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RU 58668 is a synthetic steroidal pure antiestrogen that acts as an estrogen receptor antagonist with no measurable agonist activity. It binds to estrogen receptors with high affinity and blocks estrogen-dependent signaling. RU 58668 exhibits potent antiproliferative effects in vitro in estrogen receptor-positive breast cancer cell lines, such as MCF-7, with IC50 values in the sub-nanomolar range. In vivo, it downregulates estrogen receptor expression and induces long-term regression of human mammary carcinoma xenografts, including tamoxifen-resistant tumors, in animal models. It was developed primarily for research on hormone-dependent cancers, especially breast cancer[1][3][5][8].
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