Chemical Name: (11β,17β)-11-[4-[[5-[(4,4,5,5,5-Pentafluoropentyl)sulfonyl]pentyl]oxy]phenylestra-1,3,5,(10)-triene-3,17-diol
Biological ActivityPure antiestrogen that downregulates estrogen receptor expression (IC50 = 0.04 nM). Displays potent antiproliferative activity in vitro (IC50 = 0.035 - 0.09 nM in MCF-7 cells) and causes long term regression of tamoxifen-resistant MCF-7 xenografts in vivo.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Partial antagonism between steroidal and nonsteroidal antiestrogens in human breast cancer cell lines.
Muller et al.
Cancer Res., 1998;58:263
RU 58668: Further in vitro and in vivo pharmacological data related to its antitumoral activity.
Van de Velde et al.
J.Steroid Molec.Biol., 1996;59:449
Drug delivery systems for oestrogenic hormones and antagonists: the need for selective targeting in OE-dependent cancers.
Ameller et al.
J.Steroid Molec.Biol., 2004;92:1
Citations for RU 58668
The citations listed below are publications that use Tocris products. Selected citations for RU 58668 include:
2 Citations: Showing 1 - 2
Activating ESR1 Mutations Differentially Affect the Efficacy of ER Antagonists.
Authors: Toy Et al.
Cancer Discov 2017;7:277
Oestrogen Receptor-α binds the FOXP3 promoter and modulates regulatory T-cell function in human cervical cancer.
Authors: Adurthi Et al.
Sci Rep 2017;7:17289
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