Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. It has been found to be both estrogenic and antiproliferative in ER-positive endocrine-resistant breast cancer cell lines that overexpress protein kinase C alpha (PKCα).
A large proportion of breast cancer patients have a tumor expressing estrogen receptor (ER). Compounds that block the effects of estrogen in tumor tissues are considered as promising therapeutic options for breast cancer patients. Estrogen receptor modulator 1 is a selective and orally active estrogen receptor modulator with a pIC50 of 0.46[1]. Estrogen receptor modulator 1 at a concentration of 100 nM stimulated the proliferation of T47D:A18/neo cells compared to the control group. The incubation with 100 nM estrogen receptor modulator 1 also increased colony formation in T47D:A18/neo cells, but prevented T47D:A18/PKCα and T47D:A18-TAM1 colony formation. Estrogen receptor modulator 1 at 100 nM also induced apoptosis and inhibited growth of MCF-7:5C cells. In athymic mice inoculated with T47D:A18/PKCα cells, oral administration with estrogen receptor modulator 1 (1.5 mg/day) for two weeks significantly reduced tumor volume compared to the non-treated group. Daily administration of estrogen receptor modulator 1 (1.5 mg/day) for two weeks also resulted in significant tumor regression in mice with T47D:A18-TAM1 xenograft[2].
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