AR antagonist 3

AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally[1].

Research Areas >> Cancer

Signaling Pathways >> Others >> Androgen Receptor

IC50: 0.47 µM (AR)[1]

AR antagonist 3 (compound T1-12) (0.01, 0.1, 1, 10, 100 µM) shows excellent AR antagonistic activity (eGFP IC50= 0.47 μM; PSA IC50= 1.42 μM)[1]. AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) inhibits the proliferation of LNCaP cells[1]. AR antagonist 3 (0.1, 1, 10 µM; 48 h) reduces the protein expression levels of c-Myc and KLK3[1]. AR antagonist 3 (0.01, 0.1, 1, 10, 100 µM) exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM)[1]. AR antagonist 3 (10 µM; 2 h) reduces the DHT-mediated translocation of the AR into the nucleus in LNCaP cells[1]. Cell Viability Assay[1] Cell Line: LNCaP-ARR2PB-eGFP cells Concentration: 0.01, 0.1, 1, 10, 100 µM Incubation Time: Result: Showed excellent AR antagonistic activity (eGFP IC50= 0.47 μM; PSA IC50= 1.42 μM). Cell Proliferation Assay[1] Cell Line: LNCaP, 22Rv1, C4-2, PC3, DU145 cells Concentration: 0.01, 0.1, 1, 10, 100 µM Incubation Time: 3 days Result: Inhibited the proliferation of LNCaP cells.

AR antagonist 3 (intratumorally injected; 2.5 mg/kg; every week for 25 days) inhibits tumor growth and the final tumor growth inhibition is 65%[1]. Animal Model: 6 weeks-old male CB17 SCID mice (specificpathogen-free grade), 18-24 g[1] Dosage: 2.5 mg/kg Administration: intratumorally injected; week; 25 days Result: Inhibited tumor growth and the final tumor growth inhibition is 65%.

[1]. Chai X, et al. Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2. J Med Chem. 2022, 65(3):2507-2521.