T5648-1G Display Image

Tamoxifen free base

Code: T5648-1G D2-231

Application

Tamoxifen has been used to facilitate the recombination of ect2flox allele in mouse organs91. It has also been used to study its ef...


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£269.00 1G

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.

Features and Benefits

This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

General description

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.

Packaging

1, 5 g in glass bottle

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.

antibiotic activity spectrumneoplastics
assay≥99%
Gene Informationhuman ... CYP1A2(1544), EBP(10682), ESR1(2099), ESR2(2100), ESRRA(2101)rat ... Ar(24208), Esr1(24890)
InChI keyNKANXQFJJICGDU-QPLCGJKRSA-N
InChI1S/C26H29NO/c1-4-25(21-11-7-5-8-12-21)26(22-13-9-6-10-14-22)23-15-17-24(18-16-23)28-20-19-27(2)3/h5-18H,4,19-20H2,1-3H3/b26-25-
mode of actionenzyme | inhibits
mp97-98 °C (lit.)
originatorAstraZeneca
SMILES stringCCC(c1ccccc1)=C(/c2ccccc2)c3ccc(OCCN(C)C)cc3
solubilitymethanol: soluble, ethanol: soluble, H2O: insoluble ﹤0.1% at 20 °C, chloroform: soluble 50 mg/mL, clear, colorless to faintly yellow, DMSO: soluble, 2-propanol: soluble, propylene glycol: soluble
storage temp.2-8°C
Code
Description
Unit Size
List Price
Qty
T5648-5G
Unit:5G
List Price: £953.00
Source:List Price
ADD
Cas Number10540-29-1
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