Tamoxifen (ICI 46474)

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

For research use only.

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.

Tamoxifen (ICI 46474) Chemical Structure

CAS No. 10540-29-1

Selleck's Tamoxifen (ICI 46474) has been cited by 43 publications

Purity & Quality Control

Choose Selective Antineoplastic and Immunosuppressive Antibiotics Inhibitors

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 NW\BelczTnWwY4Tpc44h[XO|YYm= MULJcohq[mm2aX;uJI9nKE2GQT3NRk01OzViYoLlZZN1KGOjbnPldkBk\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9NE4xPSEQvF2= NYTPd|ExRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUS5O|E5QTlpPkG0PVcyQDl7PD;hQi=>
MDA-MB-231 cells MXrGeY5kfGmxbjDhd5NigQ>? MmPKTY5pcWKrdHnvckBw\iCnc4Tyc4dmdiC{ZXPldJRweiCwZXfheIl3\SCPRFGtUWIuOjNzIHLy[YF{fCClYX7j[ZIh[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVAvODhizszN M2SxWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF2OUexPFk6Lz5zNEm3NVg6QTxxYU6=
MCF7 MXPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Ml35O|IhcHK| MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF3DSlch[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygRYN1cX[rdImgQUA1NjZizszNMi=> MkDzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd7MUi4NlAoRjF5OUG4PFIxRC:jPh?=
MCF7 M3vMVGFvfGmnc4Tyc4dmdmmlIHHzd4F6 NGfq[IM6PiCqcoO= NEnlVFhCdnSrZYP0do9o\W6rYzDhZ5Rqfmm2eTDpckBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGS{dXegcIV3\WxiY3H1d4lv\yCrbnjpZol1cW:wIH;mJFExOCCyTTDFNk1mdmijbnPl[EBk\WyuIIDyc4xq\mW{YYTpc44hfG9ibHX2[Ywh\XG3aY\hcIVvfCC2bzC1NEBxVSCHMjDh[pRmeiB7NjDodpMh[nliYXzhcYFzKGKudXWgZZN{[XluIFHjeIl3cXS7IE2gNE4yKM7:TT6= NXXKcoM4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OFM3OjBpPkG5PVQ{PjJyPD;hQi=>
T47D Mom2RY51cWW|dILv[4VvcWNiYYPzZZk> NWrIWJlnQTZiaILz MlLKRY51cWW|dILv[4VvcWNiYXP0bZZqfHliaX6gbJVu[W5iVES3SEBk\WyuczDhd5Nme3OnZDDhd{BlenWpIHzleoVtKGOjdYPpcochcW6qaXLpeIlwdiCxZjCxNFAheE1iRUKt[Y5p[W6lZXSgZ4VtdCCycn;sbYZmemG2aX;uJJRwKGyndnXsJIVyfWm4YXzlcpQhfG9iNUCgdG0hTTJiYX\0[ZIhQTZiaILzJIJ6KGGuYX3hdkBjdHWnIHHzd4F6NCCDY4Tpeol1gSB;IECuNUDPxE1w MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl2M{[yNEc,OTl7NEO2NlA9N2F-
MCF7 Mmf6RY51cWW|dILv[4VvcWNiYYPzZZk> NVPFdJJWQTZiaILz NWPBR3I4SW62aXXzeJJw\2WwaXOgZYN1cX[rdImgbY4hcHWvYX6gUWNHPyClZXzsd{Bie3Onc4Pl[EBieyCmcoXnJIxmfmWuIHPheZNqdmdiaX7obYJqfGmxbjDv[kAyODBicF2gSVIu\W6qYX7j[YQh[2WubDDwdo9tcW[ncnH0bY9vKHSxIHzleoVtKGWzdXn2ZYxmdnRidH:gNVAheE1iRUKgZYZ1\XJiOU[gbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7LDDBZ5Rqfmm2eTC9JFAvOiEQvF2u NWHtcW9mRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5OFM3OjBpPkG5PVQ{PjJyPD;hQi=>
MCF7 NE[wUppCdnSrZYP0do9o\W6rYzDhd5NigQ>? MUi5OkBpenN? NEPiXo1CdnSrZYP0do9o\W6rYzDhZ5Rqfmm2eTDpckBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KGS{dXegcIV3\WxiY3H1d4lv\yCrbnjpZol1cW:wIH;mJFExOCCyTTDFNk1mdmijbnPl[EBk\WyuIIDyc4xq\mW{YYTpc44hfG9ibHX2[Ywh\XG3aY\hcIVvfCC2bzCxJJBOKEV{IHHmeIVzKDl4IHjyd{BjgSCjbHHtZZIh[my3ZTDhd5NigSxiQXP0bZZqfHliPTCwMlQh|ryPLh?= NG\YeWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm0N|YzOCd-MUm5OFM3OjB:L3G+
