Fulvestrant

Catalog No.S1191 Synonyms: ICI-182780, ZD 9238

Fulvestrant Chemical Structure

Molecular Weight(MW): 606.77

Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay.

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Cited by 26 Publications

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay.
Targets
ER [1]
(Cell-free assay)
0.94 nM
In vitro

Fulvestrant is an effective inhibitor of the growth of ER-positive MCF-7 (with IC50 of 0.29 nM) but with no effect on the growth of ER-negative BT-20 human breast cancer cells. Fulvestrant causes accumulation of cells in G0/G1 and also reduces the proportion of cells capable of continued DNA synthesis. [1] Fulvestrant competitively inhibits binding of oestradiol to the estrogen receptor. Fulvestrant blocks nuclear localization of the ER through impairing receptor dimerisation, and energy-dependent nucleo-cytoplasmic shuttling. Because of the instability of fulvestrant-ER complex, the binding of Fulvestrant with ER finally results in accelerated degradation of the ER protein. [2] Fulvestrant (10 nM) not only decreases IGF-IR mRNA levels but also decreases the half-life. [3] Treatment with 100 μM Fulvestrant leads to a time dependent increase of TNFR1 and TRADD steady-state mRNA levels in MCF-7 cells. [4] Fulvestrant is capable of down-regulating androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells. Fulvestrant also significantly attenuates R1881-stimulated growth by 70%. [5] Fulvestrant is able to modulate mitosis and cell death in immature cerebellar neurons via rapid activation of MAPK. [6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 Ml7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFi2XpAyNjNvMUCwNEBvVQ>? NGPxOVQ1QCCq NUXOcZZDcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NV3DPVlMOjR7N{myPVQ>
MCF-7/LTED NWHoSHMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEC1Z44yNjNvMUCwNEBvVQ>? NEfGZZA1QCCq NGLke25qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVmyOFk4QTJ7NB?=
HCC1428 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP6NU4{NTFyMECgcm0> MnXmOFghcA>? NUPTcIFPcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M2i3OFI1QTd7Mkm0
HCC1428/LTED NXjNS2JRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTiWow1OS5|LUGwNFAhdk1? M1PhRlQ5KGh? MlXxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NF7iVHMzPDl5OUK5OC=>
LCC1 MlXpSpVv[3Srb36gRZN{[Xl? NYT5eJk1OTByIH7N NH3Mc481QC1zNESgbC=> NGf6XGFi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= NHH5WGUzPDh3OEK3Oy=>
LCC9 NFyxXnZHfW6ldHnvckBCe3OjeR?= MXqxNFAhdk1? MlrROFguOTR2IHi= MUDhZ5RqfmG2ZYOgWXBTKHOrZ37hcIlv\w>? NXH3cZdPOjR6NUiyO|c>
MCF-7  M13Wemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\1NVAxKG6P M{PH[FUh\A>? NGXIeGtqdmirYnn0d{Bk\WyuIHfyc5d1cCC2bzCxNQ+9jQ>? NUfhdVN4OjR6MUm1OVA>
mesangial  M3vBV2Z2dmO2aX;uJGF{e2G7 NVzVRVlXOC5zLUGwNEBvVQ>? NE\YcWg1QCCq MXjzeZBxemW|c3XzJHRITi4QskGtbY5lfWOnZDD0fZBmKEmYIHPvcIxi\2Ww M33SVVI1Pzl|NkO5
