In Vitro: TRIM24/BRPF1-IN-2 (compound 20l) (0-10 μM, 48 h) suppresses the growth of the prostate cell lines (C4-2B, LNCaP, and 22Rv1), with IC50 values of 0.78±0.15, 1.07±0.47, and 0.82±0.26 μM, respectively. TRIM24/BRPF1-IN-2 inhibits gene and protein expression in prostate cancer cells. TRIM24/BRPF1-IN-2 displays reasonable Caco-2 permeability.
In Vivo: TRIM24/BRPF1-IN-2 (compound 20l) (50 mg/kg, IP, once daily for 21 days) suppresses tumor growth (TGI = 53%) without exhibiting noticeable toxicity.