产品描述:
Erteberel is an estrogen receptor beta (ERβ) agonist.{37486} It is selective for ERβ over ERα in reporter assays using PC3 cells expressing the human receptors (EC50s = 0.66 and 19.4 nM, respectively). Ertebrel (5 µM) induces apoptosis and cell cycle arrest at the G2/M phase in U87MG and U251 glioblastoma cells.{34787} It enhances cytotoxicity induced by cisplatin (Item No. 13119), lomustine (Item No. 21237), or bleomycin (Item No. 13877) in U251 cells when used at a concentration of 1 µM. Ertebrel (5 mg/kg) reduces tumor growth in a U251 orthotopic model of glioblastoma in ovariectomized mice. It decreases prostate weight but does not affect serum testosterone or dihydrotestosterone levels in a mouse model of benign prostatic hyperplasia (BPH) when administered at doses of 0.01, 0.025, and 0.05 mg/kg.{34786}