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Tamoxifen Citrate

For research use only.

Catalog No.S1972 Synonyms: ICI 46474 Citrate

7 publications

Tamoxifen Citrate Chemical Structure

CAS No. 54965-24-1

Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.

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10mM (1mL in DMSO) GBP 106 In stock
GBP 79 In stock
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Selleck's Tamoxifen Citrate has been cited by 7 publications

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  • Effects of DPN, LY500307, Raloxifene and Tamoxifen on cell viability in BSO-treated FRDA fibroblasts. BSO concentration was 1 mM and all steroid concentrations were 100 nM. Depicted are mean ± SD for n= 8 per group. * indicated p<0.05 versus BSO alone-treated cells.

    University of North Texas Health Science Center, 2014.. Tamoxifen Citrate purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.
ER [1]
(Cell-free assay)
In vitro

Tamoxifen displays antitumor effect due to its antiestrogenic activity (ER). Values for the apparent affinity of Tamoxifen for the ER range between 30 and 0.01% of that obtained for estradiol, dependent on different ER source (species), protein concentration and condition used for assay. Binding of Tamoxifen to ER further leads to inhibition expression of estrogen-regulated genes, including growth factors and angiogenic factors secreted by the tumor that may stimulate growth by autocrine or paracrine mechanisms. Tamoxifen also directly induces programmed cell death. [1] Tamoxifen produces an inhibitory effect on MCF-7 cell [3H]thymidine incorporation and DNA polymerase activity as well as causing a reduction in DNA content of cultures and cell numbers. This inhibitory effect of Tamoxifen on MCF-7 cell growth can be readily reversed by addition of estradiol to the culture medium. 2 and 6 μM Tamoxifen reduces the proportion of cells in S phase and increases the number of cells in G1. At 10 μM, Tamoxifen causes cell death within 48 hr. [2] Tamoxifen inhibits MCF-7 growth with IC50 of ~10 nM after 10 days treatment. Tamoxifen inhibits plasminogen activator activity of MCF-7, and suppresses estradiol-stimulation of plasminogen activator activity. Tamoxifen also evokes minimal increases in cellular progesterone receptor levels. [3] Tamoxifen is able to inhibit the growth of prostate cancer cell PC3, PC3-M, and DU145 with IC50 ranged from 5.5-10 μM, which is related to its inhibition of protein kinase C and induction of p21(waf1/cip1). [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7 cells NGfocZlEgXSxdH;4bYPDqGG|c3H5 NFi3Xo4yQCCq NHWySoVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFE5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NVAvOiEQvF2= M1nwNlE6QTN{MEK0
human MDA-MB-231 cells MkfhR5l1d3SxeHnjxsBie3OjeR?= M1TiUlE5KGh? NWLZW3ZxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjCxPEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGyMlMh|ryP MXSxPVk{OjB{NB?=
human Ishikawa cells MlTmR5l1d3SxeHnjxsBie3OjeR?= NIHm[3AyQCCq NF:2dFhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBKe2ira3H3ZUBk\WyuczDh[pRmeiBzODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTF{LkWg{txO MV2xPVk{OjB{NB?=
human DU145 cells NUGwcFh4S3m2b4TvfIlkyqCjc4PhfS=> NUjpW3RFOThiaB?= MlrjR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgNVghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xOU4zPSEQvF2= NUPK[3pDOTl7M{KwNlQ>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-AKT / AKT ; 

PubMed: 30759864     

MCF-7 cells were treated with 2 μM tamoxifen and harvested at the indicated time point to analyze the expressions of p-AKT and AKT by western blot.

