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Cat. Number
H9711
Chemical Name
(Z)-4-Hydroxytamoxifen
CAS Number
68047-06-3
Mol. Formula
C26H29NO2
Mol. Weight
387.51
Qty 1
5mg
Appearance
White to off white powder
Application Notes
≥98%
Solubility
Soluble in DMSO, ethanol (20mg/ml) or methanol (10mg/ml); insoluble water.
Storage condition
-20°C
References

(Z)-4-Hydroxytamoxifen is the more active isomer of 4-hydroxytamoxifen. 4-Hydroxytamoxifen is the active metabolite of tamoxifen, a selective estrogen receptor modulator (SERM) that acts as an agonist or antagonist in various tissues. 4-Hydroxytamoxifen exhibits anticancer chemotherapeutic activity, inducing autophagy and vacuole formation as well as KRAS degradation in various cancer cell lines. In cardiac myocytes, 4-hydroxytamoxifen decreases Ca2+ amplitude, slowing relaxation and decreasing contractility.

参考文献:

Asp ML, Martindale JJ, Metzger JM. Direct, differential effects of tamoxifen, 4-hydroxytamoxifen, and raloxifene on cardiac myocyte contractility and calcium handling. PLoS One. 2013 Oct 24;8(10):e78768. PMID: 24205315.

Kohli L, Kaza N, Coric T, et al. 4-Hydroxytamoxifen induces autophagic death through K-Ras degradation. Cancer Res. 2013 Jul 15;73(14):4395-405. PMID: 23722551.

Schwartz JA, Zhong L, Deighton-Collins S, et al. Mutations targeted to a predicted helix in the extreme carboxyl-terminal region of the human estrogen receptor-alpha alter its response to estradiol and 4-hydroxytamoxifen. J Biol Chem. 2002 Apr 12;277(15):13202-9. Erratum in: J Biol Chem 2002 Jul 5;277(27):24842. PMID: 11823467.

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