Toremifene citrate is a selective estrogen receptor modulator (SERM). It is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on the mammary and uterine tissue.

SERM:1±0.3 μM

In tumor cells, Toremifene (5-10 mM ) was able to upregulate the levels of TRPM-2 and TGF beta1 mRNA. In human breast cancer cells, Toremifene (7.5 mM ) was able to induce apoptosis or programmed cell death. In DMBA-induced rat mammary tumors, Toremifene affected the cell cycle by inhibiting mitotic activity and modifying massive spontaneous apoptosis.

In tumor cells, Toremifene (5-10 mM ) was able to upregulate the levels of TRPM-2 and TGF beta1 mRNA. In human breast cancer cells, Toremifene (7.5 mM ) was able to induce apoptosis or programmed cell death. In DMBA-induced rat mammary tumors, Toremifene affected the cell cycle by inhibiting mitotic activity and modifying massive spontaneous apoptosis.

cDNA encoding the human MT1 gene is introduced into CHO cells. Cells are harvested at confluence in Ca2+ and Mg2+ free Hanks' balanced salt solution containing 5 mM EDTA and collected by centrifugation. Cells are homogenized in ice-cold 50 mM Tris–HCl buffer, washed twice, pelleted, and stored at -30°C until the binding assays are conducted. Test compound and 40 pM 2-[ 125I]melatonin are mixed with the thawed homogenate in a total volume of 1 mL and incubated at 25°C for 150 min. The reaction is terminated by addition of 3 mL of icecold buffer followed by vacuum filtration on a Whatman GF/B. The filter is washed twice and radioactivity is counted by a g-counter[1].