T47D Ml;MRY51cWW|dILv[4VvcWNiYYPzZZk> NHvBUYo6PiCqcoO= NUDtNVNLSW62aXXzeJJw\2WwaXOgZYN1cX[rdImgbY4hcHWvYX6gWFQ4TCClZXzsd{Bie3Onc4Pl[EBieyCmcoXnJIxmfmWuIHPheZNqdmdiaX7obYJqfGmxbjDv[kAyODBicF2gSVIu\W6qYX7j[YQh[2WubDDwdo9tcW[ncnH0bY9vKHSxIHzleoVtKGWzdXn2ZYxmdnRidH:gNVAheE1iRUKgZYZ1\XJiOU[gbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7LDDBZ5Rqfmm2eTC9JFAvPyEQvF2u NH22cYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm0N|YzOCd-MUm5OFM3OjB:L3G+
T47D MlnnRY51cWW|dILv[4VvcWNiYYPzZZk> M1TlSlk3KGi{cx?= NIH3dZpCdnSrZYP0do9o\W6rYzDhZ5Rqfmm2eTDpckBpfW2jbjDUOFdFKGOnbHzzJIF{e2W|c3XkJIF{KGS{dXegcIV3\WxiY3H1d4lv\yCrbnjpZol1cW:wIH;mJFExOCCyTTDFNk1mdmijbnPl[EBk\WyuIIDyc4xq\mW{YYTpc44hfG9ibHX2[Ywh\XG3aY\hcIVvfCC2bzCxJJBOKEV{IHHmeIVzKDl4IHjyd{BjgSCjbHHtZZIh[my3ZTDhd5NigSxiQXP0bZZqfHliPTC5JO69VS5? NInNVYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm0N|YzOCd-MUm5OFM3OjB:L3G+
HepG2 NITPVZVEgXSxdH;4bYNqfHliYYPzZZk> NHzsVXIzPCCqcoO= NGHrfmJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjZoTldkAzPCCqcoOgZpkhemW|YYr1dolvKGS7ZT3iZZNm\CCobIXvdoV{[2WwY3WgZY5idHm|aYOsJGNEPTBiPTCyOE44KM7:TT6= NYLsU3hFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzNlI4PTRpPkOwN|IzPzV2PD;hQi=>
HEK293 NXPRc5ZES3m2b4TvfIlkcXS7IHHzd4F6 MlvCNlQhcHK| NIHHO4lEgXSxdH;4bYNqfHliYXfhbY5{fCCKRVuyPVMh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IILld4F7fXKrbjDkfYUu[mG|ZXSg[ox2d3Knc3PlcoNmKGGwYXz5d4l{NCCFQ{WwJF0hOzlwNDFOwG0v MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN{Mke1OEc,OzB|MkK3OVQ9N2F-
MCF-7 NF7hTpVEgXSxdH;4bYNqfHliYYPzZZk> M3nxN2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KE2FRj23JINmdGy|IHnuJJRp\SCjYoPlcoNmKG:oIEGgeW0hTTJiKHXzeJJi\GmxbDmsJGN6fG:2b4jpZ4l1gSB;IEmuPEDPxE1w MmHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTB6OUOzNkc,QTB6OUOzNlww[T5?
MCF-7 MVPDfZRwfG:6aXPpeJkh[XO|YYm= NXvsRXQ4S3m2b4TvfIlkcXS7IHHnZYlve3RiTVPGMVch[2WubIOgbY4heHKnc3XuZ4Uhd2ZiMTD1UUBGOiBqZYP0doFlcW:uKTygR5l1d3SxeHnjbZR6KD1iMUOg{txONg>? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86ODh7M{OyK|46ODh7M{OyQE9iRg>?
MCF-7 M4iy[mZ2dmO2aX;uJIF{e2G7 NUGxVJFxTW[oZXP0bZZmKGSxc3Wg[o9zKFt|SG2tJIV{fHKjZHnvcEBi\2GrboP0JJBzd2yrZnXyZZRqd25ib3[gUWNHNTdiY3XscJMtKEWFNUCgQUAxNjByMEGxJO69VS5? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzZ7NkixK|4zPzZ7NkixQE9iRg>?
Ishikawa MYXGeY5kfGmxbjDhd5NigQ>? NFjZdoxEd26lZX70doF1cW:wIH;mJINwdXCxdX7kJJJmeXWrcnXkJJRwKGmwZIXj[UA2OCBnIH;mJJRp\SCvYYjpcZVuKHO2aX31cIF1cW:wIH;mJIFtc2GuaX7lJJBpd3OyaHH0ZZNmKGGldHn2bZR6KGmwIFnzbIls[XejIHPlcIx{NCCHQ{WwJF0hOC5yM{Og{txONg>? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek85OjBzNUi3K|45OjBzNUi3QE9iRg>?
MCF-7 NVHJeWR1TnWwY4Tpc44h[XO|YYm= M4jZNGVn\mWldHn2[UBkd26lZX70doF1cW:wIHHnZYlve3RiTVPGMVch[nKnYYP0JJR2dW:{IHPlcIx{KHW|aX7nJG1ETi15IHHzd4F6NixiRVO1NEA:KDBwMEGg{txONg>? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjh{NUmzOUc,OTJ6MkW5N|U9N2F-
