Anticancer-agent-289-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAnticanceragent289Cat.No.:HY-180260分⼦式:C₁₂H₁₈BCl₂NO₂分⼦量:289.99作⽤靶点:ReactiveOxygenSpecies(ROS)作⽤通路:Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Anticanceragent289⼀种H2O2响应性抗癌前药。Anticanceragent289表现出H2O2诱导的DNA烷基化活性，能选择性抑制⾼ROS表达的癌细胞(相较于⾮恶性细胞)的增殖，并在体内显著抑制肿瘤⽣长且⽆可见毒性。Anticanceragent289可⽤于三性乳腺癌(TNBC)的研究[1]。体外研究Anticanceragent289(compound10a)(0-200μM,48h)exhibitspreferentialcytotoxicitytowardMDA-MB-468cellswithanIC50of5.1μMbutMCF-10Acellswitha3-foldhigherIC50of16.2μM[1].Anticanceragent289hasagoodaqueoussolubility(74μM)andmoderatepermeability(logPe=−5.67)atatphysiologicalpH7.4,enhancesapassivediffusionunderacidicconditions(amodestincrease(logPe=−5.22)atpH6.4)[1].CellViabilityAssay[1]CellLine:MDA-MB-468andMCF-10AcellsConcentration:0.049,0.098,0.195,0.391,0.781,1.563,3.125,6.250,12.5,25,50,100and200μMIncubationTime:48hResult:ExhibitedsignificantgrowthinhibitioninMDA-MB-468cells,withanIC50of5.1μM.Observeda3-foldhigherIC50of15.2μM.体内研究Anticanceragent289(compound10a)(5.0mg/kg,i.p.dailyfor8weeks)selectivelysuppressestumorgrowthwhilesparingnormaltissuesandhasanantitumoractivitywithafavorablesafetyprofileinaMDA-MB-468cells-inducedxenograftmicemodel[1].Anticanceragent289(15mg/kg,i.p.,once)hasfavorablesafetyprofile,minimizingoff-targeteffectswhen1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEcombinationwiththepreciselydeuteratedanalogueinaMDA-MB-468cells-inducedxenograftmicemodel[1].AnimalModel:MDA-MB-468cells(7.5×106)induced-femalenudemice(8weeks)[1]Dosage:5.0mg/kgAdministration:i.p.dailyfor7weeksResult:Displayedsignificantlysuppressedtumorgrowthapproximately11%.Hasatumorgrowthinhibitionrate(IR)valueof89%.Inhibitstumorweights.Causednotreatment-relatedmortalityoradverseeffectsoccurred,andsteadilyincreasedbodyweights.Revealednostructuralabnormalitiesorpathologicalchanges(includingliver,kidneys,spleen,lungs,heart).AnimalModel:MDA-MB-468cells(2×106)induced-femalenudemice(8weeks)[1]Dosage:15mg/kgAdministration:i.p.,onceResult:RevealedthepresenceofphaseIImetabolites,arisingfromglucuronidationofphenolicintermediatesandexhibitadiagnosticM/M+5isotopicpatternsubstratesforUDP-glucuronosyltransferase(UGT)-catalyzedconjugatedwithuridinediphosphateglucuronicacid.REFERENCES[1].SaxonE,etal.PrecisionDeuterationinSearchofInVivoMetabolites,andActivationPathway.JMedChem.2025Dec11;68(23):25026-25037.HMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedica