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.

DETAILS

Purity: ≥98%
Synonyms: afimoxifene, 4OH-tamoxifen, 4-monohydroxytamoxifen
Cas Number: 68392-35-8
References: 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.
Application: FA
Formulation: Crystalline solid
Chemical Name: 4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
Molecular Weight: 387.5
Molecular Formula: C26H29NO2
Storage Conditions: Product should be kept at -20°C.
Pubchem Openeye Can Smiles: CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3