An active metabolite of tamoxifen that is formed by the action of CYP2D6 in human liver; inhibits MCF-7 and MDA-MB 231 cell proliferation with IC50 values of 27 and 18 µM

(E/Z)-4-hydroxy Tamoxifen – 5 mg

Brand:
Cayman
CAS:
68392-35-8
Storage:
-20
UN-No:
Non-Hazardous - /

Tamoxifen (Item No. 13258) is a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. Although it is an antagonist of ER action in breast tissue, it acts as an ER agonist in bone and blood vessels and a partial ER agonist in uterine tissues. (E/Z)-4-hydroxy Tamoxifen is an active metabolite of tamoxifen that is formed by the action of cytochrome P450 2D6 in human liver.{28446} It exhibits more potent estrogen agonist/antagonist activity than its parent compound and can inhibit MCF-7 and MDA-MB-231 cell proliferation with IC50 values of 27 and 18 µM, respectively.{28444} (E/Z)-4-hydroxy Tamoxifen has been used to stimulate LC3 lipidation and formation of autophagic vesicles in a superoxide-dependent manner.{28445}  

 

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Description

An active metabolite of tamoxifen that is formed by the action of CYP2D6 in human liver; inhibits MCF-7 and MDA-MB 231 cell proliferation with IC50 values of 27 and 18 µM, respectively; stimulates LC3 lipidation and formation of autophagic vesicles

Formal name: 4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-phenol

Synonyms:  4-hydroxy Tamoxifen|4-OHT|Afimoxifene

Molecular weight: 387.5

CAS: 68392-35-8

Purity: ≥98% (E) and (Z) isomers (50:50)

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Cancer|Autophagy||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Toxicology|Drug Metabolism|Cytochrome P450||Research Area|Toxicology|Drug Metabolism|Drug Metabolites

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