Antitumor-agent-96-DataSheet-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEAntitumoragent-96Cat.No.:HY-149972分子式: C??H??N?O?分子量: 416.56作用靶點: Apoptosis作用通路: Apoptosis儲存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Antitumoragent-96(CompoundD34)是一種有效的MRE11抑制劑。Antitumoragent-96通過與MRE11結(jié)合并抑制其內(nèi)切酶功能下調(diào)HR通路。Antitumoragent-96誘導CM細胞凋亡(apoptosis)。IC50&TargetMRE11[1]體外研究Antitumoragent-96(CompoundD34;72h)hasaparticularcytotoxicityselectivityinCMcellsofCM-AS16(IC50=2.9±0.1μM),CRMM2(IC50=0.7±0.0μM),CM2005.1(IC50=1.0±0.1μM),andCRMM1(IC50=1.3±0.3μM),comparedtoocularmelanoma,cutaneousmelanomaandnormalcells[1].Antitumoragent-96(0.1-10μM;48h)inducesCRMM1cellapoptosis[1].Antitumoragent-96(0.3μM;0-72h)inhibitsCRMM1cellmigration[1].Antitumoragent-96(0.3-10μM;48h)augmentsDNAdamageaccumulationinCMcellsanddown-regulatesMRNcomplexinHRpathway[1].CellProliferationAssay[1]CellLine:CM-AS16,CRMM2,CM2005.1,CRMM1,HL7702andPIG1Concentration:IncubationTime:72hResult:InhibitedproliferationwithIC50sof2.9±0.1,0.7±0.0,1.0±0.1,1.3±0.3,25.6±0.8and32.9±0.3μMagainstCM-AS16,CRMM2,CM2005.1,CRMM1,HL7702andPIG1,respectively.ApoptosisAnalysis[1]1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellLine:CRMM1cellsConcentration:0.1,0.3,1,3and10μMIncubationTime:48hResult:SignificantlyledtoCRMM1cellsdeathovertheconcentrationsof0.3μM.Theapoptoticratesroseto80%whenincubatedat3μM.CellMigrationAssay[1]CellLine:CRMM1cellsConcentration:0.3μMIncubationTime:0,24,48and72hResult:Inhibitedmigrationratefrom70%to45%at72h.WesternBlotAnalysis[1]CellLine:CRMM1andCRMM2Concentration:0.3,1,3and10μMIncubationTime:48hResult:Stimulatedtumorsuppressorp53.Inducedsignificantaccumulationofγ-H2AX.ThethreeMRNsubunitsMRE11,RAD50,andNBS1,weresignificantlydown-regulatedinadose-dependentmanner.TheexpressionofMRNdownstreameffectors,includingBCRA1andRAD51,werealsoinhibitedinbothCRMM1andCRMM2cells.體內(nèi)研究Antitumoragent-96dihydrochloride(CompoundD34dihydrochloride;10and20mg/kg;i.p.;fivetimesperweekfor28days)showsanti-tumoreffectinmice[1].AnimalModel:NCGmice,CRMM1xenografttumormodel[1]Dosage:10mg/kgand20mg/kgAdministration:Intraperitonealinjection,fivetimesperweekfor28daysResult:Suppressedtumorgrowth.Didnotinduceanyconspicuousbodyweightloss.REFERENCES[1].WeiJ,etal.Drugrepurposingofpropafenonetodiscovernovelanti-tumoragentsbyimpairinghomologousrecombinationtodelayDNA2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEdamagerecoveryofrarediseaseconjunctivalmelanoma.EurJMedChem.2023Mar15;250:115238.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic