PROTAC-BRD4-Degrader-8-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPROTACBRD4Degrader-8Cat.No.:HY-138555分?式:C??H??F?N?O??S?分?量:1102.23作?靶點:PROTACs;EpigeneticReaderDomain作?通路:PROTAC;Epigenetics儲存?式:-20°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實驗DMSO:90mg/mL(81.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM0.9073mL4.5363mL9.0725mL5mM0.1815mL0.9073mL1.8145mL10mM0.0907mL0.4536mL0.9073mL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(protectfromlight)。-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(dāng)?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(dāng)保存；體內(nèi)實驗的?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:≥4.5mg/mL(4.08mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥4.5mg/mL(4.08mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性PROTACBRD4Degrader-8?種由vonHippel-Lindau配體和BRD4配體相連的PROTAC，對BRD4BD1和BD2的IC50值分別為1.1nM和1.4nM。PROTACBRD4Degrader-8能夠有效降解PC3前列腺癌細(xì)胞中的BRD4蛋?。IC50&TargetIC50:1.1nM(BRD4BD1),1.4nM(BRD4BD2)[1]體外研究PROTACBRD4Degrader-8(compound8;6days)inhibitstheproliferationofPC3prostatecancercells,withanIC50of28nM[1].PROTACBRD4Degrader-8(4h)suppressesMYCgenetranscriptinMV4-11AMLcells,withanIC50of11nM[1].PROTACBRD4Degrader-8(4h)potentlydegradestheBRD4proteininPC3prostatecancercells,withanDC50of7.5nM[1].REFERENCES[1].DragovichPS,et,al.Antibody-MediatedDeliveryofChimericBRD4Degraders.Part2:ImprovementofInVitroAntiproliferationActivityandInVivoAntitumorEfficacy.JMedChem.2021Mar11;64(5):2576-2607.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400