ScN2a-cl3 M2jmSWZ2dmO2aX;uJIF{e2G7 NHT2b|g2KGSjeYO= NHjKWVdKdmirYnn0bY9vKG:oIGLNUEBxemmxbjDwdo91\WmwIHnu[oVkfGWmIHnuJI1wfXOnIHTpeollcW6pIGPjUlJiNWOuMzDj[YxteyCneIDy[ZN{cW6pIH\1cIwhdGWwZ4ToJI1wfXOnIGDyVEBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gVJJRe2NibHX2[Ywh[W[2ZYKgOUBl[Xm|IHL5JGVNUVODLDDFR|UxKD1iND6zPUDPxE1w MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF6M{W4PUc,OjRzOEO1PFk9N2F-
NCI-H460 NUnVPZBmSW62aXPhcoNmeiCjc4PhfS=> NHfPZXUzPCCqcoO= M1jyfWFvfGmlYX7j[ZIh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCjZoTldkAzPCCqcoOgZpkhW1KEIHHzd4F6NCCJSUWwJF0hPC52ODFOwG0v NGiwPWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUezN|A5PSd-MUm3N|MxQDV:L3G+
DU145 NHjvc3pCdnSrY3HuZ4VzKGG|c3H5 M2rabFI1KGi{cx?= NYrCeWF6SW62aXPhcoNmeiCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGGodHXyJFI1KGi{czDifUBUWkJiYYPzZZktKEeLNUCgQUA3NjB5IN88UU4> NGjZU3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUezN|A5PSd-MUm3N|MxQDV:L3G+
SKOV3 NWftd4FwSW62aXPhcoNmeiCjc4PhfS=> NX3He49mOjRiaILz MUjBcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vPWlMh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IGPSRkBie3OjeTygS2k2OCB;IE[uOEDPxE1w MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd|M{C4OUc,OTl5M{OwPFU9N2F-
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insect cells NWjDZ3NSTnWwY4Tpc44h[XO|YYm= MkHVNE4yKHSxIEGwNFAxKHWP M4XkSmJqdmSrbnegZYZncW6rdImgeI8hfW62YXfn[YQhcHWvYX6gdoVkd22kaX7hcpQh\nWubDDs[Y5ofGhiRWLhcJBp[SCneIDy[ZN{\WRiaX6gbY5{\WO2IHPlcIx{KDBwMTD0c{AyODByMDD1UUBjgSCIbIXvdo1wdmViRWOyJGdz\WWwIHTpd5Bt[WOnbXXueEBj[XOnZDDhd5NigQ>? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB7MUmyNEc,OzByOUG5NlA9N2F-
Assay
Methods Test Index PMID
Western blot p-AKT / AKT ; ER-α66 / ER-α36 / HER2 / EGFR ; p-AMPK / AMPK / p-ACC / ACC / p-P70S6K / p-S6 / p-4EBP1 ; CD36 / p-ERK / ERK 30759864 25203051 27020861 30573731
Immunofluorescence CD36 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 (from reference)

Cell Research:

[2]

  • 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.

Animal Research:

[4]

  • Animal Models: Pdx1PB-CreERTm mice
  • Dosages: --
  • Administration: s.c.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 371.51
Formula

C26H29NO

CAS No. 10540-29-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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 μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05156892 Not yet recruiting Drug: SUBA-itraconazole|Drug: Tamoxifen Ovarian Cancer Anthony Joshua FRACP|Royal Prince Alfred Hospital Sydney Australia|Concord Hospital|Prince of Wales Hospital Sydney|St Vincent''s Hospital Sydney February 1 2022 Phase 1
NCT05133674 Not yet recruiting Drug: Tamoxifen 20 mg Breast Cancer|Breast Carcinoma|Breast Tumors|Cancer of Breast|Malignant Neoplasm of Breast Karolinska University Hospital January 10 2022 Phase 2
NCT04200066 Not yet recruiting Drug: Temozolomide Tamoxifen Maprotiline Glioblastoma|Brain Tumor University of Rochester December 1 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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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