PRO-6E-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEPRO-6ECat.No.:HY-160506CASNo.:2353493-69-1分子式:C₄₂H₄₄Cl₂FN₇O₇分子量:848.75作用靶点:PROTACs;c-Met/HGFR;Apoptosis作用通路:PROTAC;ProteinTyrosineKinase/RTK;Apoptosis储存方式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(117.82mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.1782mL5.8910mL11.7820mL5mM0.2356mL1.1782mL2.3564mL10mM0.1178mL0.5891mL1.1782mL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。-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。BIOLOGICALACTIVITY生物活性PRO-6E是一种具有口服活性的以Cereblon配体为基础的PROTAC，可以降解MET，在1μM的浓度下对MKN-45细胞中MET的最大降解率为81.9%。PRO-6E在体内外抑制肿瘤生长。PRO-6E可以诱导细胞凋亡(apoptosis)和细胞周期阻滞(结构备注:(Blue:Cereblon配体(HY-103596),Black:linker；Pink:ALK/c-Met抑制剂Crizotinib(HY-50878))。1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemE体外研究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.体内研究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—您身边的抑制剂大师www.MedChemEChenJJ,etal.Crizotinib-basedproteolysistargetingchimerasuppressesgastriccancerbypromotingMETdegradation.CancerSci.2023;114(5):1958-1971.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch