4-Hydroxytamoxifen
description
Tamoxifen is a modulator of the of the estrogen receptor, with tissue specific agonistic and antagonistic effects. 4-hydroxy Tamoxifen is the active metabolite of tamoxifen that is also generated in the liver by the CYP2D6 enzyme. It exhibits a greater potency than the parent compound and is reported to be cytostatic and prevent cancerous cells from dividing. 4-hydroxy Tamoxifen is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers.
Additional Information
Applications:
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FA
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Synonyms:
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afimoxifene, 4OH-tamoxifen, 4-monohydroxytamoxifen
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Formulation:
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Crystalline solid
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Chemical Name:
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4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
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Molecular Formula:
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C26H29NO2 |
Molecular Weight: |
387.5
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CAS Number
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68392-35-8
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Purity:
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≥98%
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Storage Conditions:
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Product should be kept at -20°C.
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References:
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Jordan, V. C., COLLINS, M. M., ROWSBY, L., & Prestwich, G. (1977). A monohydroxylated metabolite of tamoxifen with potent antioestrogenic activity. Journal of Endocrinology, 75(2), 305-316. Seeger, H., Huober, J., Wallwiener, D., & Mueck, A. O. (2004). Inhibition of human breast cancer cell proliferation with estradiol metabolites is as effective as with tamoxifen. Hormone and metabolic research= Hormon-und Stoffwechselforschung= Hormones et metabolisme, 36(5), 277-280. Desta, Z., Ward, B. A., Soukhova, N. V., & Flockhart, D. A. (2004). Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. Journal of Pharmacology and Experimental Therapeutics, 310(3), 1062-1075. |