SG2057-DRG16-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESG2057Cat.No.:HY-101160CASNo.:260417-62-7Synonyms:DRG16分⼦式:C₃₃H₃₆N₄O₆分⼦量:584.66作⽤靶点:DNAAlkylator/Crosslinker;ADCCytotoxin作⽤通路:CellCycle/DNADamage;Antibody-drugConjugate/ADCRelated储存⽅式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:100mg/mL(171.04mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7104mL8.5520mL17.1040mL5mM0.3421mL1.7104mL3.4208mL10mM0.1710mL0.8552mL1.7104mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.28mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.28mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性SG2057(DRG16)⼀种含有戊⼆氧键的PBD⼆聚体，该键选择性地结合DNA⼩沟中的序列，形成DNA链间和链内交联加合物。SG2057⼀种⾼效抗肿瘤剂[1]。IC50&TargetPyrrolobenzodiazepines体外研究SG2057hasmultilogdifferentialinvitrocytotoxicityagainstapanelofhumantumourcelllineswithameanGI50of212pM.SG2057ishighlyefficientatproducingDNAinterstrandcross-linksincellswhichformrapidlyandpersistovera48hperiod[1].体内研究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