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ORM-15341

Katalog-Nr.GC32402

ORM-15341 ist ein potenter und vollstÄndiger Antagonist fÜr humanes AR (hAR) mit IC50-Werten von 38 nM, wie durch Transaktivierungsassays in AR-HEK293-Zellen gezeigt wurde, die hAR in voller LÄnge und ein Androgen-responsives Luciferase-Reportergenkonstrukt stabil exprimieren.

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ORM-15341 Chemische Struktur

Cas No.: 1297537-33-7

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10mM (in 1mL DMSO)
69,00 $
Auf Lager
5mg
63,00 $
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10mg
108,00 $
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50mg
405,00 $
Auf Lager
100mg
378,00 $
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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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