|
产品描述： AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer |
|
靶点：
Androgen Receptor;AndrogenReceptor |
体内研究：
AZD3514 (10-100 mg/kg; p.o. once daily for 6 days) inhibits AR signaling in rats. AZD3514 (50 mg/kg; p.o. once daily for 30 days) inhibits prostate tumor growth. AZD3514 (50-100 mg/kg; p.o. once daily for 3 days) significantly reduces nuclear AR protein in vivo |
参考文献：
1. Bradbury RH, et al. Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer. Bioorg Med Chem Lett. 2013 Apr 1;23(7):1945-8. 2. Loddick SA, et al. AZD3514: a small molecule that modulates androgen receptor signaling and function in vitro and in vivo. Mol Cancer Ther. 2013 Sep;12(9):1715-27. 3. Omlin A, et al. AZD3514, an oral selective androgen receptor down-regulator in patients with castration-resistant prostate cancer - results of two parallel first-in-human phase I studies. Invest New Drugs. 2015 Jun;33(3):679-90. |
|
溶解性：
Soluble in DMSO |
|
保存条件：
-20°C |
配置溶液浓度参考：
|
1mg |
5mg |
10mg |
| 1 mM |
1.925 ml |
9.624 ml |
19.247 ml |
| 5 mM |
0.385 ml |
1.925 ml |
3.849 ml |
| 10 mM |
0.192 ml |
0.962 ml |
1.925 ml |
| 50 mM |
0.038 ml |
0.192 ml |
0.385 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京