For research use only.
Catalog No.S1238 Synonyms: ICI 46474
CAS No. 10540-29-1
Tamoxifen (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.
Selleck's Tamoxifen has been cited by 33 publications
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|Description||Tamoxifen (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.|
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. 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)
Tamoxifen (TAM) is widely used for both treatment and prevention of breast cancer. However, it is also carcinogenic in human uterus and rat liver. 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.
-  Horwitz KB, et al. J Biol Chem, 1978,253(22):8185-91.
-  Rondón-Lagos M, et al. Endocr Relat Cancer. 2016, 23(8):635-50.
-  Zheng A, et al. Endocrinology. 2007, 148(6):2764-77.
|In vitro||DMSO||74 mg/mL (199.18 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04433494||Not yet recruiting||Drug: TY-302: capsule 25mg/50mg ; Tamoxifen: tablet10mg||Breast Cancer|Solid Tumor||TYK Medicines Inc||October 2020||Phase 1|
|NCT04174352||Recruiting||Drug: Tamoxifen|Diagnostic Test: FES PET/CT||ERα+ Breast Cancer|ESR1 Gene Mutation||University of Wisconsin Madison||October 20 2020||Early Phase 1|
|NCT04200066||Not yet recruiting||Drug: Temozolomide Tamoxifen Maprotiline||Glioblastoma|Brain Tumor||University of Rochester||February 1 2020||Phase 1|
|NCT04312347||Recruiting||Drug: Tamoxifen dose adjustment||ER+ Breast Cancer||Nalagenetics Pte Ltd||September 6 2019||Not Applicable|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Could you tell me if you have a protocol for the use of tamoxifen (S1238) in vivo in mouse? Is there an administration way that is better than another?
Tamoxifen (S1238) can be dissolved in 10% ethanol/10% Tween 80/ddH2O at 5 mg/ml clearly. But precipitation will form if the formulation was left at RT for an hour or longer. So we'd suggest that you use it quickly after formulation. Tamoxifen is often administrated via i.p injection.