Antitumor-agent-115-DataSheet-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEAntitumoragent-115Cat.No.:HY-155745CASNo.:2759277-20-6分子式:C??H??ClNO?分子量:347.96作用靶點:Apoptosis作用通路:Apoptosis儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Antitumoragent-115(SS-12)是一種有效的體外抗腫瘤化合物，其對小鼠乳腺癌細胞系4T1細胞的IC50值為0.34μM-24.14μM。Antitumoragent-115具有阻滯小鼠乳腺癌細胞系4T1細胞周期，降低線粒體膜電位，誘導細胞凋亡的作用，針對4T1細胞活力的IC50值為8-25μmol/L，可用于乳腺癌疾病的研究[1]。體外研究Antitumoragent-115(SS-12)(1.25μM,10μM,40μM,24h)induces4T1cellapoptosisprimarilybyarrestingcellcycleatG0/G1[1].Antitumoragent-115(15μM,30μM,60μM,24h)inhibits4T1cellmigrationandinvasion[1].Antitumoragent-115(10μM,24h)inducesapoptosisof4T1cellsthroughmitochondriapathway[1].CellViabilityAssay[1]CellLine:4T1cellConcentration:1-128μMIncubationTime:24,48,72hResult:Inhibited4T1cellsproliferationwithIC50valueof8-25μM.ApoptosisAnalysis[1]CellLine:4T1cellConcentration:1.25μM,10μM,40μM1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEIncubationTime:24hResult:Increasedapoptosisratesof4T1cellatconcentrationof1.25μM.CellCycleAnalysis[1]CellLine:4T1cellConcentration:1.25μM,10μM,40μMIncubationTime:24hResult:IncreasedtheproportionintheG0/G1phaseanddecreasedintheSandG2/Mphasesof4T1cells.CellMigrationAssay[1]CellLine:4T1cellConcentration:15μM,30μM,60μMIncubationTime:24hResult:Expandedthewoundareaandinhibitedcellmigrationandinvasionatconcentrationof0.03μM.WesternBlotAnalysis[1]CellLine:4T1cellConcentration:10μMIncubationTime:24hResult:Improvedthecleavedcaspase-3expressionandandBaxexpression,butinhibitedtheanti-apoptosisproteinBcl2expressionin4T1cells.體內(nèi)研究Antitumoragent-115(SS-12)(10mgstachydrine/kgequivale,200μLforOraladministration)hasgreaterbioavailabilityinrats[1].Antitumoragent-115(0.2mmol/kgforOraladministration)hasanti-tumoreffectsinbreastcancermodelmiceandimprovesmorphologicalstructureofspleeninmodelmice[1].AnimalModel:Rats[1]Dosage:10mgstachydrine/kgequivale,200μLAdministration:Oraladministration(p.o.)2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEResult:Exhibitedhighsystemicexposurewith6.10μg/mLofCmaxvalueand14.75hμg/mLofAUC0-tvalue.AnimalModel:Tumor-bearingmice[1]Dosage:0.2mmol/kgAdministration:Oraladministration(p.o.)Result:Inhibitoryratewas51.47%(P<0.01)DisplayedsignificanttumorcellshrinkageandlargervoidareasintumortissuesExhibitedmoreweightlossthanthemodelgroupandothertreatmentgroups,increasedofbothASTandALTlevelsandreducedspleenindexofthetumor-bearingmiceREFERENCESZengH,etal.Synthesis,characterizationandanti-breastcanceractivitiesofstachydrinederivatives.EurJMedChem.2023Jul26;259:115679.McePdfHeightCaution:Producthasnotbeenfullyvalidatedforme