Nitromifene

Nitromifene is an antagonist of estrogen receptor (ER).

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

ER[1]

Nitromifene is an antagonist of estrogen receptor (ER). At 0.5 μM and 1.0 μM concentrations, Nitromifene inhibits MCF 7 cell proliferation to 70% of that in drug-free controls. At higher concentrations, Nitromifene is clearly more effective than other metabolites. Specifically bound estradiol is displaced from intact MCF 7 cells by Nitromifene. Nitromifene is an effective antagonist of the ability of calmodulin (CM) to activate cyclic nucleotide phosphodiesterase[1].

MCF 7 cells are used in this study. The experiment is carried out in 6-well cluster plates. To each well is added 5 mL of a suspension of 2×105 cells in log phase growth. Medium is changed after 48 h and after 96 h, medium is replaced with 5 mL of serum-free medium containing 2 nM of the radioligand. Nitromifene is dissolved in DMSO (5 μL) to give final concentrations of 0, 0.01, 0.03, 0.1, 0.3, 1, 3, and 10 μM. Nonspecific binding is determined in incubations to which the radioinert counterpart of the radioligand is added at a concentration of 1 μM. Incubations are run in triplicate for 1 h at 37°C.

[1]. Ruenitz PC, et al. Characterization of MCF 7 breast cancer cell growth inhibition by the antiestrogen nitromifene (CI 628) and selected metabolites. J Steroid Biochem. 1989 Sep;33(3):365-9.

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