ERα-degrader-10-生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

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ERαdegrader10

Cat.No.:HY-168099

分⼦式:C₂₉H₂₅ClN₂O₂

分⼦量:468.97

作⽤靶点:EstrogenReceptor/ERR

作⽤通路:VitaminDRelated/NuclearReceptor

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性ERαdegrader10是⼀种强效、选择性且具有⼝服活性的雌激素受体α(ERα)降解剂。ERαdegrader10表

现出强效的ERα结合亲和⼒(IC50为24.0nM)和降解能⼒(EC50为5.3nM)。ERαdegrader10通过蛋⽩酶

体介导的途径降解ERα。ERαdegrader10可⽤于乳腺癌的研究。

IC50TargetERα

24nM(IC50)

体外研究ERαdegrader10(CompoundA20)showsoutstandinganti-proliferativeeffectsonMCF-7cells(IC50=0.28

nM).ERαdegrader10(CompoundA20;0.1-1000nM;1-48h)showstheERαdegradationinaconcentration-

dependentmanner,andthedegradationeffectisbestat24hviaaproteasome-mediatedprotein

degradationpathway[1].

ERαdegrader10(10-100nM;24h)couldsuppresstheERαsignaltransduction,inducingtheMCF-7cell

cyclearrestinG1phase[1].

WesternBlotAnalysis[1]

CellLine:MCF-7cells

Concentration:0.1nM,1nM,10nM,50nM,100nM,500nM,1000nM

Incub