PRO-6E-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEPRO-6ECat.No.:HY-160506CASNo.:2353493-69-1分子式:C??H??Cl?FN?O?分子量:848.75作用靶點(diǎn):PROTACs;c-Met/HGFR;Apoptosis作用通路:PROTAC;ProteinTyrosineKinase/RTK;Apoptosis儲(chǔ)存方式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥100mg/mL(117.82mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.1782mL5.8910mL11.7820mL5mM0.2356mL1.1782mL2.3564mL10mM0.1178mL0.5891mL1.1782mL請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存方式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。BIOLOGICALACTIVITY生物活性PRO-6E是一種具有口服活性的以Cereblon配體為基礎(chǔ)的PROTAC，可以降解MET，在1μM的濃度下對(duì)MKN-45細(xì)胞中MET的最大降解率為81.9%。PRO-6E在體內(nèi)外抑制腫瘤生長(zhǎng)。PRO-6E可以誘導(dǎo)細(xì)胞凋亡(apoptosis)和細(xì)胞周期阻滯(結(jié)構(gòu)備注:(Blue:Cereblon配體(HY-103596),Black:linker；Pink:ALK/c-Met抑制劑Crizotinib(HY-50878))。1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemE體外研究PRO-6E(0.03-10μM;48h)inhibitsthecellgrowthinMKN-45,SNU-638cells[1].PRO‐6?E(1μM;over24h)facilitatesMETdegradationinMKN-45cells[1].PRO‐6?E(0.1-1μM;48h)increaseinthepercentageofG2/MphasecellsanddecreaseinthepercentageofSphasecellsinMKN-45cells[1].CellViabilityAssay[1]CellLine:MKN-45,SNU-638cellsConcentration:0,0.03,0.1,0.3,1,3,10μMIncubationTime:48hResult:Inhibitedthecellgrowth.CellCycleAnalysis[1]CellLine:MKN-45cellsConcentration:0,0.1,0.3,1,3μMIncubationTime:48hResult:IncreasedinthepercentageofG2/MphasecellsanddecreasedinthepercentageofSphasecells.WesternBlotAnalysis[1]CellLine:MKN-45cellsConcentration:0,0.03,0.1,0.3,1,3μMIncubationTime:12,24,36,48,and72hResult:facilitatedMETdegradationover24hours.體內(nèi)研究PRO-6E(oralgavage;30?mg/kg/dayfor15days)inhibitstumorgrowthinMKN‐45cell‐derivedxenografttumormodel[1].AnimalModel:MKN‐45cell‐derivedxenografttumormodel[1]Dosage:30?mg/kg/dayfor15daysAdministration:OralgavageResult:Inhibitedtumorgrowth.REFERENCES2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEChenJJ,etal.Crizotinib-basedproteolysistargetingchimerasuppressesgastriccancerbypromotingMETdegradation.CancerSci.2023;114(5):1958-1971.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch