MD-222-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMD-222Cat.No.:HY-134823CASNo.:2136246-72-3分⼦式:C₄₈H₄₇Cl₂FN₆O₆分⼦量:893.83作⽤靶点:MDM-2/p53;PROTACs;E1/E2/E3Enzyme作⽤通路:Apoptosis;PROTAC;MetabolicEnzyme/Protease储存⽅式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:200mg/mL(223.76mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.1188mL5.5939mL11.1878mL5mM0.2238mL1.1188mL2.2376mL10mM0.1119mL0.5594mL1.1188mL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(sealedstorage,awayfrommoisture)。-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%salineSolubility:5mg/mL(5.59mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(5.59mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性MD-222⼀种⾸创的⾼效的于PROTAC的MDM2降解剂。MD-222由Cereblon和MDM2配体组成。MD-222诱导MDM2蛋⽩快速降解并激活细胞中的野⽣型p53。MD-222具有抗癌作⽤。IC50&TargetMDM2体外研究MD-222(1-30nM;1-2hours)treatmentshowsveryeffectiveinreducingthelevelsofMDM2proteinandincreasingthelevelsofp53inatime-anddose-dependentmannerinRS4;11andRS4;11/IRMI-2cells[1].MD-222(30-100nM;6hours)iseffectiveinincreasingtheexpressionofseveralp53-targetedgenes,suchasMDM2,CDKN1A,andPUMAinRS4;11cells,indicatingstrongactivationofp53[2].MD-222(4days)showscellgrowthinhibitoryactivityinRS4;11cellswithanIC50of5.5nM,andhasnoeffectonRS4;11/IRMI-2,MDA-MB-231andMDA-MB-468cells[1].WesternBlotAnalysis[1]CellLine:RS4;11andRS4;11/IRMI-2cellsConcentration:1nM,3nM,10nM,30nMIncubationTime:1hour,2hoursResult:ReducedthelevelofMDM2andincreasedthelevelofp53.RT-PCR[2]CellLine:RS4;11cellsConcentration:30nM,100nMIncubationTime:6hoursResult:Increasdtheexpressionofseveralp53-targetedgenes,suchasMDM2,CDKN1A,andPUMA.REFERENCES[1].JiulingYang,etal.SimpleStructuralModificationsConvertingaBonafideMDM2PROTACDegraderintoaMolecularGlueMolecule:ACautionaryTaleintheDesignofPROTACDegraders.JMedChem.2019Nov14;62(21):9471-9487.[2].LiY,etal.DiscoveryofMD-224asaFirst-in-Class,HighlyPotent,andEfficaciousProteolysisTargetingChimeraMurineDoubleMinute2DegraderCapableofAchievingCompleteandDurableTumorRegression.JMedChem.2019Jan24;62(2):448-466.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical