JMolMed(Berl).2019Aug;97(8):1183-1193.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HuangP,etal.SelectiveHDACinhibitionbyACY-241enhancestheactivityofNSC125973insolidtumormodels.Oncotarget.2017Jan10;8(2):2694-2707.McePdfHeightCaution:Produc