Date published: 2026-4-4

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Idoxifene (CAS 116057-75-1)

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Alternate Names:
1-[2-[4-[(1E)-1-(4-Iodophenyl)-2-phenyl-1-buten-1-yl]phenoxy]ethyl]-pyrrolidine; 1-[2-[4-[(1E)-1-(4-Iodophenyl)-2-phenyl-1-butenyl]phenoxy]ethyl]-pyrrolidine; (E)-1-[2-[4-[1-(4-iodophenyl)-2-phenyl-1-butenyl]phenoxy]ethyl]-pyrrolidine
CAS Number:
116057-75-1
Purity:
≥98%
Molecular Weight:
523.45
Molecular Formula:
C28H30INO
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Idoxifene is a non-steroidal estrogen antagonist. It is also structurally analogous to tamoxifen. Idoxifene may act to have potent antagonist activity against tamoxifen, which may be due to its ability to inhibit the synthesis of both estrogen and testosterone. Idoxifene does not bind to the estrogen receptors, but it blocks tamoxifen from binding and thus prevents the formation of active complexes with DNA.


Idoxifene (CAS 116057-75-1) References

  1. Idoxifene derivatives are less reactive to DNA than tamoxifen derivatives, both chemically and in human and rat liver cells.  |  Osborne, MR., et al. 1999. Carcinogenesis. 20: 293-7. PMID: 10069467
  2. Idoxifene antagonizes estradiol-dependent MCF-7 breast cancer xenograft growth through sustained induction of apoptosis.  |  Johnston, SR., et al. 1999. Cancer Res. 59: 3646-51. PMID: 10446976
  3. Idoxifene, a novel selective estrogen receptor modulator, is effective in a rat model of adjuvant-induced arthritis.  |  Badger, AM., et al. 1999. J Pharmacol Exp Ther. 291: 1380-6. PMID: 10565864
  4. The selective oestrogen receptor modulators idoxifene and raloxifene have fundamentally different cell-specific oestrogen-response element (ERE)-dependent/independent mechanisms in vitro.  |  Nuttall, ME., et al. 2000. Eur J Cancer. 36 Suppl 4: S63-4. PMID: 11056323
  5. Effects of idoxifene and estradiol on NF-kappaB activation in cultured rat hepatocytes undergoing oxidative stress.  |  Omoya, T., et al. 2001. Liver. 21: 183-91. PMID: 11422781
  6. Reduction of oxidative stress and AT1 receptor expression by the selective oestrogen receptor modulator idoxifene.  |  Bäumer, AT., et al. 2001. Br J Pharmacol. 134: 579-84. PMID: 11588112
  7. Idoxifene causes endothelium-dependent, nitric oxide-mediated vasorelaxation in male rats.  |  Christopher, TA., et al. 2002. Eur J Pharmacol. 446: 139-43. PMID: 12098595
  8. Idoxifene and estradiol enhance antiapoptotic activity through estrogen receptor-beta in cultured rat hepatocytes.  |  Inoue, H., et al. 2003. Dig Dis Sci. 48: 570-80. PMID: 12757172
  9. Antioxidant and antiapoptotic activities of idoxifene and estradiol in hepatic fibrosis in rats.  |  Lu, G., et al. 2004. Life Sci. 74: 897-907. PMID: 14659978
  10. Inhibitory effects of idoxifene on hepatic fibrosis in rats.  |  Zhou, YJ., et al. 2005. Acta Pharmacol Sin. 26: 581-6. PMID: 15842777
  11. Pharmacokinetics and biodistribution of radiolabelled idoxifene: prospects for the use of PET in the evaluation of a novel antioestrogen for cancer therapy.  |  Young, H., et al. 1995. Nucl Med Biol. 22: 405-11. PMID: 7550016
  12. Effects of a new antioestrogen, idoxifene, on cisplatin- and doxorubicin-sensitive and -resistant human ovarian carcinoma cell lines.  |  Sharp, SY., et al. 1994. Br J Cancer. 70: 409-14. PMID: 8080723
  13. The novel anti-oestrogen idoxifene inhibits the growth of human MCF-7 breast cancer xenografts and reduces the frequency of acquired anti-oestrogen resistance.  |  Johnston, SR., et al. 1997. Br J Cancer. 75: 804-9. PMID: 9062399
  14. Idoxifene is equipotent to tamoxifen in inhibiting mammary carcinogenesis but forms lower levels of hepatic DNA adducts.  |  Pace, P., et al. 1997. Br J Cancer. 76: 700-4. PMID: 9310233
  15. Idoxifene: a novel selective estrogen receptor modulator prevents bone loss and lowers cholesterol levels in ovariectomized rats and decreases uterine weight in intact rats.  |  Nuttall, ME., et al. 1998. Endocrinology. 139: 5224-34. PMID: 9832463

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Idoxifene, 5 mg

sc-488293
5 mg
$347.00