Tamoxifen Citrate

Catalog No.S1972 Synonyms: ICI 46474 Citrate

Tamoxifen Citrate Chemical Structure

Molecular Weight(MW): 563.64

Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding.

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In DMSO USD 130 In stock
USD 97 In stock
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1 Customer Review

  • 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.

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Biological Activity

Description Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding.
Targets
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 NGPjOXZEgXSxdH;4bYPDqGG|c3H5 M4XEcFE5KGh? MY\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEG4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUCuNkDPxE1? NH7IZ|EyQTl|MkCyOC=>
human MDA-MB-231 cells NUn6PGpIS3m2b4TvfIlkyqCjc4PhfS=> MXqxPEBp NILHblJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIFnfGW{IEG4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUKuN{DPxE1? M{PmRlE6QTN{MEK0
human Ishikawa cells Mo\JR5l1d3SxeHnjxsBie3OjeR?= NI\BTFEyQCCq MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDJd4hqc2G5YTDj[YxteyCjZoTldkAyQCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEzNjVizszN M3\qUVE6QTN{MEK0
human DU145 cells NVXCS|NzS3m2b4TvfIlkyqCjc4PhfS=> NWfofXI{OThiaB?= MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bi\nSncjCxPEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUG1MlI2KM7:TR?= MnroNVk6OzJyMkS=

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:

[3]

+ Expand

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:

[3]

+ Expand
  • 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:

[5]

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

Solubility (25°C)

In vitro DMSO 100 mg/mL (177.41 mM)
Ethanol 100 mg/mL (177.41 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
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
Formula

C26H29NO.C6H8O7

CAS No. 54965-24-1
Storage powder
Synonyms ICI 46474 Citrate

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00026585 Completed Bipolar Disorder National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC) November 9, 2001 Phase 2
NCT03024580 Not yet recruiting Breast Neoplasm Instituto Nacional de Cancer, Brazil|Cancer Research UK Cambridge Institute March 2017 Phase 2
NCT02993159 Not yet recruiting Ductal Breast Carcinoma In Situ|Estrogen Receptor Positive National Cancer Institute (NCI) March 2017 Phase 2
NCT02988986 Not yet recruiting Estrogen Receptor Positive Breast Cancer Jenny C. Chang, MD|Millennium Pharmaceuticals, Inc.|The Methodist Hospital System February 2017 Phase 2
NCT02903121 Not yet recruiting Bleeding|Implants|Breakthrough Bleeding Oregon Health and Science University|Merck Womens Health Investigator Initiated Studies Program January 2017 Phase 2
NCT02690870 Not yet recruiting Infertility Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University|Sun Yat-sen University January 2017 Phase 4

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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