Anticancer-agent-108-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEAnticanceragent108Cat.No.:HY-149240分子式: C??H?NO?S?分子量: 383.4作用靶點(diǎn): P-glycoprotein作用通路: MembraneTransporter/IonChannel儲(chǔ)存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Anticanceragent108(Compound3.10)是一種有效的P-gp抑制劑，具有抗腫瘤活性且對(duì)正常和假正常細(xì)胞的毒性較小，對(duì)С57BL/6小鼠無(wú)急性毒性作用。體外研究Anticanceragent108(10μM;48h)significantlyinhibitstheproliferationofcancercells[1].Anticanceragent108(50,100,250,500nM;72h)inhibitstheproliferationofKB-3-1cells[1].Anticanceragent108(0.5,2.5,5μM;3,24h)usesendoplasmicreticulum(ER)stresstoinduceapoptosis[1].Anticanceragent108(5,10μM;24h)inducesapoptosisofMDA-MB-231cells[1].CellProliferationAssay[1]CellLine:60cancercelllinesrepresentingninedifferenttypes(leukemia,melanoma,lung,colon,CNS,ovarian,renal,prostate,andbreastcancers)Concentration:10μMIncubationTime:48hResult:Possessedprominentantitumoractivity(meangrowth?61.06%;therangeofgrowth?99.55to18.52).Inaddition,inhibitedthegrowthof25testedcancercelllineswithpercentgrowthof<0,andshowednotonlycytostaticeffectbutalsocytotoxicproperties.CellProliferationAssay[1]CellLine:KB-3-1cells1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEConcentration:50,100,250,500nMIncubationTime:72hResult:Almost14timesbiggercomparingtosurvivalfractionafterincubationofKB-3-1cellswithdoxorubicininthesameconcentration(100nM)usedasapositivecontrol.However,atapplying500nMconcentration,didnotobservethegrowthofKB-3-1cellcoloniesafter72hofdrugexposure.WesternBlotAnalysis[1]CellLine:KB-3-1cellsConcentration:0.5,2.5,5μMIncubationTime:3,24hResult:Dose-dependentlyincreasedtheexpressionofBIP(immunoglobulinheavychainbindingprotein)at24hours,whilenochangesinthelevelsoftheaboveproteinswerefoundat3hours.ApoptosisAnalysis[1]CellLine:MDA-MB-231breastcancercellsConcentration:5,10μMIncubationTime:24hResult:InducedapoptosisintheMDA-MB-231breastcancercellsproceedingthroughtwopathways,extrinsicandintrinsic.體內(nèi)研究Anticanceragent108(singledose,i.p.20mg/kg)doesnotinducealossofbodymassinanimals,theirrapiddeath,leukopenia,erythropenia,andadecreaseinthelevelofhemoglobininbloodofmice.AnimalModel:С57BL/6mice[1]Dosage:20mg/kgAdministration:singledose,i.p.20mg/kgResult:Didnotinducealossofbodymassinanimals,theirrapiddeath,leukopenia,erythropenia,andadecreaseinthelevelofhemoglobininbloodofmice.REFERENCES2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEIvasechkoI,etal.Moleculardesign,synthesisandanticanceractivityofnewthiopyrano[2,3-d]thiazolesbasedon5-hydroxy-1,4-naphthoquinone(juglone).EurJMedChem.2023Apr5;252:115304.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform