ORM-15341 |
| رقم الكتالوجGC32402 |
ORM-15341 هو خصم قوي وكامل لـ AR (hAR) مع قيم IC البالغة 38 نانومتر كما هو موضح في فحوصات المعاملات في خلايا AR-HEK293 التي تعبر بشكل ثابت عن hAR كامل الطول وبناء الجين مراسل لوسيفيراز المستجيب للأندروجين
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Cas No.: 1297537-33-7
Sample solution is provided at 25 µL, 10mM.
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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 nMTarget: androgen receptorin 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).
[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.
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