Mesangial NVzQbYRWTnWwY4Tpc44hSXO|YYm= NVrjOYF[OC5zLUGwNEBvVQ>? NYjlPG1kOC53IHi= NE\sSlNqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgV41i\DJicHjvd5Bpd3K7bHH0bY9vKH[rYTDHVGVT MonPNlQ4QTN4M{m=
ER+ MCF-7/2a NGrtOI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkP4TWM2OD1yLkCwOEDPxE1? NVr1PHFROTV|MkS4PFQ>
ER+ MCF-7 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TLdFIxOCCq NUfwdXNlUUN3ME2wMlIyKG6P NHflVWgyPTN{NEi4OC=>
MCF-7  M{fDWWZ2dmO2aX;uJGF{e2G7 NG[wNXIyOMLibl5CpC=> MUe3NkBp MYLy[ZZmenOnczD0bIUh\XO2cn;n[Y4h\W[oZXP0LGlEPTBiMT65JOOYKDFy4pkSPUBOMQ>? NI\U[2kzPDlyOE[1Ni=>
MCF-7  MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxyqCxZjDhdJBzd3irbXH0[Yx6KDJibl2= NWHUe4tTOjN2NEizOFY>
H1975  M1S1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1f5bFPDqM7:TR?= MkL1NUBu NGLNTW1qdmO{ZXHz[ZMhfGinIHfl[ol1cW6rYjDz[Y5{cXSrdnn0fUBw\iCKMUm3OUBk\Wyuc9Mg MYWyOFI3QDhzMB?=
H1975 M3rjWWZ2dmO2aX;uJGF{e2G7 M33TSVPDqM7:TR?= M1LnN|EhdQ>? MUD1dJJm\3WuYYTld{B1cGVibHX2[Ywhd2ZiTHX0MVdk MmjENlQzPjh6MUC=
MCF-7  MXTGeY5kfGmxbjDBd5NigQ>? Ml;qNVAx6oDLbl5CpC=> M4XkS|czKGh? NICxZ4Zz\X[ncoPld{B1cGVicILveIVkfGm4ZTDl[oZm[3Rib3[gSVLDqGmwIHPlcIwhcW64YYPpc44> NX\GTndiOjN7M{[3O|M>
MCF-7  M4fWOmZ2dmO2aX;uJGF{e2G7 NHP2eoEyODEkgJnuUeKh NYfjPIs2OjRxNEigbC=> Mo\2[oFkcWyrdHH0[ZMhcW64YYPpc44hfGi{b4XnbEBOVVC|JzDtc4R2dGG2aX;u M1H6XVI{QTN4N{ez
BT474-tet-shMED1 NF\jVHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTZOHVyOC5zLUWg{txO NF3pUFU4KGR? NU\XSG86cW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MnLnNlM6OzZ{M{S=
ZR75-1-tet-shMED1  NUTTeGM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvhTmx4OC5zLUWg{txO MlLlO{Bl NWTzTWVocW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MmDRNlM6OzZ{M{S=
MCF-7-tet-shMED1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYWwMlEuPSEQvF2= M{[1W|ch\A>? M3LuXolv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NGjDWIczOzl|NkKzOC=>
HepG2  NYruZopxTnWwY4Tpc44hSXO|YYm= M{DmdlAvODFvMUCg{txO MnTxNVghcMLi NWLC[HR6[WO2aY\heIV{KHSqZTDFVmUudWWmaXH0[YQhfHKjboPjdolxfGmxbjDv[kBCTjKHUh?= MmnVNlM4OzNzOEi=
MCF-7L  NHHUXFlHfW6ldHnvckBCe3OjeR?= M3L3WlExOCCwTdMg MVixNEBucW5xMkSgbE81QCCq NHPYdZBz\XO3bITzJIlvKEWJRmKsJGhGWjJiYX7kJGhGWjNicHjvd5Bpd3K7bHH0bY9vKGG2IIDyc4xwdmenZDDlfJBwe3W{ZR?= MoTINlM3QDZ2MU[=
MCF-7L  NG\hT5JHfW6ldHnvckBCe3OjeR?= NH\3cYUyODBibl5CpC=> M2DKWlQ5KGh? NYW5ZWt1cW6mdXPld{B2eHKnZ4XsZZRqd25ib3[gcXJPSSCxZjDFS2ZTKGyrZ3Hu[EBJSi2HR1[= NVfYWHJXOjN4OE[0NVY>
MCF-7L NVm2dXZ1TnWwY4Tpc44hSXO|YYm= NWDYRYRFOTByIH7NxsA> M3HHXVQ5KGh? MYPpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT M3fNVVI{Pjh4NEG2
C4-12  NHrVTG5HfW6ldHnvckBCe3OjeR?= NYfqTWs4OTByIH7NxsA> NWOyPFU2PDhiaB?= NYrObWNIcW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= MViyN|Y5PjRzNh?=
MCF-7L MYrGeY5kfGmxbjDBd5NigQ>? M1XCcVExOCCwTdMg NVjjOXluOjRiaB?= MX3pcoR2[2W|IFXHSnIheGixc4Doc5J6dGG2aX;uJJJmeXWrcnXkJGhDNUWJRjDmeY5kfGmxbh?= MV:yN|Y5PjRzNh?=
MMQ  NU[4S|NHTnWwY4Tpc44hSXO|YYm= NYjpcW5YOC14MkWgcm0> MkXIO|IhcA>? MVPkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCnc4Tyc4dmdiC{ZXPldJRwei4QsTCoSXLPuSl? M3PRUlI{PTJ|M{W3
