Tamoxifen Citrate

Name: Tamoxifen Citrate
Brand: Selleck Chemicals
SKU: S1972
Rating: 5 (2 reviews)

For research use only. Not for use in humans.

Catalog No.S1972 Synonyms: ICI 46474 Citrate

2 publications

Molecular Weight(MW): 563.64

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

Selleck's Tamoxifen Citrate has been cited by 2 publications

Cell Chem Biol, 2019, 26(3):420-432

PubMed: 30686757 ( click the link to review the publication )

University of North Texas, 2014, Timothy E. Richardson

PubMed: ( click the link to review the publication )

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.

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

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	Incubation Time	Activity Description	PMID
human MCF7 cells	NEfpe4VEgXSxdH;4bYPDqGG\|c3H5	NXjpOI5NOThiaB?=	NWfsNphtS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkAyQCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVExNjJizszN	MX2xPVk{OjB{NB?=
human MDA-MB-231 cells	MX3DfZRwfG:6aXRCpIF{e2G7	NXO3XJQ{OThiaB?=	NULrfol7S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjCxPEBpenNiYomgUXRVKGG\|c3H5MEBKSzVyPUGyMlMh\|ryP	MVixPVk{OjB{NB?=
human Ishikawa cells	M4DNWmN6fG:2b4jpZ:Kh[XO\|YYm=	NYjaOJJKOThiaB?=	MmSyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTZNpcWujd3GgZ4VtdHNiYX\0[ZIhOThiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yOi53IN88US=>	NVzqO2dnOTl7M{KwNlQ>
human DU145 cells	M1LL[mN6fG:2b4jpZ:Kh[XO\|YYm=	NGHKSFIyQCCq	MlfLR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgNVghcHK\|IHL5JG1VXCCjc4PhfUwhUUN3ME2xOU4zPSEQvF2=	NVX6PVdnOTl7M{KwNlQ>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-AKT / AKT ; PubMed: 30759864 Cancers (Basel) 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 PLoS One 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 Cancer Res 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 Oncogenesis 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
Immunofluorescence	CD36; PubMed: 30573731 Oncogenesis MCF-7 cells were treated with tamoxifen (Tam) at the indicated concentrations for 16 h. Expression of CD36 was determined by immunofluorescent staining .	30573731

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

References

- Collapse

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(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 Download Tamoxifen Citrate SDF

Molecular Weight	563.64
Formula	C₂₆H₂₉NO.C₆H₈O₇
CAS No.	54965-24-1
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	ICI 46474 Citrate
Smiles	CC/C(C1=CC=CC=C1)=C(C2=CC=CC=C2)/C3=CC=C(OCCN(C)C)C=C3.OC(=O)CC(O)(CC(O)=O)C(O)=O

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03582865	Not yet recruiting	Drug: Tamoxifen 20 mg	Breast Cancer	Assiut University	September 1 2019	--
NCT02801786	Not yet recruiting	Drug: Placebo\|Drug: Lidocaine\|Drug: Tamoxifen	Pain\|Discomfort	Universidade Federal de Goias	November 2018	Phase 2\|Phase 3
NCT03707340	Recruiting	Drug: Flibanserin Pill	Breast Cancer\|Hyposexual Desire Disorder	Memorial Sloan Kettering Cancer Center	September 14 2018	--

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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Tamoxifen Citrate