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抑制剂描述:

产品名称:Enzalutamide

产品别名:见爱必信官网

英文别名:Enzalutamide

靶点:Androgen Receptor

CAS:915087-33-1

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

MDV3100 is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

溶解性:DMSO :92 mg/mL warmed (198.08 mM)

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.

体内研究:Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg.

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