产品信息
抗原名称
Androgen Receptor
商品描述
MDV3100 is an androgen-receptor (AR) antagonist with IC50 of 36 nM.
分子量
464.43
纯度
>98%
可溶性
DMSO ：92 mg/mL warmed (198.08 mM)
外观
White to off-white powder
In vitro(体外研究)
Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys). Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex.
In vivo(体内研究)
Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg.
背景
别名
恩杂鲁胺；MDV-3100；MDV 3100
分子式
C21H16F4N4O2S
CAS号
915087-33-1
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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