| 4-Hydroxytamoxifenestrogen receptor modulator |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.32%
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| Cas No. | 68392-35-8 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)ethyl)phenol compound with sec-butylbenzene (1:1) | ||
| Canonical SMILES | OC1=CC=C(C=C1)C(C)C2=CC=C(C=C2)OCCN(C)C.CCC(C)C3=CC=CC=C3 | ||
| Formula | C28H37NO2 | M.Wt | 419.60 |
| Solubility | ≥42mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 27 and 18 μM for MCF-7 and MDA-MB-231 cell proliferation
4-Hydroxytamoxifen is an estrogen receptor modulator.
Estrogen receptor can be selectively stimulated or inhibited, providing promising therapeutic opportunities for auto-immune diseases, prostate and breast cancer, as well as depression.
In vitro: Previous study was conducted to evaluate the effects of tamoxifen and its active metabolite 4-hydroxytamoxifen on isolated rat cardiac myocyte mechanical function and calcium handling. Results showed that myocytes treated with 4-hydroxytamoxifen had similarly to tamoxifen-treated cells to both calcium handling and contractility [1].
In vivo: Previous animal study compared the extent of DNA adduct formation in SD rats treated with seven tamoxifen or 4-hydroxytamoxifen. Results showed that the liver weights and microsomal rates were not changed by tamoxifen or 4-hydroxytamoxifen treatment. Moreover, the uterine weights were significantly decreased and uterine peroxidase activity was marginally decreased in tamoxifen or 4-hydroxytamoxifen treated rats. In addition, hepatic DNA adduct levels in rats treated with 4-hydroxytamoxifen did not differ from control rats. Similaryly, the adduct levels in uterus DNA from rats treated with tamoxifen or 4-hydroxytamoxifen were not different from those in control rats [2].
Clinical trial: Previous clinical study showed that the antiproliferative effect of 4-hydroxytamoxifen gel to breast skin was similar to that of oral tamoxifen, but the effects on endocrine and coagulation parameters decreased [3].
References:[1] 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. [2] Beland FA,McDaniel LP,Marques MM. Comparison of the DNA adducts formed by tamoxifen and 4-hydroxytamoxifen in vivo. Carcinogenesis.1999 Mar;20(3):471-7.[3] Lee O et al. A randomized phase II presurgical trial of transdermal 4-hydroxytamoxifen gel versus oral tamoxifen in women with ductal carcinoma in situ of the breast. Clin Cancer Res.2014 Jul 15;20(14):3672-82.
