Androgen receptor antagonist 7

Androgen receptor antagonist 7 is an effective androgen receptor (AR) antagonist with an IC50 value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI50 value of 7.9 µM [1].

Research Areas >> Cancer

Signaling Pathways >> Others >> Androgen Receptor

IC50: 1.18 µM[1]

Androgen receptor antagonist 7 (compound 3d) (10 µM；24 h) 显著降低 AR 蛋白表达水平[1]。 Androgen receptor antagonist 7 (20 µM；72 h) 抑制 LAPC-4 和 22Rv1 细胞的增值[1]。 Androgen receptor antagonist 7 (0-20 µM；24、48 和 72 h) 以时间和剂量依赖的方式抑制 AR 的表达，但不诱导细胞凋亡[1]。 Androgen receptor antagonist 7 (10 µM；3 d) 在体外靶向 AR 并降低 AR 的表达[1]。 Western Blot Analysis[1] Cell Line: LAPC-4 cell Concentration: 0-20 µM Incubation Time: 24, 48 and 72 h Result: Showed inhibitory effect. Cell Viability Assay[1] Cell Line: LAPC-4 and 22Rv1 cells Concentration: 20 µM Incubation Time: 72 h Result: Showed antiproliferative effect (cell viability < 40 %).

[1]. Peřina M, et al. A-ring-fused pyrazoles of dihydrotestosterone targeting prostate cancer cells via the downregulation of the androgen receptor. Eur J Med Chem. 2023 Jan 13;249:115086.