ER degrader 5

ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer[1].

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

ER degrader 5 (compound 27d) (5 days) 抑制 MCF-7 细胞的增殖，IC50 值为 55 nM[1]。 ER degrader 5 阻断 MCF-7 细胞 G0/G1 期细胞周期[1]。 ER degrader 5 (1 nM-10 μM; 24 h) 降解 MCF-7 细胞中的雌激素受体 (ER)[1]。 ER degrader 5 (1-10 μM; 24 h) 显着降低 MCF-7 细胞中GREB1，PGR 和 TFF1 的表达水平[1]。 Western Blot Analysis[1] Cell Line: MCF-7 cells Concentration: 1, 10, 100, 1000, 10000 nM Incubation Time: 24 hours Result: Degraded ER in a dose-dependent manner. Real Time qPCR[1] Cell Line: MCF-7 cells Concentration: 1, 5, 10 μM Incubation Time: 24 hours Result: Decreased the expression levels of GREB1, PGR, and TFF1 in a dose-dependent manner.

ER degrader 5 (compound 27d) (30 mg/kg; i.p. daily for 30 days) 显着抑制 MCF-7 异种移植模型中的肿瘤生长[1]。 ER degrader 5 (3 mg/kg; i.v.) 的半衰期为 1.23 小时，Cmax 为 4497 ng/mL[1]。 ER degrader 5 (30 mg/kg; p.o.) 产生 62.9% 的口服生物利用度[1]。 Animal Model: Female nude mice injected with MCF-7 cells[1] Dosage: 30 mg/kg Administration: I.p. daily for 30 days Result: Inhibited tumor growth and observed no significant body weight loss.

[1]. Lu Y, et, al. Design, synthesis and biological evaluation of fluorinated selective estrogen receptor degraders (FSERDs) --- A promising strategy for advanced ER positive breast cancer. Eur J Med Chem. 2023 May 5;253:115324.