H1975  MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHtNE4{OTJ3LUGwJO69VQ>? NWnpcpFtPiCm M2LiRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MX[yN|M6QTl3Nx?=
H1975  M1z4XGFxd3C2b4Ppd{BCe3OjeR?= M4Ttc|IxOCCwTR?= MXe3NkBp NGq5cVBmdmijbnPld{BmemyxdHnubYIhcW6mdXPl[EBieG:ydH;zbZM> NYPMc2o1OjN|OUm5OVc>
MCF-7  MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\B[|ExNzFyMD:xNFAxKG6P NH[zWnMzNzRxNjDk NGPw[I5FVVOR NHXRZnVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy NYTBNIs6OjN|MUO1NFY>
MCF-7  NHfRcpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PZeFExOCCwTR?= Mn62OEBl NGjSPHhFVVOR M{e1dYlv\HWlZYOgZUBpcWeqZYKgdJJweG:{dHnvckBw\iClZXzsd{BqdiC2aHWgS|EheGijc3ZCpC=> NX;ZVYcyOjN|MUO1NFY>
MLO-Y4  MYDGeY5kfGmxbjDBd5NigQ>? Moe3NeKh|ryP MmHVNUBp MmC3bY5pcWKrdIOgSVIucW6mdXPl[EBEgDR|IHX4dJJme3Orb36= NY[zUI9{OjN{NEewOVc>
MCF-7 M{fuWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPQe4YyODBibl2= M12xdFQ5KGh? NHHrfZFi[nKxZ3H0[ZMhfGinIIDyc4xq\mW{YYTpeoUh\W[oZXP0JI9nKG2xZHXyZZRmKG6rdILvd4F1cX[nIIP0doV{ew>? Mne3NlMzOTZ5NES=
TG1-1  NFvTfHVHfW6ldHnvckBCe3OjeR?= NVP1cIZpOcLizszN MnnwNlQhcA>? MWrhZpJw\2G2ZYOgSVLDqGmwZIXj[YQh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= NWPa[WdQOjNyOEi2NFc>
TG1-1  M{CzXGZ2dmO2aX;uJGF{e2G7 MofzNeKh|ryP MkT0NlQhcA>? M2DFRYFjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhWEl|Sx?= MXOyN|A5QDZyNx?=
MCF7 NGrSc4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEK0dWgyODBibl2= NEf4dJc1QCCq M4Gx[Yxm[WS|IITvJIEhe2mvaXzhdkBtd3O|IHnuJJN2en[rdnHsJIF{KHerdHig[I95d3K3YnnjbY4h[WyxbnW= MXiyN|A4PzJ2OR?=
MCF7 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLJZpQyODBibl2= MV:0PEBp NWLaVXhC\W6qYX7j[ZMhdnW2bHnuMY1m\GmjdHXkJINmdGxiZHXheIg> NHO5e2kzOzB5N{K0PS=>
MCF-7  MkTLSpVv[3Srb36gRZN{[Xl? MkTZOkBp M2nxcWROW09? MUDheJRmdnWjdHXzJJRp\SCobIXkbY95d26rbD2gc5Ih\mWwaHX4ZY1q\C2rbnT1Z4VlKGmwY4LlZZNmKGmwIH3pVk0zOSCneIDy[ZN{cW:w NIS2emMzOzB3MkCzOi=>
MCF-7 M3Ppe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVO1TJNqOTByIH7NM|Eh|ryP NFfzb2Q2KGR? M{jobIlvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kAyP87{LXXzeJJi\GmxbB?= NIPNPJMzOjl6Mke2OS=>
MCF-7 MkjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;TT3dyOTByIH7N MnTlOUBl NUnHPY5PcW6qaXLpeJMhfGinIIP0bY12dGG2aX;uJI9nKG[3c3HybYVtcW5iSB?= NUPJe3VOOjJ7OEK3OlU>
1471.1 MXrGeY5kfGmxbjDBd5NigQ>? MVGxNFAhdk1? MoK4NUBp MX3FeG9JyqB? MnqweIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu MoXRNlI5PjlzME[=
MCF-7 NFXiRlhHfW6ldHnvckBCe3OjeR?= Ml3CNVAxKG6P M1rWflEhcA>? NIjqclVGfE:KwrC= NYT4eFlXfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv NXTGelg1OjJ6NkmxNFY>
HeLa M33GOGZ2dmO2aX;uJGF{e2G7 NV\Fc4x7OTByIH7N M4jtNlEhcA>? MXfFeG9JyqB? NYjZfGlbfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv NIfITY8zOjh4OUGwOi=>
COS-7  MkPPSpVv[3Srb36gRZN{[Xl? MU[xNFAhdk1? NXnMbplVOSCq MWXFeG9JyqB? M2PpOpRic2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> MXeyNlg3QTFyNh?=
