Tamoxifen Citrate

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

For research use only.

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	M4X6NGN6fG:2b4jpZ:Kh[XO\|YYm=	MXSxPEBp	MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEG4JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTB;MUCuNkDPxE1?	NEPrZ2kyQTl\|MkCyOC=>
human MDA-MB-231 cells	M1zzSWN6fG:2b4jpZ:Kh[XO\|YYm=	NWDzbVc1OThiaB?=	MoHoR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiBzODDodpMh[nliTWTUJIF{e2G7LDDJR\|UxRTF{LkOg{txO	M3j0SFE6QTN{MEK0
human Ishikawa cells	NGDTOlNEgXSxdH;4bYPDqGG\|c3H5	MW[xPEBp	MlHwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTZNpcWujd3GgZ4VtdHNiYX\0[ZIhOThiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yOi53IN88US=>	M1vXXlE6QTN{MEK0
human DU145 cells	NGm5Z29EgXSxdH;4bYPDqGG\|c3H5	NH3wclIyQCCq	NVTVWHVwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiYX\0[ZIhOThiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yPS5{NTFOwG0>	MUixPVk{OjB{NB?=

... 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 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 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

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

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

Calculate Reset

Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：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.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-05-15)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04174352	Suspended	Drug: Tamoxifen\|Diagnostic Test: FES PET/CT	ERα+ Breast Cancer\|ESR1 Gene Mutation	University of Wisconsin Madison	June 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
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

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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.

Estrogen/progestogen Receptor Signaling Pathway Map

Estrogen/progestogen Receptor Inhibitors with Unique Features

Selective AR agonist

Andarine : Selective non-steroidal AR agonist, K_i=4 nM.
Most Potent AR Antagonist

ARN-509 : Androgen receptor, IC50=16 nM.
FDA-approved AR Antagonist

Bicalutamide : Approved by FDA for prostate cancer.
Newest AR Antagonist

AZD3514 : Potent and oral androgen receptor downregulator with K_i of 2.2 μM.

Related Estrogen/progestogen Receptor Products

Licochalcone A ^New

Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.
Endoxifen HCl ^New

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Sacubitril/valsartan (LCZ696) ^New

Sacubitril/valsartan (LCZ696), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.
Fulvestrant

Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.
Mifepristone

Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively.

Features:Mifepristone is the first approved medication for patients with endogenous cushing's syndrome.
Raloxifene HCl

Raloxifene is an estrogen antagonist, which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.

Features:Raloxifene is as effective as tamoxifen in reducing the incidence of breast cancer in postmenopausal women at increased risk.
Estradiol

Estradiol, or more precisely, 17β-estradiol, is a human sex hormone and steroid, and the primary female sex hormone.
Toremifene Citrate

Toremifene Citrate is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.
Progesterone

Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.
Bazedoxifene HCl

Bazedoxifene HCl is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively.

Choose Your Country or Region

By Signaling Pathways

By product type

Tamoxifen Citrate