Quinacrine-hydrochloride-hydrate-Mepacrine-hydrochloride-hydrate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEQuinacrinehydrochloridehydrateCat.No.:HY-13735BCASNo.:6151-30-0Synonyms:Mepacrinehydrochloridehydrate;SN-390hydrochloridehydrate分?式:C??H??Cl?N?O?分?量:508.91作?靶點:Parasite;Apoptosis;Autophagy;Mitophagy作?通路:Anti-infection;Apoptosis;Autophagy儲存?式:PleasestoretheproductundertherecommendedconditionsintheCOA.BIOLOGICALACTIVITY?物活性Quinacrinehydrochloridehydrate(Mepacrinehydrochloridehydrate)?種抗瘧劑(antimalarial)，在體內(nèi)外均具有抗腫瘤作?。Quinacrinehydrochloridehydrate抑制NF-κB并激活p53信號轉(zhuǎn)導(dǎo)，誘導(dǎo)腫瘤細胞發(fā)?凋亡(apoptosis)[1]。體外研究Quinacrine(5-20μM;24hours)inhibitsthegrowthofSGC-7901cells[1].Quinacrine(7.5and15μM;24hours)inducesapoptosisinSGC-7901cells,whichisassociatedwithmitochondria-dependentsignalpathwayandinvolvesp53upregulationandcaspase-3activationpathway[1].Quinacrine(15μM;24hours)treatmentsignificantlyincreasedthelevelsofproapoptoticproteins,includingcytochromec,Bax,andp53,anddecreasedthelevelsofantiapoptoticproteinBcl-2,thusshiftingtheratioofBax/Bcl-2infavorofapoptosis[1].CellViabilityAssay[1]CellLine:SGC-7901cellsConcentration:0,5,10,15,and20μMIncubationTime:24hoursResult:Cellviabilitywasinhibitedinadose-dependentmanner,andthemeanIC50valueis16.18μM.ApoptosisAnalysis[1]1/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemECellLine:SGC-7901cellsConcentration:7.5and15μMIncubationTime:24hoursResult:Thepercentageofapoptoticcells,includingtheearlyphaseandlatephaseapoptosis,increasedto26.30%,comparedwithcontrolgroupof3.37%.WesternBlotAnalysis[1]CellLine:SGC-7901cellsConcentration:15μMIncubationTime:24hoursResult:Therelativequantityofcytochromecproteinwasupregulated,increasedfrom0.10to0.24.Therelativequantityofp53proteinwasdramaticallyincreased,from0.06to0.19.TheBax/Bcl-2ratiowasdramaticallyelevatedfrom1.21to2.59.體內(nèi)研究Quinacrine(100mg/kgthreetimesperweekfortwoconsecutiveweeks)significantlysuppressescirculatingblastcellsatdays30/31andincreasesthemediansurvivaltime(MST).Quinacrinedoesnotdecreasethebodyweightoftreatedanimalsatthetesteddose[2].AnimalModel:FemaleSCIDmicewithacutemyeloidleukemia(AML)-PSmodel[2]Dosage:100mg/kgAdministration:Administeredbyoralgavage(po);threetimesaweekfortwoconsecutiveweeksResult:InthefirstAMLmouseinvivostudy,evaluationofcirculatingleukemiccellsdetectedinbloodsamples(inpercentofwhitebloodcells(WBC))atday30/31showed72%humantumorcellsinthecontrolmice,whereasinmicetreatedwithQuinacrine,thiswasonly2.2%.TheMSTofcontrolmicewas34dayswhereasitwas46daysinQuinacrine-treatedmice.?ACSNano.2020Jun23;14(6):7639-7650.Seemorecustomervalidationsonwww.MedChemE2/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].XiaoyangWu,etal.QuinacrineInhibitsCellGrowthandInducesApoptosisinHumanGastricCancerCellLineSGC-7901.CurrTherResClinExp.2012Feb;73(1-2):52-64.[2].AnnaEriksson,etal.Towardsrepositioningofquinacrinefortreatmentofacutemyeloidleukemia-Promisingsynergiesandinvivoeffects.LeukRes.2017Dec;63:41-46.McePdfHeightCaution:Producthasnotbee