BG1L-OHTLT  NVXrNGMxTnWwY4Tpc44hSXO|YYm= M1XM[|ExyqCwTR?= MUWyOOKhcMLi M3vCdIlvcGmkaYTzJGVT|rFiZYjwdoV{e2mxbh?= NFWxd2IzOjZ3MkW1PC=>
BG1L-ICILT MlvkSpVv[3Srb36gRZN{[Xl? M2P1[FExyqCwTR?= MnrONlTDqGkEoB?= Mk\0bY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w NV;xVJhsOjJ4NUK1OVg>
PC-9 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DYW|AvODB|LUOwJO69VQ>? NEnZSXk1QCCq NF\xfIRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVzCVWU{OjJ3NkC2N|Q>
H1650 MmfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTOPI0xNjByMz2zNEDPxE1? NWezc3g{PDhiaB?= M2TvZolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MlfRNlI2PjB4M{S=
H1975 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVj5U2p1OC5yMEOtN|Ah|ryP MorROFghcA>? MoDlbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MlHRNlI2PjB4M{S=
H1975 NV;URpJ1TnWwY4Tpc44hSXO|YYm= MonaN:Kh|ryP MXmzJIg> NFXOT2Zi[nKxZ3H0[ZMhfGinIIDoc5NxcG9vRVfGVkBqdmS3Y4Tpc44h[nliZYP0do9o\W5? NUDUdmN2OjJ3NkC2N|Q>
H1975 MVTGeY5kfGmxbjDBd5NigQ>? NVH6PZhwO8LizszN Ml7NO{Bl M{HPbYlv\HWlZYOgSWdHWiCneIDy[ZN{cW:w M3jkUlIzPTZyNkO0
HTR-8 NXjyTWl4TnWwY4Tpc44hSXO|YYm= NYjLZpVYOcLizszN MnvsNU01QCCq MXfkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCLR1\CVFchdVKQQR?= NHTzXmozOjN6M{GxNS=>
JEG-3 MkHXSpVv[3Srb36gRZN{[Xl? M1nzPFHDqM7:TR?= NYmzbJBKOS12ODDo M33TToRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B NEW2bmkzOjN6M{GxNS=>
Huh7 MWnGeY5kfGmxbjDBd5NigQ>? M1Hn[VUxyqEQvF2= MVi0PEBp MUPpcohq[mm2czDn[Y5qe3SnaX6tcYVlcWG2ZXSgVG9POSC2cnHud4FkfGm4YYTpc44> M{nzVlIzOzB2Mkm2
201T MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWm1JO69VQ>? MWq3NkBp MVvpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIghfmGwZHX0ZY5q[g>? Mnv1NlIzPTh2N{[=
A549  NHLD[IJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUO1JO69VQ>? NVTYUVBUPzJiaB?= NWq5dXhQcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\hcoRmfGGwaXK= MkHHNlIzPTh2N{[=
MCF-7 NY\ETHpETnWwY4Tpc44hSXO|YYm= NF;v[mUyyqEQvF2= M33kSlI1KGkEoB?= NEjQNGdld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? NVm3eVNiOjJyNEmzNVY>
HCC-1428 M{X0UmZ2dmO2aX;uJGF{e2G7 M1fCdVHDqM7:TR?= MkKyNlQhcMLi Mn\2[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh NWfHZlQ5OjJyNEmzNVY>
MDA-361 MXLGeY5kfGmxbjDBd5NigQ>? M3T6cVHDqM7:TR?= NFrTR3UzPCCqwrC= MWXkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb36gbY5lfWOnZDDifUA1NU:KLWSgxsA> MnPCNlIxPDl|MU[=
ZR75-1 MkXwSpVv[3Srb36gRZN{[Xl? NVHWRWpUOcLizszN MnzONlQhcMLi NXv5XVgz\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi MXiyNlA1QTNzNh?=
MCF-7 NWjEcXdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVuxxsDPxE1? MV:1MVExKGR? M17jfJN2eHC{ZYPz[ZMhTTJvaX7keYNm\CCpcn;3eIghcW6qaXLpeIlwdg>? NF\XN|IzOjB2OUOxOi=>
HCC-1428 M{HseWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXWXnh7OcLizszN NXzpeFAzPS1zMDDk M{fvV5N2eHC{ZYPz[ZMhTTJvaX7keYNm\CCpcn;3eIghcW6qaXLpeIlwdg>? NXLDOY1XOjJyNEmzNVY>
MDA-361 MkHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HQSlHDqM7:TR?= MXO1MVExKGR? NHOzOXh{fXCycnXzd4V{KEV{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? NVzUUGpJOjJyNEmzNVY>
