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Specifications Synonym: (Z)-1-(p-Dimethylaminoethoxyphenyl)-1,2-diphenyl-1-butene, trans-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamineCAS Number: 10540-29-1Linear Formula: C6H5C(C2H5)=C(C6H5)C6H4OCH2CH2N(CH3)2Molecular Weight: 371.51EC Number: 234-118-0MDL number: MFCD00010454PubChem Substance ID: 24900307General 'Tamoxifen is a selective estrogen response modifier (SERM), protein kinase C inhibitor and anti-angiogenetic factor. Tamoxifen is a prodrug that is metabolized to active metabolites 4-hydroxytamoxifen (4-OHT) and endoxifen by cytochrome P450 isoforms CYP2D6 and CYP3A4. In breast cancer, the gene repressor activity of tamoxifen against ERBB2 is dependent upon PAX2. Blocks estradiol-stimulated VEGF production in breast tumor cells.Preparation Note Tamoxifen is soluble in chloroform at 50 mg/ml and yields a clear, colorless to faint yellow solution. It is also soluble in methanol, ethanol, 2-propanol and propylene glycol. Stock solutions of tamoxifen can also be prepared in DMSO at 10 mM. However, it is practically insoluble in water (solubility is <0.01%, 20° C). Solutions are sensitive to UV light, and DMSO solutions are stable when stored at -20° C in the dark.Application Tamoxifen has been used to facilitate the recombination of ect2flox allele in mouse organs91. It has also been used to study its effect on lipopolysaccharide (LPS)-induced microglial activation92.Biochem/physiol Actions Protein kinase C inhibitor. Induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-stimulated VEGF production in breast tumor cells.Assay: =99%MP: 97-98 °C(lit.)Solubility: H2O: insoluble <0.1% at 20 °C; chloroform: soluble50 mg/mL, clear, colorless to faintly yellow; 2-propanol: soluble; DMSO: soluble; ethanol: soluble; methanol: soluble; propylene glycol: solubleStorage Temp.: 2-8°CGene Information: human ... CYP1A2, EBP, ESR1, ESR2, ESRRA; rat ... Ar, Esr1
