Erteberel

Erteberel is an estrogen receptor beta (ERβ) agonist.¹ 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.² 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.³

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1. Sareddy, G.R., Li, X., Liu, J., et al. Selective estrogen receptor β agonist LY500307 as a novel therapeutic agent for glioblastoma. Sci. Rep. 6:24185, (2016).

2. Norman, B.H., Dodge, J.A., Richardson, T.I., et al. Benzopyrans are selective estrogen receptor β agonists with novel activity in models of benign prostatic hyperplasia. J. Med. Chem. 49(21), 6155-6157 (2006).