ZR75-1 NXK1VWZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjtVXF[OcLizszN MXu1MVExKGR? MXfzeZBxemW|c3XzJGUzNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> M3u3b|IzODR7M{G2
MCF-7/AC-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3rfnZyOC1yLkKg{txO NVHIOXhOPiCm MUHpcohq[mm2czDj[YxtKGe{b4f0bEBud2Snc4TsfS=> M3PEdlIzODR{N{my
MCF7 NGrWdG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PMdVExKML3TR?= NYG5U29KPDhiaB?= MlvVbY5lfWOnczDj[YxtKGmwaHnibZRqd25id3jpZ4gh[2GwIHLlJIVvcGGwY3XkJIJ6KG[rYoLvZoxie3S| Ml;mNlIxPDF6OEe=
MMQ MlT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3DNE03OjVibl2= M1jmelczKGh? M{faR5Bzd2S3Y3XzJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd28EoB?= MV:yNlAyPTFyMR?=
MMQ M3TmNmZ2dmO2aX;uJGF{e2G7 NWT4clcxOC14MkWgcm0> NH3BPHA4OiCq M2XLXpBzd2S3Y3XzJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEwh\G:|ZT3k[ZBmdmSnboSgdoVlfWO2aX;uJIlvKFCUTDDz[YNz\XSrb36= MmXwNlIxOTVzMEG=
MCF7 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjFeGN3OC1zIN88US=> MVWyOE0yOjBiaB?= MUXpcohq[mm2czD0bIUh\3Kxd4ToJI9nKE2FRketXWIuOcLi MorKNlE5PjN{NUi=
HepG2 NGOxc3lCeG:ydH;zbZMhSXO|YYm= M3TrZ|AvOcLizszN MVeyOEBp NFzvbpdi[m:uaYPo[ZMhfGinIHXzeJJw\2WwLXnu[JVk\WRidYCtdoVofWyjdHnvckBw\iCjcH;BTUBidmRiYYDvUS=> NIThdJIzOThzNkKzNy=>
MCF7–iFR3 M{nnfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7zNlAuOTByIH7N M2jXVVk3KGh? MYLlcohidmOnczDBVE1qdmS3Y3XkJINmdGxiZ4Lve5RpKGmwaHnibZRqd25? NWj6WVJSOjF5OUK4PFk>
MCF7S NFe0VlVHfW6ldHnvckBCe3OjeR?= Mn3tNeKh|ryP M3zMdlQ5KGh? NFK0SHNld3ewcnXneYxifGW|IH;2[ZJidGxiRWNOtUBxem:2ZXnuJIxmfmWucx?= MXSyNVU{OzF7NR?=
MCF7 NWHIOGtYTnWwY4Tpc44hSXO|YYm= NVXINZRKOcLizszN NUnldZF7PDhiaB?= M3nWfYRwf26{ZXf1cIF1\XNib4\ldoFtdCCHUt8xJJBzd3SnaX6gcIV3\Wy| M4XlcVIyPTN|MUm1
MCF7S MVfGeY5kfGmxbjDBd5NigQ>? MUexxsDPxE1? M1;ENFch\A>? M{TMPYF1fGWwdXH0[ZMhfHWvb4LzdIhmemViZn;ycYF1cW:wIHHu[EBxem:uaX\ldoF1cW:w M1zoS|IyPTN|MUm1
MCF7S MlvPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPabGkxNjVxMTFOwG0> MX:3JIQ> MoXYSG1UVw>? NXPaUmtZ\GWlcnXhd4V{KGOnbHyg[Zhx[W6|aX;u MojGNlE2OzNzOUW=
T47D  Mny5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULud40xPCCwTR?= MV60NEBp NEXKRXR{fXCycnXzd4V{KGOnbHyg[5Jwf3SqIH3v[IVz[XSnbIm= M2TkNlIyPDhyM{mx
BT474  M3vzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYi0JI5O MmHNOFAhcA>? NUfNPVBoe3WycILld5NmeyClZXzsJIdzd3e2aDDtc4RmemG2ZXz5 NITpWVUzOTR6MEO5NS=>
T47D  NE[4VGVHfW6ldHnvckBCe3OjeR?= NGDubGwyOCCwTR?= MVO0NEBp NYXNW|NI\G:5boLl[5Vt[XSnczDFVu6yKHC{b4TlbY4> MUWyNVQ5ODN7MR?=
BT474  MkPnSpVv[3Srb36gRZN{[Xl? MVSxNEBvVQ>? M37MR|QxKGh? NUPkXHFI\G:5boLl[5Vt[XSnczDFVu6yKHC{b4TlbY4> NE\OW5czOTR6MEO5NS=>
MCF7 MnT2SpVv[3Srb36gRZN{[Xl? NGjpZ2gyODBibl2= NEjkZYI4KGR? MnT4doVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> M2PIZVIyOzl4MEm0
T47D  Mo\2SpVv[3Srb36gRZN{[Xl? MmDsNVAxKG6P Ml7EO{Bl NEDndGhz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 MknmNlE{QTZyOUS=
