| 產品描述： | ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct. IC50 value: 38 nM Target: androgen receptor in vitro: In competitive AR binding assays, the inhibition constant (Ki) values of ORM-15341 was 8 nM. ORM-15341 functions as a full antagonist for all tested mutant ARs , with IC50 of 25, 51, 700, and 1160 nM for wtAR, AR(F876L), AR(T877A), and AR(W741L). |
| 靶點： |
Androgen Receptor;AndrogenReceptor |
| 體外研究： |
The antagonistic properties of the different compounds in a cell - based transactivation assay using an MMT - driven luciferase reporter were determined. For darolutamide, the (S,R)‐ and (S,S)‐diastereomers, and the main in vivo metabolite keto‐darolutamide, a strong antagonistic activity against AR wild type, when stimulating with 1 nM R1881, was found. This was reduced but still significantly better than observed for other AR antagonists when increasing the androgen level used for stimulation to 10 nM. Strong antagonism was also measured for darolutamide, its diastereomers and for keto‐darolutamide when testing the W742C and W742L forms. |
| 體內研究： |
The absorption, distribution, metabolism and excretion properties of darolutamide in rats are reported. Keto-darolutamide was the most abundant metabolite in rat hepatocytes and the only major one in plasma. Interconversion between diastereoisomers was observed. |
| 參考文獻： |
1. Moilanen AM, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms toandrogen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007. 2. Toermaekangas Olli, et al. Preparation of heteroaryl carboxamides as androgen receptor modulators. From PCT Int. Appl. (2012), WO 2012143599 A1 20121026. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.52 ml |
12.6 ml |
25.2 ml |
| 5 mM |
0.504 ml |
2.52 ml |
5.04 ml |
| 10 mM |
0.252 ml |
1.26 ml |
2.52 ml |
| 50 mM |
0.05 ml |
0.252 ml |
0.504 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京