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ARantagonist17

Cat.No.:HY-178148

CASNo.:3064715-04-1

分⼦式:C₂₁H₂₀F₃N₃O₄S₂

分⼦量:499.53

作⽤靶点:AndrogenReceptor

作⽤通路:VitaminDRelated/NuclearReceptor

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性ARantagonist17是⼀种具有选择性、⼝服活性、不易透过⾎脑屏障的雄激素受体(AR)拮抗剂(IC50=0.010

μM)，可有效阻断AR⼆聚化和核转位，并在多种去势抵抗性前列腺癌(CRPC)细胞中表现出强效作⽤。AR

antagonist17对多种耐药性AR突变体表现出优异的疗效。ARantagonist17在LNCaP异种移植模型中抑制

肿瘤⽣长，且⽆明显毒性。ARantagonist17可⽤于去势抵抗性前列腺癌(CRPC)的研究[1]。

体外研究ARantagonist17(CompoundC13)showsexcellentARantagonisticactivityandantiproliferativeeffects

againstAR-positivePCacelllines(LNCaP(IC50=1.02μM),C4−2B(IC50=3.86μM),22RV1(IC50=8.45

μM),andVCaP(IC50=5.72μM)),accompaniedbylowtoxicityonnormalcelllines3T3andGes-1(IC50

20μM)[1].

ARantagonist17(0.2-2μM,2weeks)completelyinhibitsclonalproliferationinLNCaPcells[1].

ARantagonist17(0.02-2μM,48h)dose-dependentlysuppressesthedihydrotestosterone(DHT)-induced

transcriptionallevelsofprostate-specificantigen(PSA),andremarkablys