BT474  NXnpVmtJTnWwY4Tpc44hSXO|YYm= NWfkcXFJOTByIH7N NXT1eHVLPyCm M3;5eJJm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> MoW4NlE{QTZyOUS=
MDAMB361 MVXGeY5kfGmxbjDBd5NigQ>? MkXsNVAxKG6P NULseIF4PyCm MXzy[YR2[2W|IFXS{tEh\XiycnXzd4lwdiC|aXfubYZq[2GwdHz5 M2rUcFIyOzl4MEm0
MCF7 MlvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\i[W0xNjBzLUGg{txO MVO3JIQ> NF;DfXRz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NXrJdVl1OjF|OU[wPVQ>
T47D  M{DIbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TQRlAvODFvMTFOwG0> NWXOflFjPyCm Mn3idoVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MmHuNlE{QTZyOUS=
BT474  NGXMVIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrRNE4xOS1zIN88US=> Mk\aO{Bl NUXhW|JoemWmdXPld{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MlXjNlE{QTZyOUS=
MDAMB361 NF3KS4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HmTFAvODFvMTFOwG0> M3X0OVch\A>? NUPVXIs3emWmdXPld{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NYL4VI1QOjF|OU[wPVQ>
MCF7 NWrhSpUzTnWwY4Tpc44hSXO|YYm= NG\kXIQyODBibl2= NFPEfHI4KGR? MnLtbY5lfWOnczDv[kBGemKEMzDhcoQhTXKkQkSgdoVk\XC2b4Kg[ZhxemW|c3nvckBidmRic3nncoFtdGmwZx?= NV;2fm06OjF|OU[wPVQ>
T47D  MXXGeY5kfGmxbjDBd5NigQ>? MnvkNVAxKG6P MX:3JIQ> MoG4bY5lfWOnczDv[kBGemKEMzDhcoQhTXKkQkSgdoVk\XC2b4Kg[ZhxemW|c3nvckBidmRic3nncoFtdGmwZx?= NXLDNVVbOjF|OU[wPVQ>
BT474  MVTGeY5kfGmxbjDBd5NigQ>? NEjUbFUyODBibl2= MV63JIQ> NGLsZ4hqdmS3Y3XzJI9nKEW{YlKzJIFv\CCHcnLCOEBz\WOncITvdkBmgHC{ZYPzbY9vKGGwZDDzbYdv[WyuaX7n NFexN4czOTN7NkC5OC=>
MDAMB361 MVTGeY5kfGmxbjDBd5NigQ>? Mn7DNVAxKG6P M1y1dlch\A>? MYLpcoR2[2W|IH;mJGVz[kJ|IHHu[EBGemKENDDy[YNmeHSxcjDlfJBz\XO|aX;uJIFv\CC|aXfuZYxtcW6p NX3KdYlnOjF|OU[wPVQ>
MCF7 MlW5SpVv[3Srb36gRZN{[Xl? MYWxNEBvVQ>? NIjiWmg6PiCq M17pRYRwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvcuKh NYX4R4lvOjF|N{izN|M>
MDA-MB-231 M1XtOGZ2dmO2aX;uJGF{e2G7 MlO5NVAhdk1? MUG5OkBp NH60e2Vld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc47DqA>? M2nhbVIyOzd6M{Oz
SK-BR-3 NGPBWIZHfW6ldHnvckBCe3OjeR?= MUSxNEBvVQ>? NXS2SoxOQTZiaB?= MXnkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb39CpC=> MYmyNVM4QDN|Mx?=
MCF-7 M2jBPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\yNVAxKG6P NGX5Xoo4Oi97NjDo M2LUOINifXOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NX3JWm9XOjF{OUm4OlI>
MMQ NHm5SHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHTNE4xODhvNkK1JI5O M1zRZlczKGh? MlnBbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nLTDhcoQh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NVW0[nM6OjB5MEC3OVU>
MMQ Mn73SpVv[3Srb36gRZN{[Xl? NEHGVpYxNjByOD22NlUhdk1? MmrJO|IhcA>? M{DqTIlvcGmkaYTzJHBTVCC|ZXPy[ZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M2rjO|IxPzByN{W1
MMQ MXrGeY5kfGmxbjDBd5NigQ>? MWKwMlA1NTZ{NTDuUS=> M4jkU|czKGh? MkTlbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w M1TGcFIxPzByN{W1
MMQ M2TxOmZ2dmO2aX;uJGF{e2G7 NYr4cmE3OC5yND22NlUhdk1? NUnpcXJDPzJiaB?= MkDMeZBz\We3bHH0[ZMhXEeIzsKzJIFv\CCWR1dOtnJKUSCneIDy[ZN{cW:w MnvrNlA4ODB5NUW=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
MDM2 / ER; 

