产品描述: | Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator |
靶点: |
IC50: 36 nM (androgen-receptor, in LNCaP cells);AndrogenReceptor; Autophagy |
体内研究: |
Enzalutamide (MDV3100) induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. Enzalutamide shows dose-independent pharmacokinetics at intravenous and oral doses of 0.5-5 mg/kg. |
参考文献: |
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. 4. Kim TH, et al. Pharmacokinetics of enzalutamide, an anti-prostate cancer drug, in rats. Arch Pharm Res. 2015 Nov;38(11):2076-82. |
溶解性: |
DMSO : ≥ 50 mg/mL (107.66 mM) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.153 ml |
10.766 ml |
21.531 ml |
5 mM |
0.431 ml |
2.153 ml |
4.306 ml |
10 mM |
0.215 ml |
1.077 ml |
2.153 ml |
50 mM |
0.043 ml |
0.215 ml |
0.431 ml |
|
注意: |
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