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

在DEN诱导的大鼠中,Toremifene在最高测试剂量下,提高肝细胞癌和肾上腺样瘤的发生率.

在肿瘤细胞中,Toremifene（5-10 mM ）能够上调TRPM-2和TGF beta1的mRNA的水平。在人乳腺癌细胞中,Toremifene（7.5 mM ）能够诱导细胞凋亡或发生程序性死亡。在DMBA诱导的大鼠乳腺肿瘤中,Toremifene通过抑制有丝分裂活性和修改大量自发凋亡来影响细胞周期的。

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].