Description

Cancer

Description

Hexestrol binds to Erα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.

Targets

IC₅₀

In Vitro

Hexestrol binds to ERα with EC50 of 0.07 nM and to ERβ with EC50 of 0.175 nM. ^[1] Hexestrol inhibits activity of AKR1B13 with IC50 of 3.2 μM. ^[2] Hexestrol inhibits the d-galactose dehydrogenase activity of thermophilus aldose 1-dehydrogenase with IC50 of 0.063 mM. ^[3] Hexestrol inhibits the dehydrogenase activity of AKR1C20 towards 10 μM 4-androsten-3α-o1-17-one with IC50 values of 2.7 μM. ^[4] Hexestrol inhibits 17HSD5 with IC50 of 30 μM, and inhibits TBER1 with IC50 of 0.8 μM. ^[5] Hexestrol reacts with DNA through the catechol quinone, thus can be a carcinogen. ^[6]

In Vivo

Hexestrol administered intraperitoneally at dose of 6 mg/kg may decrease ovulation in mice, as evident by smaller ovaries and decreased luteal bodies and oocytes. ^[7]

Clinical Trials

Features

Much higher ERβ binding selectivity than Erα

Estrogen Receptor Binding Affinity Assays

Relative binding affinities are determined by a competitive radiometric binding assay, using 10 nM [³H]estradiol as tracer, and purified full-length human ERα and ERβ. Incubations are for 18–24 h at 0 °C, then the receptor-ligand complexes are absorbed onto hydroxyapatite and unbound ligand is washed away. The binding affinities are expressed as relative binding affinity (RBA) values, with the RBA of estradiol set to 100. The values given are the average ± range or SD of two or more independent determinations. Hexestrol is tested as racemate.

Animal Models

adult mice aged 90-120 days

Formulation

Saline

Doses

3 mg/kg and 6 mg/kg

Administration

administered intraperitoneally once daily for 30 days