PubMed: 24747123     


MCF7 (A) and T47D (B) cells were cultured in the presence of different concentrations of fulvestrant (Fulv) for 66 h. ER and MDM2 were detected by Western blot and normalized to β-actin. The decrease in protein expression (shown relative to vehicle control treatment) after fulvestrant treatment was calculated for each drug concentration. *P < 0.05 compared to vehicle control treatment. 

p-ErbB3 Y1289 / ErbB3 / p-ErbB4 Y1056 / ErbB4 / p-AKT / AKT / p-ERK / ERK; 

PubMed: 21396094     


Western blots showing the effect of increasing concentrations of heregulin β1 (HRGβ1) (0.1 to 10 ng/ml for five minutes) on total and phosphorylated ErbB3, ErbB4, AKT and extracellular signal-regulated kinases 1 and 2 (ERK1/2) protein expression in MCF-7 and T47D cells, maintained for 7 days in the presence of either fulvestrant (100 nM) of vehicle control (ethanol). 

ErbB3; 

PubMed: 23999432     


Immunofluorescence of ErbB3 in cells cultured for 24 hours with or without fulvestrant. 

ERα; 

PubMed: 19815064     


Breast cancer cells were treated with different doses of ICI for 3 hours. The expression levels of ERα and actin were assayed by Western blot using anti-ERα and anti-actin antibodies.

