Tamoxifen (ICI 46474)

For research use only.

Catalog No.S1238 Synonyms: (Z)-Tamoxifen, trans-Tamoxifen

37 publications

Tamoxifen (ICI 46474) Chemical Structure

CAS No. 10540-29-1

Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.

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Selleck's Tamoxifen (ICI 46474) has been cited by 37 publications

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Biological Activity

Description Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.
Targets
estrogen receptor [1]
In vitro

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[2]. 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)[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-435 cells NGPmXFFHfW6ldHnvckBie3OjeR?= NEjvXJVKdmirYnn0bY9vKG:oIF3ERU1OSi12M{WgZpJm[XO2IHPhcoNmeiClZXzsJJBzd2yrZnXyZZRqd25uIFnDOVA:OC5yNTFOwG0> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPDl5MUi5PUc,OTR7N{G4PVk9N2F-
MDA-MB-231 cells NVLLcI9NTnWwY4Tpc44h[XO|YYm= NXzJNHo6UW6qaXLpeIlwdiCxZjDld5Rzd2enbjDy[YNmeHSxcjDu[YdifGm4ZTDNSGEuVUJvMkOxJIJz\WG|dDDjZY5k\XJiY3XscEBxem:uaX\ldoF1cW:wLDDJR|UxRTBwMEig{txO NUPCVHF3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUS5O|E5QTlpPkG0PVcyQDl7PD;hQi=>
MCF7 NIXSR3BCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MYO3NkBpenN? NUG5WHF[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBOS0Z5IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEGldHn2bZR6KD1iND62JO69VS5? NVnHeodvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe5NVg5OjBpPkG3PVE5QDJyPD;hQi=>
MCF7 NVnqWm1CSW62aXXzeJJw\2WwaXOgZZN{[Xl? M33nWlk3KGi{cx?= M17Nc2FvfGmnc4Tyc4dmdmmlIHHjeIl3cXS7IHnuJIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh\HK3ZzDs[ZZmdCClYYXzbY5oKGmwaHnibZRqd25ib3[gNVAxKHCPIFWyMYVvcGGwY3XkJINmdGxicILvcIln\XKjdHnvckB1dyCuZY\lcEBmeXWrdnHs[Y51KHSxIEWwJJBOKEV{IHHmeIVzKDl4IHjyd{BjgSCjbHHtZZIh[my3ZTDhd5NigSxiQXP0bZZqfHliPTCwMlEh|ryPLh?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2M{[yNEc,OTl7NEO2NlA9N2F-
T47D Mn;QRY51cWW|dILv[4VvcWNiYYPzZZk> NHzwUmQ6PiCqcoO= MnvFRY51cWW|dILv[4VvcWNiYXP0bZZqfHliaX6gbJVu[W5iVES3SEBk\WyuczDhd5Nme3OnZDDhd{BlenWpIHzleoVtKGOjdYPpcochcW6qaXLpeIlwdiCxZjCxNFAheE1iRUKt[Y5p[W6lZXSgZ4VtdCCycn;sbYZmemG2aX;uJJRwKGyndnXsJIVyfWm4YXzlcpQhfG9iNUCgdG0hTTJiYX\0[ZIhQTZiaILzJIJ6KGGuYX3hdkBjdHWnIHHzd4F6NCCDY4Tpeol1gSB;IECuNUDPxE1w MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2M{[yNEc,OTl7NEO2NlA9N2F-
MCF7 Ml\qRY51cWW|dILv[4VvcWNiYYPzZZk> MlnUPVYhcHK| NG\oVlFCdnSrZYP0do9o\W6rYzDhZ5Rqfmm2eTDpckBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGS{dXegcIV3\WxiY3H1d4lv\yCrbnjpZol1cW:wIH;mJFExOCCyTTDFNk1mdmijbnPl[EBk\WyuIIDyc4xq\mW{YYTpc44hfG9ibHX2[Ywh\XG3aY\hcIVvfCC2bzCxNEBxVSCHMjDh[pRmeiB7NjDodpMh[nliYXzhcYFzKGKudXWgZZN{[XluIFHjeIl3cXS7IE2gNE4zKM7:TT6= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2M{[yNEc,OTl7NEO2NlA9N2F-
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HepG2 MnzIR5l1d3SxeHnjbZR6KGG|c3H5 NGe2[GgzPCCqcoO= NXPpOlU2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KHKnc3H6eZJqdiCmeXWtZoF{\WRiZnz1c5Jme2OnbnPlJIFv[Wy7c3nzMEBESzVyIE2gNlQvPyEQvF2u NUTqWoxTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzNlI4PTRpPkOwN|IzPzV2PD;hQi=>
HEK293 MoHrR5l1d3SxeHnjbZR6KGG|c3H5 Mk\lNlQhcHK| NVzmO5dzS3m2b4TvfIlkcXS7IHHnZYlve3RiSFXLNlk{KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDy[ZNignW{aX6g[JlmNWKjc3XkJIZtfW:{ZYPj[Y5k\SCjbnHsfZNqeyxiQ1O1NEA:KDN7LkSg{txONg>? NXv0fo1HRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzNlI4PTRpPkOwN|IzPzV2PD;hQi=>
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Ishikawa Ml\xSpVv[3Srb36gZZN{[Xl? NWC1V5BuS2:wY3XueJJifGmxbjDv[kBkd22yb4Xu[EBz\XG3aYLl[EB1dyCrbnT1Z4UhPTBiJTDv[kB1cGVibXH4bY12dSC|dHnteYxifGmxbjDv[kBidGujbHnu[UBxcG:|cHjheIF{\SCjY4Tpeol1gSCrbjDJd4hqc2G5YTDj[YxteyxiRVO1NEA:KDBwMEOzJO69VS5? Mn7nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQDJyMUW4O{c,QDJyMUW4O|ww[T5?
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NCI-H460 NULoTlZRSW62aXPhcoNmeiCjc4PhfS=> NEPaRY0zPCCqcoO= M1fScWFvfGmlYX7j[ZIh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCjZoTldkAzPCCqcoOgZpkhW1KEIHHzd4F6NCCJSUWwJF0hPC52ODFOwG0v MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd|M{C4OUc,OTl5M{OwPFU9N2F-
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MCF7 M1f6OmZ2dmO2aX;uJIF{e2G7 MmfQOlAhdWdxa3e= NUPmcHdWPSCmYYnzJJBmeiC5ZXXrJIZweiB2ODDkZZl{ MWLEc5dvemWpdXzheIlwdiCxZjDwdo9o\XO2ZYLvcoUhemWlZYD0c5IhdVKQQTDs[ZZmdCCrbjDOU2QhW0OLRDDnZY1u[SCvb4Xz[UB5\W6xZ4Lh[pRm\CC5aYToJIh2dWGwIF3DSlch[2WubIOgZZQhPjBibXevb4ctKHCxIEWg[IF6eyCyZYKge4VmcyCob4KgOFgh\GG7czDwc5N1KHS3bX;yJIlueGyjboTheIlwdiCvZXHzeZJm\CB5IHjyd{Bxd3O2IHzhd5Qh\G:|ZTDifUBTXC2SQ2KgcYV1cG:m NGP4SlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW2Nlc{Pyd-Mkm1OlI4Ozd:L3G+
MCF7 NVj0d3RXSW62aYT1cY9zKGG|c3H5 NIexRos3OCCvZz;r[y=> NFSwT3M1KHenZXvz MoLVRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczD4[Y5w\3KjZoTl[EBqdiCwdT;ueUBud3W|ZTDtc4RmdCCxZjD0ZY1wgGmoZX6td4Vve2m2aY\lJIJz\WG|dDDjZY5k\XJieHXuc4dz[W[2IHntdIxidnSnZDD3bZRpKDF5YnX0ZU1me3S{YXTpc4whfGmvZTDy[Yxm[XOnIIDlcIxmfHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJJR2dW:{II\vcJVu\SCjdDC2NEBu\y:tZzygdI8heWRiZn;yJFQhf2Wna4O= NWT0bVlQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwPFY3OjZpPkOwNFg3PjJ4PD;hQi=>
insect cells M3zPZmZ2dmO2aX;uJIF{e2G7 NGnDbZExNjFidH:gNVAxODBidV2= NX7oXZZCSmmwZHnu[{Bi\m[rbnn0fUB1dyC3boTh[4dm\CCqdX3hckBz\WOxbXLpcoFvfCCodXzsJIxmdme2aDDFVoFteGijIHX4dJJme3OnZDDpckBqdnOnY4SgZ4VtdHNiMD6xJJRwKDFyMECwJJVOKGK7IF\seY9zdW:wZTDFV|IhT3KnZX6g[Il{eGyjY3Xt[Y51KGKjc3XkJIF{e2G7 M{TsN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEmxPVIxLz5|MEC5NVkzODxxYU6=