ER-α66 / ER-α36 / HER2 / EGFR ; 

PubMed: 25203051     

Western blot analysis of the expression levels of ER-α66, ER-α36, HER2 and EGFR in ER-positive breast cancer MCF7 (A), T47D (B) and H3396 (C) cells treated with 1 µM of tamoxifen (TAM) for indicated time period.

p-AMPK / AMPK / p-ACC / ACC / p-P70S6K / p-S6 / p-4EBP1 ; 

PubMed: 27020861     

B. Immunoblot of AMPK pathway activation following treatment with 30μM tamoxifen in MCF7 and C. in MDA-MB-231 cells. 

CD36 / p-ERK / ERK ; 

PubMed: 30573731     

MCF-7 cells MCF-7 cells were treated with tamoxifen (Tam) at the indicated concentrations for 16 h, or with 5 μM Tam for the indicated times. Expression of CD36, p-ERK1/2 and ERK1/2 was determined by western blot.

30759864 25203051 27020861 30573731

PubMed: 30573731     

MCF-7 cells were treated with tamoxifen (Tam) at the indicated concentrations for 16 h. Expression of CD36 was determined by immunofluorescent staining . 

In vivo

Tamoxifen administration to rapidly growing, estradiol-stimulated MCF-7 xenografts results in a dose-dependent retardation or cessation of tumor growth by significantly decreasing tumor cell proliferation in tumor. Tamoxifen treatment results in a slowing of tumor growth (tumor doubling time, 12 days), a significant increase in tumor potential doubling time (Tpot) (6.6 days), and a decrease in labeling index (%LI) (to 8%) by 23 days posttreatment, compared with untreated mice which shows a volume doubling time of 5 days, a Tpot of 2.3 days, and a %LI of 23%. [5] Tamoxifen has not only antiestrogenic but also estrogenic properties depending on the species, tissue, and gene. Tamoxifen displays favorable effects on bone and serum lipid concentrations and stimulation endometrium. [1]


Kinase Assay:


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Competitive binding assays:

Cells are harvested from 150-sq cm T-flasks, and cytosol is prepared at a protein concentration of approximately 2 mg/mL in phosphate buffer. Aliquots of this 180,000 ×g supernatant are then incubated with various concentrations of Tamoxifen and 2.5 nM [3H]estradiol for 16 hr at 0-4 ℃. The free steroids are absorbed by dextran-charcoal [l0 μL of 0.5% Dextran C-5% Norite A in TE buffer] for 1 hr at 0 ℃, and aliquots are counted after centrifugation at 800 ×g, 30 min. The relative binding ability of each competitor is taken as the ratio of the concentration of radioinert estradiol/competitor required to inhibit one-half of the specific [3H]estradiol binding, with the affinity of estradiol set at 100%.
Cell Research:


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  • Cell lines: Human breast cancer cells MCF-7
  • Concentrations: ~1 μM
  • Incubation Time: 10 days
  • Method:

    MCF-7 cells are seeded into T-25 flasks (1.5×105 cells/flask) and grown for 2 days in the MEM supplemented with 10 mM HEPES buffer, gentamicin (50 μg/mL), penicillin (100 units/mL), streptomycin (0.1 mg/mL), bovine insulin (6 ng/mL), hydrocortisone (3.75 ng/mL), and 5% calf serum that has been treated with dextran-coated charcoal for 45 min at 55 ℃ to remove endogenous hormones. The medium is then changed to MEM supplemented as described above, except that it contains 2% charcoal dextran-treated calf serum and various concentrations of Tamoxifen. At the end of incubation, cell numbers are counted.

    (Only for Reference)
Animal Research:


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  • Animal Models: Human breast carcinoma xenografts MCF-7
  • Dosages: 2 cm Tamoxifen capsules
  • Administration: Subcutaneous implantation
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (177.41 mM)
Water Insoluble
Ethanol '''100 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* 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.

Chemical Information

Molecular Weight 563.64


CAS No. 54965-24-1
Storage powder
in solvent
Synonyms ICI 46474 Citrate
Smiles CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

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% DMSO % % Tween 80 % ddH2O

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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

Tech Support

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

  • Question 1:

    I am wondering if the Tamoxifen (product Cat # S1972) is a 4-hydroxy Tamoxifen form or just plain Tamoxifen Citrate?

  • Answer:

    The Tamoxifen (S1972) is a prodrug, just plain Tamoxifen citrate.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID