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Ralaniten is an antagonist of the androgen receptor N-terminal domain (NTD).1 It inhibits androgen receptor NTD transactivation in a reporter assay (IC50 = 7.4 µM). Ralaniten (10-30 µM) reduces androgen-dependent growth of LNCaP prostate cancer cells. In vivo, ralaniten (50 mg/kg) decreases tumor volume in an LNCaP castration-resistant prostate cancer (CRPC) mouse xenograft model.
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1. An androgen receptor N-