Tamoxifen

Catalog No.S1238 Batch:S123803

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Technical Data

Formula

C26H29NO
Molecular Weight 371.51 CAS No. 10540-29-1
Solubility (25°C)* In vitro Ethanol 74 mg/mL (199.18 mM)
DMSO 7.5 mg/mL (20.18 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
10%DMSO 40%PEG300 5%Tween80 45%ddH2O
0.75mg/ml Taking the 1 mL working solution as an example, add 100 μL of 7.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
Targets
estrogen receptor [1]
In vitro

TAM treatment inhibits significantly MCF7 cell proliferation. Low doses of TAM are able to induce structural chromosomal aberrations (deletions, isochromosomes, translocations, and dicentric chromosomes) in both ER+ and ER- breast cancer cells. This genotoxic effect is higher in those cell lines with HER2 gene amplification[2]. Whereas TAM at lower concentrations (0.1-1 μM) induces a cell-cycle arrest, pharmacological concentrations (above 5 μM) of TAM have been found to induce apoptosis of breast cancer cells. 5 μM TAM rapidly induced sustained activation of ERK1/2 in ER-positive breast cancer cell lines (MCF-7 and T47D)[3]
In vivo

Tamoxifen (TAM) is widely used for both treatment and prevention of breast cancer. However, it is also carcinogenic in human uterus and rat liver[2]. Tm-inducible Cre-loxP systems are being used in broad areas of research and are providing important biologic insights in tissue development, maintenance, and function. Tamoxifen-induced nuclear localization of Cre recombinase is time- and dose-dependent. Higher doses of tamoxifen induce recombination weeks following administration and Lower doses of tamoxifen induce recombination up to one week following administration. Duration of tamoxifen-induced gene recombination is also dose-dependent. Administration of high Tm doses leads to extended CreER nuclear localization. Tm treatment induces side effects that may have physiologic consequences in Tm-inducible models[4].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    MCF7 and T47D

  • Concentrations

    10-6 mol/L

  • Incubation Time

    24, 48, and 96 h

  • Method

    48 h before the addition of E2 and TAM, cells were washed with 5 mL phosphate-buffered saline (PBS) and then switched to phenol red-free RPMI-1640 containing 10% charcoal-stripped FBS. E2 and TAM were dissolved in absolute ethanol and diluted in the media at 10-8 mol/L and 10-6 mol/L, respectively, and then added to the culture medium at 24, 48, and 96 h.
Animal Study:

[4]
  • Animal Models

    Pdx1PB-CreERTm mice

  • Dosages

    --

  • Administration

    s.c.

Customer Product Validation

, , Oncotarget, 2015, 6(4):2315-30.

Selleck's Tamoxifen has been cited by 63 publications

Therapeutic targeting nudix hydrolase 1 creates a MYC-driven metabolic vulnerability [ Nat Commun, 2024, 15(1):2377] PubMed: 38493213
Small molecule inhibitor targeting the Hsp70-Bim protein-protein interaction in estrogen receptor-positive breast cancer overcomes tamoxifen resistance [ Breast Cancer Res, 2024, 26(1):33] PubMed: 38409088
An Integrated Approach of Bioassays and Non-Target Screening for the Assessment of Endocrine-Disrupting Activities in Tap Water and Identification of Novel Endocrine-Disrupting Chemicals [ Toxics, 2024, 12(4)247] PubMed: 38668470
Dual-targeting class I HDAC inhibitor and ATM activator, SP-1-303, preferentially inhibits estrogen receptor positive breast cancer cell growth [ PLoS One, 2024, 19(7):e0306168] PubMed: 39008483
Myelin-Specific microRNA-23a/b Cluster Deletion Inhibits Myelination in the Central Nervous System during Postnatal Growth and Aging [ Genes (Basel), 2024, 15(4)402] PubMed: 38674338
Single cell profiling of female breast fibroadenoma reveals distinct epithelial cell compositions and therapeutic targets [ Nat Commun, 2023, 10.1038/s41467-023-39059-3] PubMed: 37328469
CircRREB1 mediates lipid metabolism related senescent phenotypes in chondrocytes through FASN post-translational modifications [ Nat Commun, 2023, 14(1):5242] PubMed: 37640697
Single cell profiling of female breast fibroadenoma reveals distinct epithelial cell compositions and therapeutic targets [ Nat Commun, 2023, 14(1):3469] PubMed: 37328469
CircRREB1 mediates lipid metabolism related senescent phenotypes in chondrocytes through FASN post-translational modifications [ Nat Commun, 2023, 14(1):5242] PubMed: 37640697
Dlg1 deletion in microglia ameliorates chronic restraint stress induced mice depression-like behavior [ Front Pharmacol, 2023, 14:1124845] PubMed: 36909184

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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