Anticancer-agent-84-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAnticanceragent84Cat.No.:HY-151471CASNo.:2714510-72-0分?式:C??H??N?O?分?量:994.18作?靶點(diǎn):c-Myc作?通路:Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Anticanceragent84抗癌劑。Anticanceragent84通過穩(wěn)定G-四鏈體(G4)結(jié)構(gòu)來抑制c-MYC的轉(zhuǎn)錄。Anticanceragent84可?于癌癥研究。IC50&TargetIC50:5.0μM(HepG2);3.9μM(MDA-MB-231);＞100μM(HBL-100)[1]體外研究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?邊的抑制劑?師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?邊的抑制劑?師www.MedChemEResult:Exhibitsgoodantiproliferativeactivity.CellInvasionAssay[1]CellLine:MDA-MB-231cellsConcentration:1.25,2.5,5μMIncubationTime:24hResult:ObviouslydecreasedtheinvasionwithanIC50valueof1.7μM.體內(nèi)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