Anticancer-agent-84-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAnticanceragent84Cat.No.:HY-151471CASNo.:2714510-72-0分⼦式:C₅₇H₆₇N₇O₉分⼦量:994.18作⽤靶点:c-Myc作⽤通路:Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Anticanceragent84抗癌剂。Anticanceragent84通过稳定G-四链体(G4)结构来抑制c-MYC的转录。Anticanceragent84可⽤于癌症研究。IC50&TargetIC50:5.0μM(HepG2);3.9μM(MDA-MB-231);＞100μM(HBL-100)[1]体外研究Anticanceragent84hascytotoxicityincancercells(HepG2,MDA-MB-231)andnormalcells(HBL-100)withIC50valuesof5.0μM,3.9μMand＞100μM,respectively[1].Anticanceragent84displaysgoodc-MYCG4bindingandstabilizationabilities[1].Anticanceragent84blocksc-MYCtranscriptionbytargetingthepromoterG4,leadingtoc-MYC-dependentcancercelldeathintriple-negativebreastcancercellMDA-MB-23[1].Anticanceragent84(2μM)significantlydisruptsthebindingofthethreeproteins(NM23-H2,BLMandDHX36)toc-MYCG4withIC50valuesof0.16μM,2.3μMand7.0μM,respectively[1].Anticanceragent84(0-5μM)impactsc-MYC-relatedeventsinTNBC,includingproliferation,invasion,cellcycle,andapoptosis[1].WesternBlotAnalysis[1]CellLine:MDA-MB-231cellsConcentration:1.25,2.5,5μMIncubationTime:48hResult:DecreasedthemRNAlevelsofc-MYC.1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellCycleAnalysis[1]CellLine:MDA-MB-231cellsConcentration:1.25,2.5,5μMIncubationTime:24hResult:CouldarrestMDA-MB-231cellsattheSubG0phase.ApoptosisAnalysis[1]CellLine:MDA-MB-231cellsConcentration:1.25,2.5,5μMIncubationTime:24hResult:InducedearlyapoptosisandnecrosisinMDA-MB-231cells.RT-PCR[1]CellLine:MDA-MB-231cellsConcentration:1.25,2.5μMIncubationTime:24hResult:Exhibitedrelativelyweakeffectsonothergenesandsuppressedc-MYCtranscriptionbytargetingc-MYCG4.CellCytotoxicityAssay[1]CellLine:MDA-MB-231cellsConcentration:IncubationTime:48hResult:Displayedgoodcytotoxicityagainstvariouscancercells,includingMDA-MB-231,MCF-7,HepG2,andSiHaanddisplayedlesscytotoxicityagainstnormalHBL-100andNCM460cells.CellProliferationAssay[1]CellLine:MDA-MB-231cellsConcentration:1.25,2.5,5μMIncubationTime:10days2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Exhibitsgoodantiproliferativeactivity.CellInvasionAssay[1]CellLine:MDA-MB-231cellsConcentration:1.25,2.5,5μMIncubationTime:24hResult:ObviouslydecreasedtheinvasionwithanIC50valueof1.7μM.体内研究Anticanceragent84(i.p.;2.5mg/kg;daily;for24days)significantlyinhibitstumorgrowthintheMDAMB-231mousexenograftmodelaccompaniedbyc-MYCdownregulation[1].AnimalModel:BALB/C-nu/numice(female,five-week-aged,10−12g)[1]Dosage:2.5mg/kgAdministration:intraperitoneally,daily,for24daysResult:Exhibitedpotentantitumoractivityandcouldactasac-MYCrepressorinvivo.REFERENCES[1].Mao-LinLi,etal.Design,Synthesis,andEvaluationofNewSugar-SubstitutedImidazoleDerivativesasSelectivec-MYCTranscriptionRepressorsTargetingthePromoterG-Quadruplex.JMedChem.2022Sep19.McePdfHeightCaution:Producthasnotbeenfullyv