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恩杂鲁胺Enzalutamide (MDV3100) 是一种雄激素受体 (androgen receptor (AR)) 拮抗剂,在LNCaP前列腺细胞中抑制AR 的 IC50 值为36 nM。
中文别名:
4-(3-(4-氰基-3-(三氟甲基)苯基)-5,5-二甲基-4-氧代-2-硫氧代咪唑啉-1-基)-2-氟-N-甲基苯甲酰胺;
恩杂鲁胺;
恩扎鲁胺
物化属性:
密度:1.49
折射率:1.629
PSA:108.53000
LOGP:4.51338
[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science, 2009, 324 (5928), 787-790.
[2]. Scher HI, et al. Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet, 2010, 375(9724), 1437-1446.
[3]. Guerrero J, et al. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer. Prostate. 2013 Sep;73(12):1291-305.
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