Tamoxifen-d₅

Tamoxifen-d₅ is intended for use as an internal standard for the quantification of tamoxifen (Item No. 13258) by GC- or LC-MS. Tamoxifen is an estrogen receptor antagonist (IC₅₀ = 45 nM for the rabbit receptor).¹ It reduces the proliferation of MCF-7 breast cancer cells when used at a concentration of 10 µM.² Tamoxifen is active against S. cerevisiae, C. neoformans, and five Candida species (MICs = 12, 64, and 8-64 µg/ml, respectively).³ It decreases tumor proliferation, weight, and volume in an MCF-7 mouse xenograft model when administered at a dose of 100 µg/animal per day.⁴ Tamoxifen (0.8 mg/kg every two weeks) also reduces proteinuria and increases survival in an NZBWF1 mouse model of systemic lupus erythematosus (SLE).⁵ It can be used as a regulator for Cre-recombinase inducible gene expression in vivo.⁶ Formulations containing tamoxifen have been used in the treatment of estrogen receptor-positive breast cancer.

WARNING This product is not for human or veterinary use.

1. Löser, R., Seibel, K., Roos, W., et al. In vivo and in vitro antiestrogenic action of 3-hydroxytamoxifen, tamoxifen and 4-hydroxytamoxifen. Eur. J. Cancer Clin. Oncol. 21(8), 985-990 (1985).

2. Lippman, M., Bolan, G., and Huff, K. The effects of estrogens and antiestrogens on hormone-responsive human breast cancer in long-term tissue culture. Cancer Res. 36(12), 4595-4601 (1976).

3. Dolan, K., Montgomery, S., Buchheit, B., et al. Antifungal activity of tamoxifen: In vitro and in vivo activities and mechanistic characterization. Antimicrob. Agents Chemother. 53(8), 3337-3346 (2009).

4. Long, B.J., Jelovac, D., Handratta, V., et al. Therapeutic strategies using the aromatase inhibitor letrozole and tamoxifen in a breast cancer model. J. Natl. Cancer Inst. 96(6), 456-465 (2004).

5. Wu, W.-M., Lin, B.-F., Su, Y.-C., et al. Tamoxifen decreases renal inflammation and alleviates disease severity in autoimmune NZB/W F1 mice. Scand. J. Immunol. 52(4), 393-400 (2000).

6. Chen, M., Lichtler, A.C., Sheu, T.-J., et al. Generation of a transgenic mouse model with chondrocyte-specific and tamoxifen-inducible expression of Cre recombinase. Genesis 45(1), 44-50 (2007).