AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor ( IC 50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC 50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer.