4-Hydroxytamoxifen

Catalog No.S7827 Synonyms: Afimoxifene

4-Hydroxytamoxifen Chemical Structure

Molecular Weight(MW): 387.51

4-Hydroxytamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.

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Cited by 3 Publications

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  • CDK4/6 inhibitor resistance promotes diminished ER expression and activity. (a and b) Proliferation of MCF-7 and MR cells in the presence of different concentrations of ICI (a) or 4-hydroxytamoxifen (4-OHT) (b) was measured by the alamarBlue assay and plotted as % inhibition of proliferation against log concentration of inhibitor. Each data point represents the average value±s.d. of six replicates obtained in three independent experiments.

    Oncogene, 2016, 36(16):2255-2264. 4-Hydroxytamoxifen purchased from Selleck.

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Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description 4-Hydroxytamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. It activates on-target modification frequency for intein-Cas9 variants.
In vitro

4-OHT is a potent activator of ER and has been shown to have a higher affinity for estrogen receptors compared to tamoxifen. It has significant dose and time-dependent direct effects to alter the contractile function of isolated adult rat cardiac myocytes[1]. 4-HT activates on-target modification frequency for intein-Cas9 variants [3].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells NWKy[2xqWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWLJcohq[mm2aX;uJI9nKGW|dILv[4VvNXO2aX31cIF1\WRiTVPGMVch[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVAvPSCwTR?= NHfOcGE6PTR6OEG3
MCF7 cells MnPjSpVv[3Srb36gZZN{[Xl? MXrJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCPQ1[tO{BjemWjc4SgeJVud3JiY3XscJMhfXOrbnegUWNHNTdiYYPzZZktKEmFNUC9PE42KG6P Mn;4NVI5OjV7M{W=
MCF7 cells MWXQdo9tcW[ncnH0bY9vKGG|c3H5 MWC3NkBp NWjMXGRESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBme3S{b3flckBz\WOncITvdkBl\XCnbnTlcpQhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNVA4KM7:TR?= NF;IR28yQDh|NUG3Oi=>
MCF7 cells MnjoVJJwdGmoZYLheIlwdiCjc4PhfS=> NYDHXo0xOjRiaB?= MkX1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCPVGOgZZN{[XluIFnDOVA:QC53IH7N MXuxPFI4OjJ3Nh?=
T47D:C:4:2 cells Mo\QSpVv[3Srb36gZZN{[Xl? NGXG[HRGe3S{b3flcolkKGGldHn2bZR6KGG2IIfpcIQhfHmyZTDFVkBidHCqYTDlfJBz\XO|ZXSgbY4hXDR5RErDPlQ7OiClZXzsd{Bkd2W6cILld5NqdmdiZYP0do9o\W5icnXzdI9ve2ViZXzlcYVvfCCkeTDkeYVtKGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= NWXZbo1bOjB|M{SzOlg>
MDA-MB-231 cells MYDGeY5kfGmxbjDhd5NigQ>? M4fHPFMh\GG7cx?= NUCxZm1ZS3m2b4P0ZZRq[yCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IH3pZ5JwfGm2ZYKgZZN{[Xl? NUW2c2x1OjB3OUi1OVU>
PC3 cells NWXtc|F6WHKxbHnm[ZJifGmxbjDhd5NigQ>? NHjpV|k1QCCq NFruNW1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIFv\HKxZ3XuJJJm[2WydH;yMYRm\mmlaXXueEBpfW2jbjDQR|Mh[2WubIOgbY5kfWKjdHXkJJdqfGhiMD62JI5OKG:oIHXzeJJi\GmxbDDhcoQhOC55IH7NJI9nKHSnc4Tvd5Rmem:wZTDh[pRmeiB2ODDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhT0l3ME23MlU5PTd6IN88US=> NWTURWZvOjF3MUOyO|U>
DU145 cells NWjqNIFUWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYTqWWxwPDhiaB?= MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHHu[JJw\2WwIILlZ4VxfG:{LXTl[olkcWWwdDDoeY1idiCGVUG0OUBk\WyuczDpcoN2[mG2ZXSge4l1cCByLk[gcm0hd2ZiZYP0doFlcW:uIHHu[EAxNjdibl2gc4YhfGW|dH;zeIVzd26nIHHmeIVzKDR6IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBIUTVyPUGwMlcyPTJizszN NX20PIdpOjF3MUOyO|U>
LNCAP cells MnrZVJJwdGmoZYLheIlwdiCjc4PhfS=> MUS0PEBp M2q5[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOg[ZhxemW|c3nu[{BidmS{b3flckBz\WOncITvdkBqdmO3YnH0[YQhf2m2aDCwMlYhdk1ib3[g[ZN1emGmaX;sJIFv\CByLkegcm0hd2ZidHXzeI9{fGW{b37lJIFnfGW{IES4JIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCJSUWwQVgvOzF5NkSg{txO MXGyNVUyOzJ5NR?=
T47D cells NX;kdHJ2S3m2b4TvfIlkcXS7IHHzd4F6 NX\WR5c1PSCmYYnz NH3SblJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVPDeGIHPlcIx{KGGodHXyJFUh\GG7czygTWM2OD1yLkKxJO69VQ>? M2Th[lI{QDZ2OUK4
MDA-MB-231 cells NYP4SpFsWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXKyOEBp M1W3fWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVExNjRizszN NEDlXo0zPDF6OUC1OS=>
MCF7 cells Mny1SpVv[3Srb36gZZN{[Xl? MWixNEDPxE1? MlzpOkBp NGf0O|FWeHKnZ4XsZZRqd25ib3[gSXJidHCqYTDwdo91\WmwIHzleoVteyCrbjDoeY1idiCPQ1[3JINmdGy|IHH0JFExKHWPIHHmeIVzKDZiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? M2Lk[VI1OzN{NkOw
SKOV3 cells Mkj1SpVv[3Srb36gZZN{[Xl? M17TOlQ5KGh? NFf6WWFCdnSrY3HuZ4VzKGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMhd3[ncnX4dJJme3OrbnegVE1oeCCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVcvPDZizszN NUW5bI5tOjR7NE[xOFU>
MDA-MB-231 cells M{PTR2Z2dmO2aX;uJIF{e2G7 MUW0PEBp NHi1VnNCdnSrY3HuZ4VzKGGpYXnud5QhcHWvYX6gSXIueG:|aYTpeoUhVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUWuOEDPxE1? M2q4V|I1QTR4MUS1
MCF7 cells NWLIN|ViTnWwY4Tpc44h[XO|YYm= NETZN|c1QCCq NXPUR4plSW62aXPhcoNmeiCjZ3HpcpN1KGi3bXHuJGVTNXCxc3n0bZZmKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF06NjJizszN NWrxfXN2OjR7NE[xOFU>
MDA-MB-231 cells MnzySpVv[3Srb36gZZN{[Xl? NV7YOXV6PDhiaB?= MYXBcpRq[2GwY3XyJIFo[Wmwc4SgbJVu[W5iRWKtcoVo[XSrdnWgUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuII\pZYJqdGm2eTDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDJR|UxRTZwMjFOwG0> MUKyOFk1PjF2NR?=
MCF7 cells MkjKSpVv[3Srb36gZZN{[Xl? NEfKVWkzPTBidH:gOVAxKG6P MlnwOUBl[Xm| Ml7rRY51cWOjbnPldkBi\2GrboP0JIh2dWGwIFXSMZBwe2m2aY\lJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBme3S{YXTpc4wucW6mdXPl[EBk\WyuIIDyc4xq\mW{YYTpc44h[XRiMkWwJJRwKDVyMDDuUUBi\nSncjC1JIRigXN? M1nOVlI1QTR4MUS1
MCF7 cells NWrM[JFWS3m2b4TvfIlkcXS7IHHzd4F6 M3vtOVQ5KGh? MlrYR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGzMlYh|ryP Mk\FNlU3OTh3OUW=
DU145 cells NH;mPGRRem:uaX\ldoF1cW:wIHHzd4F6 MlTmO|IhcA>? MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKESXMUS1JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xOU4{KM7:TR?= MnnoNlU6QTN{Nkm=
african green monkey Vero cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 NELUeFU4OiCq M3nXVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgZYZzcWOjbjDndoVmdiCvb37r[ZkhXmW{bzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUWuNUDPxE1? NHL1V3QzPTl7M{K2PS=>
BT-20 cells M{jiPXBzd2yrZnXyZZRqd25iYYPzZZk> NGi2R4FKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QheHKxbHnm[ZJifGmxbjDv[kBDXC1{MDDj[YxteyCrbjDwdoV{\W6lZTDv[kBVWEViYYSgNVBmNTViTTDjc45k\W62cnH0bY9v M1\RPFI4Pjl4OEG=
Ishikawa endometrial cells M1LuWGZ2dmO2aX;uJIF{e2G7 MmGwRY51[WexbnnzeEBi[3Srdnn0fUBieyCrbnjpZol1cW:wIH;mJFEhdk1iMUetZoV1[S2nc4TyZYRqd2xic4TpcZVt[XSnZDDhcItidGmwZTDwbI9{eGijdHHz[UBqdmS3Y4Tpc44hcW5iSYPobYtif2FiZX7kc41mfHKrYXygZ4VtdHNuIFnDOVA:OC53MTFOwG0> M4DZXVE2OzhyMkC4
MCF-7-2a cells M1rxeWZ2dmO2aX;uJIF{e2G7 MoPKTY5pcWKrdHnvckBw\iCnc4TyZYRqd2xiaX7keYNm\CCnc4Tyc4dmdiC{ZXPldJRweiC2cnHud4NzcXC2aX;uZYwh[WO2aY\heIlwdiCrbjDNR2YuPy1{YTDj[YxteyxiSVO1NF0xNjByNzFOwG0> MkmzNVI3PzJ{NEm=
Calu-1 cells NUPnTYk6TnWwY4Tpc44h[XO|YYm= NWXV[mduOzBibXnudy=> NX3nSoFbUW6qaXLpeIlwdiCxZjDQUGQyKGmwIHj1cYFvKEOjbIWtNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCyaH;zdIhifGmmeXzieZRidm:uLWvkPX0heHKxZIXjeIlwdiCjZoTldkA{OCCvaX7zJIJ6KG2jc4Ogd5Bm[3S{b33leJJq[yCjbnHsfZNqeyxiSVO1NF01NjhizszN M4XBU|E6OTN4OUe1
MCF12A cells NWTXPXA4WHKxbHnm[ZJifGmxbjDhd5NigQ>? M13aVFQ5KGh? NWf1cmxqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBme3S{b3flckBz\WOncITvdk1l\W[rY3nlcpQhcHWvYX6gUWNHOTKDIHPlcIx{KGmwY4XiZZRm\CC5aYToJFAvODB|IH7NJI9nKGW|dILh[IlwdCCjbnSgNE4xOSCwTTDv[kB1\XO2b4P0[ZJwdmViYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmgbY4heHKnc3XuZ4Uhd2ZiNTWg[oV1[WxiYn;2bY5mKHOncoXtMEBIUTVyPUOuN|EyOzFizszN MWOyNVUyOzJ5NR?=
MCF7:WS8 cells NWLrNZo4TnWwY4Tpc44h[XO|YYm= NHTHRWJC[3SrdnH0bY9vKG:oIHj1cYFvKEWUIHnuJIh2dWGwIF3DSlc7X1N6IHPlcIx{KGW6cILld5NqdmdiZYP0do9o\W5icnXzdI9ve2m4ZTDlcIVu\W62IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigQ>? Mk\NNlA{OzR|Nki=
HEK293 cell NX74bGM4TnWwY4Tpc44h[XO|YYm= NYPRN2U1OzBibXnudy=> MmrTTY5pcWKrdHnvckBw\iCJRmCteIFo\2WmIHj1cYFvKFCOREKg[ZhxemW|c3XkJIlvKGi3bXHuJGhGUzJ7MzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBxcG:|cHjheIllgWykdYThco9tNVumOW2gdJJw\HWldHnvckBi\nSncjCzNEBucW6|IHL5JI1ie3Nic4DlZ5Rzd22ndILpZ{BidmGueYPpd{whUUN3ME2wMlA1PCEQvF2= MU[xPVE{Pjl5NR?=
MCF12A cells M371TXBzd2yrZnXyZZRqd25iYYPzZZk> M2HGVFQ5KGh? NIHR[4JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIV{fHKxZ3XuJJJm[2WydH;yMYRm\mmlaXXueEBpfW2jbjDNR2YyOkFiY3XscJMhcW6ldXLheIVlKHerdHigNE4xPiCwTTDv[kBme3S{YXTpc4wh[W6mIECuNFchdk1ib3[geIV{fG:|dHXyc45mKGGodHXyJFQ5KGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7IHnuJJBz\XOnbnPlJI9nKG[ndHHsJIJwfmmwZTDz[ZJ2dSCjbnSgUpVU\XK3bTygS2k2OD1|Lki5NFQ2KM7:TR?= NEPWcnYzOTVzM{K3OS=>
HEK293 cells NEK3e4JHfW6ldHnvckBie3OjeR?= MUPB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIHXzeJJw\2WwIILlcIF1\WRicnXj[ZB1d3JiZ3HtcYEh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGdKPTB;MT6zOUDPxE1? M4fOZlI2OzB3Nki4
rat GH3 cells M4jGNGZ2dmO2aX;uJIF{e2G7 MoXVOFghcA>? M1TUVWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiRWKgbY4hemG2IFfIN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHXzeJJi\GmxbD3pcoR2[2WmIIDyc4xi[3SrbjDn[Y5mKGW6cILld5Nqd25iYYSgNVAoNTZiTTDh[pRmeiB2ODDodpMh[nliUmStVGNTKGGwYXz5d4l{ MlXDNlQ5ODVzOUm=
MCF7:WS8 cells MojySpVv[3Srb36gZZN{[Xl? M4XEOFQ5KGh? MljXRYdwdmm|dDDhZ5Rqfmm2eTDheEBGWiCrbjDoeY1idiCPQ1[3PndUQCClZXzsd{Bie3Onc4Pl[EBieyCJUlXCNUBo\W6nIHX4dJJme3Orb36gZZQhOTBpLU[gUUBi\nSncjC0PEBpenNiYomgVnQuWEOUIHHuZYx6e2m| MmraNlQ5ODVzOUm=
rat GH3 cells M2DH[mZ2dmO2aX;uJIF{e2G7 NUXGZlVEPDhiaB?= M1fuNGFvfGGpb37pd5Qh[WO2aY\peJkh[XRiRWKgbY4hemG2IFfIN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHXzeJJi\GmxbD3pcoR2[2WmIIDyc4xi[3SrbjDn[Y5mKGW6cILld5Nqd25iYYSgNVAoNTFyIITvJFExLy14IF2gZYZ1\XJiNEigbJJ{KGK7IGLUMXBEWiCjbnHsfZNqew>? NWTVdmlJOjR6MEWxPVk>

... Click to View More Cell Line Experimental Data

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: Adult Rat and Mouse Cardiac Myocytes
  • Concentrations: 0, 0.5, 1, 3, 5, and 10 µM
  • Incubation Time: 15-45 min
  • Method:

    For sarcomere length measurements, cells are covered in Tyrode’s containing 4OHT, allowed to reach 36 ± 1°C, and then stimulated at 0.2 Hz.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: Sprague-Dawley rats
  • Formulation: dissolved in 200 μl tricaprylin
  • Dosages: 21 mg/kg, 54 μmol/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 77 mg/mL (198.7 mM)
Water Insoluble
Ethanol Insoluble

* 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 387.51
Formula

C26H29NO2

CAS No. 68392-35-8
Storage powder
in solvent
Synonyms Afimoxifene

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03063619 Recruiting Mammographically Dense Breast M.D. Anderson Cancer Center|National Cancer Institute (NCI) May 1 2017 Phase 2
NCT02993159 Recruiting Ductal Breast Carcinoma In Situ|Estrogen Receptor Positive Northwestern University|National Cancer Institute (NCI)|BHR Pharma LLC May 31 2017 Phase 2
NCT03063619 Recruiting Mammographically Dense Breast M.D. Anderson Cancer Center|National Cancer Institute (NCI) May 1 2017 Phase 2
NCT02993159 Recruiting Ductal Breast Carcinoma In Situ|Estrogen Receptor Positive Northwestern University|National Cancer Institute (NCI)|BHR Pharma LLC May 31 2017 Phase 2
NCT00952731 Completed Ductal Breast Carcinoma in Situ|Estrogen Receptor-positive Breast Cancer Northwestern University|National Cancer Institute (NCI) December 2009 Phase 2
NCT00952731 Completed Ductal Breast Carcinoma in Situ|Estrogen Receptor-positive Breast Cancer Northwestern University|National Cancer Institute (NCI) December 2009 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID