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RU 58668

Cat. No. 3224

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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 Activity

Pure 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.

Technical Data

M.Wt:

658.76

Formula:

C₃₄F₄₃F₅O₅S

Solubility:

Soluble to 100 mM in DMSO and to 100 mM in ethanol

Purity:

>95 %

Storage:

Store at +4°C

CAS No:

151555-47-4

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Van de Velde et al (1996) RU 58668: Further in vitro and in vivo pharmacological data related to its antitumoral activity. J.Steroid Molec.Biol. 59 449.

Muller et al (1998) Partial antagonism between steroidal and nonsteroidal antiestrogens in human breast cancer cell lines. Cancer Res. 58 263. PMID: 9443403.

Ameller et al (2004) Drug delivery systems for oestrogenic hormones and antagonists: the need for selective targeting in estradiol-dependent cancers. J.Steroid Molec.Biol. 92 1.

If you know of a relevant citation for this product please let us know.

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