Ketodarolutamide

MedChem Express

Ketodarolutamide [1297537-33-7]

10

1297537-33-7

Research Use Only

98.72

C19H17ClN6O2

396.83

Ketodarolutamide (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 Ketodarolutamide (ORM-15341) was 8 nM. Ketodarolutamide (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).

ClC1=C(C#N)C=CC(C2=NN(C[C@H](C)NC(C3=NNC(C(C)=O)=C3)=O)C=C2)=C1

-20°C,2°C to 8°C

12352200