... Click to View More Cell Line Experimental Data

Assay
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
Immunofluorescence
CD36; 

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. 

30573731
In vivo

Tamoxifen (TAM) is widely used for both treatment and prevention of breast cancer. However, it is also carcinogenic in human uterus and rat liver[2]. 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[4].

Protocol

Cell Research:

[2]

- Collapse
  • Cell lines: MCF7 and T47D
  • Concentrations: 10-6 mol/L
  • Incubation Time: 24, 48, and 96 h
  • Method:

    48 h before the addition of E2 and TAM, cells were washed with 5 mL phosphate-buffered saline (PBS) and then switched to phenol red-free RPMI-1640 containing 10% charcoal-stripped FBS. E2 and TAM were dissolved in absolute ethanol and diluted in the media at 10-8 mol/L and 10-6 mol/L, respectively, and then added to the culture medium at 24, 48, and 96 h.


    (Only for Reference)
Animal Research:

[4]

- Collapse
  • Animal Models: Pdx1PB-CreERTm mice
  • Dosages: --
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (199.18 mM)
Water Insoluble
Ethanol '''74 mg/mL
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.
1mg/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 371.51
Formula

C26H29NO

CAS No. 10540-29-1
Storage powder
in solvent
Synonyms (Z)-Tamoxifen, trans-Tamoxifen
Smiles CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3

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
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Bio Calculators

Molarity Calculator

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)

  • Mass
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*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

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 )

  • C1
    V1
    C2
    V2

* 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

  • 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):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

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

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04200066 Not yet recruiting Drug: Temozolomide Tamoxifen Maprotiline Glioblastoma|Brain Tumor University of Rochester May 1 2021 Phase 1
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
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.

Handling Instructions

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

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Frequently Asked Questions

  • Question 1:

    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?

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID