AZD1208-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAZD1208hydrochlorideCat.No.:HY-15604ACASNo.:1621866-96-3分⼦式:C₂₁H₂₂ClN₃O₂S分⼦量:415.94作⽤靶点:Pim;Autophagy;Apoptosis作⽤通路:JAK/STATSignaling;Autophagy;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:83.3mg/mL(200.27mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4042mL12.0210mL24.0419mL5mM0.4808mL2.4042mL4.8084mL10mM0.2404mL1.2021mL2.4042mLBIOLOGICALACTIVITY⽣物活性AZD1208hydrochloride⼀种有效的，具有⼝服活性的，具有⾼度选择性的PIM抑制剂[1]。IC50&TargetPIM[1]体外研究AZD1208hydrochlorideshowsgoodantiproliferativeactivityinamegakaryoblasticleukemiacellline,MOLM-16,withGI50valueslessthan100nM[1].AZD1208hydrochloride(10μM)inhibitsthegrowthofRamoscells,andat1μM,stronglyinhibitsPIMkinasesinallcellsat1μM.AZD1208hydrochlorideinducesapoptosis,andPIM2knockdownismainlyassociatedwithanalterationofthecellcycle[2].ThecombinationofAZD1208hydrochlorideandAZD2014rapidlyactivatesAMPKα,anegativeregulatoroftranslationmachinerythroughmTORC1/2signalinginAMLcells;profoundlyinhibitsAKTand4EBP1activation;and1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEsuppressespolysomeformation[3].PROTOCOLCellAssay[1]MOLM-16cells,purchasedfromDSMZandculturedinRPMIcontaining10%fetalbovineserum(FBS)and1%L-glutamine,areplatedat20,000cellsperwellin96wellplatesovernight.Cellsaretreatedfor72hourswithcompound(includingAZD1208hydrochloride)orcontrolvehicle(dimethylsulfoxide)andcellviabilityismeasuredaftertheadditionofCellTiter-Bluefor4hoursat37˚CandreadingoffluorescenceonaTecanInfinite®200.TheGI50isdeterminedbycalculatinggrowthateachdoserelativetovehicletreatedcellsandcellviabilityatthetimeoftreatment[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Science.2017Dec1;358(6367):eaan4368.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•NatCommun.2019Apr23;10(1):1844.•eNeuro.2019Aug22;6(4):ENEURO.0003-19.2019.•ExpTherMed.November25,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DakinLA,etal.Discoveryofnovelbenzylidene-1,3-thiazolidine-2,4-dionesaspotentandselectiveinhibitorsofthePIM-1,PIM-2,andPIM-3proteinkinases.BioorgMedChemLett.2012Jul15;22(14):4599-604.[2].KreuzS,etal.LossofPIM2enhancestheanti-proliferativeeffectofthepan-PIMkinaseinhibitorAZD1208innon-Hodgkinlymphomas.MolCancer.2015Dec8;14:205.[3].HaradaM,etal.ThenovelcombinationofdualmTORinhibitorAZD2014andpan-PIMinhibitorAZD1208inhibitsgrowthinacutemyeloidleukemiaviaHSFpathwaysuppression.Oncotarget.2015Nov10;6(35):37930-47.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform