SG2057-DRG16-DataSheet-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESG2057Cat.No.:HY-101160CASNo.:260417-62-7Synonyms:DRG16分?式:C??H??N?O?分?量:584.66作?靶點:DNAAlkylator/Crosslinker;ADCCytotoxin作?通路:CellCycle/DNADamage;Antibody-drugConjugate/ADCRelated儲存?式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(171.04mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7104mL8.5520mL17.1040mL5mM0.3421mL1.7104mL3.4208mL10mM0.1710mL0.8552mL1.7104mL請根據(jù)產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.28mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.28mM);ClearsolutionBIOLOGICALACTIVITY?物活性SG2057(DRG16)?種含有戊?氧鍵的PBD?聚體，該鍵選擇性地結合DNA?溝中的序列，形成DNA鏈間和鏈內交聯(lián)加合物。SG2057?種?效抗腫瘤劑[1]。IC50&TargetPyrrolobenzodiazepines體外研究SG2057hasmultilogdifferentialinvitrocytotoxicityagainstapanelofhumantumourcelllineswithameanGI50of212pM.SG2057ishighlyefficientatproducingDNAinterstrandcross-linksincellswhichformrapidlyandpersistovera48hperiod[1].體內研究SG2057(5-60μg/kg;i.v)exhibitsdose-dependentantitumoractivityinhumantumorxenograftmodels[1].AnimalModel:FemaleNCr-nudemiceinjectedwithSKOV-3cells[1]Dosage:5μg/kg,10μg/kg,20μg/kg,30μg/kg,40μg/kg,50μg/kg,60μg/kgAdministration:i.v.;daily,onceaweek,oronceeveryfourdaysResult:Showedsignificantantitumoractivity.REFERENCES[1].JohnAHartley,etal.DNAinterstrandcross-linkingandinvivoantitumoractivityoftheextendedpyrrolo[2,1-c][1,4]benzodiazepinedimerSG2057.InvestNewDrugs.2012Jun;30(3):950-8.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseon