ORM-15341 |
Catalog No.GC32402 |
ORM-15341 est un antagoniste puissant et complet de l'AR humain (hAR) avec des valeurs IC50 de 38 nM, comme le montrent les tests de transactivation dans les cellules AR-HEK293 exprimant de manière stable le hAR complet et une construction de gène rapporteur de la luciférase sensible aux androgènes.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1297537-33-7
Sample solution is provided at 25 µL, 10mM.
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.
Average Rating: 5
(Based on Reviews and 8 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *