Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEQTX125TFACat.No.:HY-120448A分?式:C??H??F?N?O?分?量:531.44作?靶點:HDAC;Apoptosis作?通路:CellCycle/DNADamage;Epigenetics;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(235.21mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8817mL9.4084mL18.8168mL5mM0.3763mL1.8817mL3.7634mL10mM0.1882mL0.9408mL1.8817mL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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.91mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.91mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性QTX125TFA?種有效且?度選擇性的HDAC6抑制劑。與其他HDAC相?，QTX125對HDAC6具有出?的選擇性。QTX125TFA具有抗腫瘤作?。IC50&TargetHDAC6體外研究QTX125(25-500nM;24-48hours)TFAtreatmentinducesthesubsequentapoptosisdemonstratedbyannexinV/propidiumiodidedoublestainingandthecleavageofcaspase-9,caspase-8,caspase-3,andPARP[1].InMCLcelllinesMINO,REC-1,IRM-2andHBL-2cells,QTX125TFA(10nM,10μM,100μM)inducesdose-dependenthyperacetylationofα-tubulin[1].QTX125TFAhasthestrongestgrowth-inhibitoryeffectinBurkittcelllymphoma,follicularlymphoma,andmantlecelllymphoma(MCL)[1].ApoptosisAnalysis[1]CellLine:MINO,REC-1,IRM-2andHBL-2cellsConcentration:25nM,50nM,100nM,500nMIncubationTime:24hours,48hoursResult:InhibitedannexinV/propidiumiodidedoublestaining.WesternBlotAnalysis[1]CellLine:MINO,REC-1,IRM-2andHBL-2cellsConcentration:25nM,50nM,100nM,500nMIncubationTime:24hoursResult:Inhibitedthecleavageofcaspase-9,caspase-8,caspase-3,andPARP.體內(nèi)研究QTX125TFA(60mg/kg;i.p.;dailydosingfor5days;for4weeks)treatmentinhibitstumorgrowthinREC-1orMINOcellsxenograftedinnudemice[1].AnimalModel:NudemicebearingREC-1orMINOcells[1]Dosage:60mg/kgAdministration:Intraperitonealadministration;dailydosingfor5days;for4weeksResult:InhibitedtumorgrowthinREC-1orMINOcellsxenograftedinnudemice.REFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].MontserratPérez-Salvia,etal.Invitroandinvivoactivityofanewsmall-moleculeinhibitorofHDAC6inmantlecelllymphoma.Haematologica.2018Nov;103(11):e537-e540.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap