Abacavir-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAbacavirhydrochlorideCat.No.:HY-17423ECASNo.:136777-48-5分⼦式:C₁₄H₁₉ClN₆O分⼦量:322.79作⽤靶点:HIV;Apoptosis;ReverseTranscriptase;Telomerase作⽤通路:Anti-infection;Apoptosis;CellCycle/DNADamage储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Abacavirhydrochloride⼀种具有⼝服活性、竞争性核苷酸逆转录酶(nucleosidereversetranscriptase)抑制剂。Abacavirhydrochloride可抑制HIV的复制。Abacavirhydrochloride在前列腺癌细胞系中显⽰出抗癌活性。Abacavirhydrochloride可透过⾎脑屏障，抑制端粒酶(telomerase)活性。体外研究Abacavirhydrochloride(15and150μM,0-120h)inhibitscellgrowth,affectscellcycleprogression,inducessenescenceandmodulatesLINE-1mRNAexpressioninprostatecancercelllines[1].Abacavirhydrochloride(15and150μM,18h)significantlyreducescellmigrationandinhibitscellinvasion[1].Abacavirhydrochlorideinducesfatapoptosis[4].CellProliferationAssay[1]CellLine:PC3,LNCaPandWI-38Concentration:15μMand150μMIncubationTime:0,24,48,72and96hoursResult:Showedadose-dependentgrowthinhibitiononPC3andLNCaP.CellCycleAnalysis[1]CellLine:PC3,LNCaPandWI-38Concentration:150μM1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:0,18,24,48,72,96and120hoursResult:CausedaveryhighaccumulationofcellsinSphaseinPC3andLNCaPcells,andG2/MphaseincrementwasobservedinPC3cells.CellMigrationAssay[1]CellLine:PC3,LNCaPandWI-38Concentration:15and150μMIncubationTime:18hoursResult:Significantlyreducedcellmigration.CellInvasionAssay[1]CellLine:PC3,LNCaPandWI-38Concentration:15and150μMIncubationTime:18hoursResult:Significantlyinhibitedcellinvision.体内研究Abacavirhydrochloride(100and200mg/kg,p.o.;4h)dose-dependentlypromotesthrombusformation[2].Abacavirhydrochloride(50mg/kg/d;i.p.;14d)with0.1mg/kg/dDecitabine(HY-A0004)enhancessurvivalofhigh-riskmedulloblastoma-bearingmice[3].AnimalModel:Malemice(9-weeksold,22-30g)-wild-type(WT)C57BL/6orhomozygousknockout(P2rx7KO,B6.129P2-P2rx7tm1Gab/J)[2]Dosage:Route1:2.5,5,and7.5μg/mL,100μLRoute2:100and200mg/kgAdministration:Intrascrotalororaladministrationfor4hResult:Dose-dependentlypromotedthrombusformation.AnimalModel:NSGTMmice,patient-derivedxenograft(PDX)cellsofnon-WNT/non-SHH,Group3andofSHH/TP53-mutatedmedulloblastoma[3]Dosage:50mg/kg/dwith0.1mg/kg/dDecitabineAdministration:Intraperitonealinjection,dailyfor14daysResult:Inhibitedtumorgrowthandenhancedmousesurvival.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•IntJAntimicrobAgents.2019Dec;54(6):814-819.•JMolLiq.2018Feb;251:345-357.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CarliniF,etal.Thereversetranscriptioninhibitorabacavirshowsanticanceractivityinprostatecancercelllines.PLoSOne.2010Dec3;5(12):e14221.[2].Collado-DiazV,etal.AbacavirInducesArterialThrombosisinaMurineModel.JInfectDis.2018Jun20;218(2):228-233.[3].GringmuthM,etal.EnhancedSurvivalofHigh-RiskMedulloblastoma-BearingMiceafterMultimodalTreatmentwithRadiotherapy,Decitabine,andAbacavir.IntJMolSci.2022Mar30;23(7):3815.[4].McComseyGA,etal.Improvementsinlipoatrophy,mitochondrialDNAlevelsandfatapoptosisafterreplacingstavudinewithabacavirorzidovudine.AIDS.2005Jan3;19(1):15-23.McePdfHeightCaution:Producthasn