24747123 21396094 23999432 19815064
Immunofluorescence
IGF-1R / Erα; 

PubMed: 19815064     


Confocal microscope study of fulvestrant-induced ERα and IGF-1R co-localization on the cell membrane in non-permeabilized condition. Cells were starved in 1% DCC medium for 24 hr and then treated with either vehicle (left) or ICI at 100 nM (right) for 15 min. Treated cells were fixed in 4% formaldehyde and stained with mouse monoclonal anti-IGF-1R antibody (a), rabbit polyclonal anti-ERα antibody (b), or nuclear staining with DAPI (c). The merged images are shown in d. Scale bar = 20 μm.

Snail / E-cadherin ; 

PubMed: 23936773     


E-cadherin and Snail protein localization in MCF-7 cells 48 h after treatment of cells with E2 and the tested agents. C: control (untreated cells); E2: cells treated with 17β-estradiol; Fulv: cells treated with E2 + 100 nM Fulv. The image is representative of three independent experiments using a magnification of 63X.

19815064 23936773
Growth inhibition assay
Cell viability; 

PubMed: 29787591     


MTT assay of MCF-7 cells treated with various concentration of fulvestrant. Statistically significant reduced the % viability in MCF-7 cells (One-way ANOVA; ****p < 0.0001).

29787591
In vivo Fulvestrant is devoid of uterotropic activity, and when co-administered with estradiol, it effectively blocks the uterotropic action of estradiol with ED50 of 0.06 mg/kg/day s.c. in immature female rats. A single s.c. injection of 5 mg of Fulvestrant suspension blocks completely the growth of MCF-7 xenografts. The growth of transplants of the BrlO human breast tumor is also suppressed effectively by 10 μM Fulvestrant. [1] Fulvestrant (10 mg/rat, s.c.) reduces the androgen receptor expression, ERK1/2 phosphorylation and cell proliferation in the rat ventral prostate. [7] Fulvestrant also displays anti-angiogenesis in the chick egg chorioallantoic membrane. [8]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: MCF-7 breast cancer cells
  • Concentrations: 2.9 nM
  • Incubation Time: 5 days
  • Method: MCF-7 cells are cultured in multiwell plates (24-well, seeding density 4 × 104) in minimal essential medium containing phenol red, insulin (10 μg/mL), and 5% charcoal-stripped fetal calf serum without additional estradiol. Fulvestrant and/or estradiol are added in fresh medium 2 days after seeding. Cultures are maintained for 5 days with one further medium change and growth is assessed by measurement of total cell protein at the beginning and end of treatment and compared with that of controls treated with ethanol (0.1%) alone.
    (Only for Reference)
Animal Research:[6]
+ Expand
  • Animal Models: The human breast cancer xenografts MCF-7 in nude mice
  • Formulation: 50 mg/mL in arachis oil
  • Dosages: 5 mg/mouse
  • Administration: s.c. injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (164.8 mM)
Ethanol 100 mg/mL warmed (164.8 mM)
Water Insoluble
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.
0.4mg/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 606.77
Formula

C32H47F5O3S

CAS No. 129453-61-8
Storage powder
in solvent
Synonyms ICI-182780, ZD 9238

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04024436 Not yet recruiting Drug: TAS-120|Drug: Fulvestrant Metastatic Breast Cancer|FGFR2 Amplification Taiho Oncology Inc. August 30 2019 Phase 2
NCT03854903 Recruiting Drug: Palbociclib|Drug: Bosutinib|Drug: Fulvestrant Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer Georgetown University|Pfizer April 1 2019 Phase 1
NCT03584009 Recruiting Drug: Venetoclax|Drug: Fulvestrant Estrogen Receptor-positive (ER+)/Human Epidermal Growth Factor Receptor (HER2)-Negative Locally Advanced or Metastatic Breast Cancer Hoffmann-La Roche September 6 2018 Phase 2
NCT03393845 Recruiting Drug: Pembrolizumab|Drug: Fulvestrant Breast Cancer Nancy Chan MD|Merck Sharp & Dohme Corp.|Big Ten Cancer Research Consortium January 29 2018 Phase 2

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:

    Is there any information for the half-life of fulvestrant (Cat No.S1191)?

  • Answer:

    S1191, is about 13.5 to 18.5 hours in vivo: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2750771/. The half life of these compounds in cell culture might be different and we generally recommend replenishing with fresh drug every 24-48 hours.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID