Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki of 11 nM for rat wild-type AR (wtAR) and IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation[1]. Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation[1]. Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants[1]. Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer[1].
Molecular Weight:
398.85
Purity:
99.73
CAS Number:
[1297538-32-9]
Formula:
C19H19ClN6O2
Target:
Androgen Receptor
Application Notes:
MCE Product type: Reference compound
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