Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemERomidepsinCat.No.:HY-15149CASNo.:128517-07-7分?式:C??H??N?O?S?分?量:540.7作?靶點(diǎn):HDAC;Apoptosis作?通路:CellCycle/DNADamage;Epigenetics;Apoptosis儲(chǔ)存?式:Powder-20°C3years*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(92.47mM;Needultrasonic)掃描?維碼，運(yùn)?溶解?案計(jì)算器獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8495mL9.2473mL18.4945mL5mM0.3699mL1.8495mL3.6989mL10mM0.1849mL0.9247mL1.8495mL請(qǐng)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(chǔ)備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶1.請(qǐng)依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.08mg/mL(3.85mM);Clearsolution此?案可獲得≥2.08mg/mL(3.85mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲(chǔ)備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。1/4www.MedChemEwww.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.62mM);Clearsolution此?案可獲得≥2.5mg/mL(4.62mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請(qǐng)依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.5mg/mL(4.62mM);Clearsolution此?案可獲得≥2.5mg/mL(4.62mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性Romidepsin(FK228)具有抗腫瘤活性的組蛋?去??；?HDAC)抑制劑，抑制HDAC1，HDAC2，HDAC4和HDAC6，IC50值分別為36nM，47nM，510nM和1.4μM。Romidepsin(FK228)由紫?桿產(chǎn)?，誘導(dǎo)G2/M細(xì)胞周期阻滯和凋亡(apoptosis)。IC50&TargetHDAC1HDAC2HDAC4HDAC636nM(IC50)47nM(IC50)510nM(IC50)14000nM(IC50)體外研究Romidepsin(0-72hours;0-80nM)inhibitsproliferationofHCCcellsindose-dependentmanner[2].Romidepsin(0-48hours;0-60nM)leadstoatime-anddose-dependentinductionofcellcyclearrestintheG2/MphaseinHCCcells[2].Romidepsin(0-48hours;0-60nM)promotesapoptosisinHCCcells,increasesc-caspase-3,c-caspase-9,andc-PARPproteinexpression[2].CellProliferationAssay[2]CellLine:HCCcellsConcentration:0nM;10nM;20nM;30nM;40nM;50nM;60nM;70nM;80nMIncubationTime:0hours;12hours;24hours;48hours;72hoursResult:InhibitedHCCcellsproliferation.CellCycleAnalysis[2]CellLine:HCCcellsConcentration:0nM;15nM;30nM;60nMIncubationTime:12hours;24hours;48hoursResult:CausedaG2/Marrest.WesternBlotAnalysis[2]2/4www.MedChemEwww.MedChemECellLine:HCCcellsConcentration:0nM;15nM;30nM;60nMIncubationTime:12hours;24hours;48hoursResult:Increaesdc-caspase-3,c-caspase-9,andc-PARPexpressioninHCCcells.體內(nèi)研究Romidepsin(intraperitonealinjection;0.5and1mg/kg;every3day;21days)inhibitedthetumorgrowth,revealsahigherexpressionofp-cdc25C,ki67,c-caspase-3andc-PARP,andalowerexpressionofKi-67inRomidepsintreatedtumors[2].AnimalModel:NudemicewithHuh7cells[2]Dosage:0.5and1mg/kgAdministration:Intraperitonealinjection;0.5and1mg/kg;every3day;21daysResult:Suppressedtumorgrowthinmousexenograftmodels.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CancerRes.2020Oct15;80(20):4426-4438.?CancerRes.2016Dec1;76(23):7001-7011.?Theranostics.2021Mar20;11(11):5605-5619.?CellDeathDis.2020Sep18;11(9):778.?CellDeathDis.2020Sep15;11(9):753.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FurumaiR,etal.FK228(depsipeptide)asanaturalprodrugthatinhibitsclassIhistonedeacetylases.CancerRes.2002Sep1;62(17):4916-21.[2].SunWJ,etal.RomidepsininducesG2/MphasearrestviaErk/cdc25C/cdc2/cyclinBpathwayandapoptosisinductionthroughJNK/c-Jun/caspase3pathwayinhepatocellularcarcinomacells.BiochemPharmacol.2017Mar1;127:90-100.McePdfHeight3/4www.MedChemEwww.MedChemE關(guān)注MCE中國(guó)公眾號(hào)，

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