R547-Standard-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemER547(Standard)Cat.No.:HY-10014RCASNo.:741713-40-6分子式:C₁₈H₂₁F₂N₅O₄S分子量:441.45作用靶点:CDK;ReferenceStandards;GSK-3;Apoptosis作用通路:CellCycle/DNADamage;Others;PI3K/Akt/mTOR;StemCell/Wnt;Apoptosis储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性R547(Standard)是R547(HY-10014)的分析标准品。本产品用于研究及分析应用。R547是一种高效、选择性的，口服有效的ATP竞争性的CDK抑制剂，对CDK1/cyclinB、CDK2/cyclinE和CDK4/cyclinD1作用的Ki值分别为2nM、3nM、1nM[1][2][3][4][5REFERENCESChuXJ,DePintoW,BartkovitzD,SoSS,VuBT,PackmanK,LukacsC,DingQ,JiangN,WangK,GoelzerP,YinX,SmithMA,HigginsBX,ChenY,XiangQ,MoliterniJ,KaplanG,GravesB,LoveyA,FotouhiN.Discoveryof[4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone(R547),apotentandselectivecyclin-dependentkinaseinhibitorwithsignificantinvivoantitumoractivity.JMedChem.2006Nov2;49(22):6549-60.BayésM,RabassedaX,ProusJR.Gatewaystoclinicaltrials.MethodsFindExpClinPharmacol.2007Jul-Aug;29(6):427-37.MartinF,ThomsonTM,SewerA,DrubinDA,MathisC,WeisenseeD,PrattD,HoengJ,PeitschMC.Assessmentofnetworkperturbationamplitudesbyapplyinghigh-throughputdatatocausalbiologicalnetworks.BMCSystBiol.2012May31;6:54.DePinto,WandaetalInvitroandinvivoactivityofR547:apotentandselectivecyclin-dependentkinaseinhibitorcurrentlyinphaseIclinicaltrialsMolecularCancerTherapeutics(2006),5(11),2644-2658Jones,CliffordD.;Andrews,DavidM.Imidazolepyrimidineamidesaspotent,orallybioavailablecyclin-dependentkinaseinhibitorsBioorganic&MedicinalChemistryLetters(2008),18(24),6486-6489McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-37