| Identification | Back Directory | [Name]
4Hydroxy Tamoxifen | [CAS]
82413-23-8 | [Synonyms]
4'-Hydroxy TaMoxifen (contains up to 10% E isoMer)
4-[(1Z)-1-[[4-[2-(Dimethylamino)ethoxy]phenyl]phenylmethylene]propyl]phenol | [Molecular Formula]
C26H29NO2 | [MOL File]
82413-23-8.mol | [Molecular Weight]
387.51 |
| Chemical Properties | Back Directory | [Appearance]
White Solid | [Melting point ]
150-153°C | [Boiling point ]
514.4±50.0 °C(Predicted) | [density ]
1.092±0.06 g/cm3(Predicted) | [storage temp. ]
Amber Vial, -20°C Freezer, Under Inert Atmosphere | [solubility ]
Chloroform (Slightly), Dichloromethane, Methanol (Slightly) | [form ]
Solid | [pka]
10.32±0.15(Predicted) | [color ]
White to Off-White | [Stability:]
Light Sensitive |
| Hazard Information | Back Directory | [Chemical Properties]
White Solid | [Uses]
A metabolite of Tamoxifen (T006000). | [Description]
4’-hydroxy Tamoxifen is one of five main phase I metabolites of tamoxifen , a well-known estrogen receptor antagonist in breast but partial estrogen receptor agonist in endometrium. 4’-hydroxy Tamoxifen is a product of cytochrome P450 (CYP)2D6 and CYP2B6 activity. With the addition of a hydroxyl group, 4’-hydroxy tamoxifen has been shown to have a higher affinity for estrogen receptors compared to tamoxifen. At 10-100 μM, 4’-hydroxy tamoxifen is cytotoxic, in a non-apoptotic manner, to HEC-1B and HEC-1A human endometrial adenocarcinoma cell lines. | [References]
[1] ROLAND L?SER . In vivo and in vitro antiestrogenic action of 3-hydroxytamoxifen, tamoxifen and 4-hydroxytamoxifen[J]. European Journal of Cancer and Clinical Oncology, 1985, 21 8: Pages 985-990. DOI: 10.1016/0277-5379(85)90119-1
[2] H KIM CREWE. Metabolism of tamoxifen by recombinant human cytochrome P450 enzymes: formation of the 4-hydroxy, 4’-hydroxy and N-desmethyl metabolites and isomerization of trans-4-hydroxytamoxifen.[J]. Drug Metabolism and Disposition, 2002, 32 1: 869-874. DOI: 10.1124/dmd.30.8.869
[3] H SEEGER. Inhibition of human breast cancer cell proliferation with estradiol metabolites is as effective as with tamoxifen.[J]. Hormone and Metabolic Research, 2004, 36 5: 277-280. DOI: 10.1055/s-2004-814480
[4] MARIA E CUEVAS Tracey E L. In vitro cytotoxicity of 4’-OH-tamoxifen and estradiol in human endometrial adenocarcinoma cells HEC-1A and HEC-1B.[J]. Oncology reports, 2015, 33 1: 464-470. DOI: 10.3892/or.2014.3565
[5] GIORGIA URBINATI. Therapeutic potential of new 4-hydroxy-tamoxifen-loaded pH-gradient liposomes in a multiple myeloma experimental model.[J]. Pharmaceutical Research, 2010, 27 2: 327-339. DOI: 10.1007/s11095-009-0023-z |
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BOC Sciences
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| Company Name: |
BOC Sciences
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16314854226 |
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www.bocsci.com |
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Energy Chemical
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