Fulvestrant

For research use only. Not for use in humans.

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

71 publications

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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Selleck's Fulvestrant has been cited by 71 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 M3zJfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPHUJlHOS5|LUGwNFAhdk1? NVv1VFBYPDhiaB?= M4G2ZYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkDmNlQ6Pzl{OUS=
MCF-7/LTED M{n3cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HmblEvOy1zMECwJI5O NVzKbXhrPDhiaB?= M1LZXolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVjXeIs3OjR7N{myPVQ>
HCC1428 NEnSXmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUf4e|RNOS5|LUGwNFAhdk1? MmTaOFghcA>? MmrmbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mn;CNlQ6Pzl{OUS=
HCC1428/LTED M4LZcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Swe|EvOy1zMECwJI5O NGDx[JM1QCCq M3;5b4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHXpO4wzPDl5OUK5OC=>
LCC1 M4S3cWZ2dmO2aX;uJGF{e2G7 M3[wV|ExOCCwTR?= NF74R5A1QC1zNESgbC=> Mm\rZYN1cX[jdHXzJHVRWiC|aXfuZYxqdmd? MVuyOFg2QDJ5Nx?=
LCC9 NUfiVpFnTnWwY4Tpc44hSXO|YYm= NGnjWWEyODBibl2= NGjKSpU1QC1zNESgbC=> NYPpSGJK[WO2aY\heIV{KFWSUjDzbYdv[Wyrbne= NYjvdWt4OjR6NUiyO|c>
MCF-7  NUfNbm1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;lNmY3OTByIH7N Mm\iOUBl MUPpcohq[mm2czDj[YxtKGe{b4f0bEB1dyBzMP-8iS=> MkjwNlQ5OTl3NUC=
mesangial  NGmydpJHfW6ldHnvckBCe3OjeR?= NFH2bmQxNjFvMUCwJI5O MVi0PEBp NEPFV5F{fXCycnXzd4V{KFSJRj5OtlEucW6mdXPl[EB1gXCnIFnWJINwdGyjZ3Xu NHe0c|MzPDd7M{[zPS=>
Mesangial MULGeY5kfGmxbjDBd5NigQ>? NUnkSVY1OC5zLUGwNEBvVQ>? NUPJN|UyOC53IHi= MmG4bY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIGPtZYQzKHCqb4PwbI9zgWyjdHnvckB3cWFiR2DFVi=> NV\v[HdxOjR5OUO2N|k>
ER+ MCF-7/2a M2DXeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnflTWM2OD1yLkCwOEDPxE1? NWTqUnAyOTV|MkS4PFQ>
ER+ MCF-7 NV3NeWs{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjYeHZlOjByIHi= NGLKOVNKSzVyPUCuNlEhdk1? NHTJd5AyPTN{NEi4OC=>
MCF-7  NUDMXo9zTnWwY4Tpc44hSXO|YYm= MXSxNOKhdk4EoB?= NGfISWc4OiCq M{HLcJJmfmW{c3XzJJRp\SCnc4Tyc4dmdiCnZn\lZ5QpUUN3MDCxMlkhy5diMUFijLI6KE1r NGK1fmYzPDlyOE[1Ni=>
MCF-7  M{DRdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWqxUINvUUN3MNMgc4Yh[XCycn;4bY1ifGWueTCyJI5O MmqzNlM1PDh|NE[=
H1975  M4jJT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrhcWQ{yqEQvF2= M3;Ed|EhdQ>? M2L0TYlv[3KnYYPld{B1cGViZ3XmbZRqdmmkIIPlcpNqfGm4aYT5JI9nKEhzOUe1JINmdGy|wrC= M1rtdVI1OjZ6OEGw
H1975 NVvjRo1tTnWwY4Tpc44hSXO|YYm= MVKzxsDPxE1? M4ezZlEhdQ>? MmnpeZBz\We3bHH0[ZMhfGinIHzleoVtKG:oIFzleE04[w>? MlnXNlQzPjh6MUC=
MCF-7  MmDhSpVv[3Srb36gRZN{[Xl? MkXSNVAx6oDLbl5CpC=> MYi3NkBp M4T5VJJmfmW{c3XzJJRp\SCycn;0[YN1cX[nIHXm[oVkfCCxZjDFNuKhcW5iY3XscEBqdn[jc3nvci=> M4\icFI{QTN4N{ez
MCF-7  NVvybGpjTnWwY4Tpc44hSXO|YYm= NYrlVYZ1OTBy4pEJcm3DqA>? MkLUNlQwPDhiaB?= M1;PU4Zi[2muaYTheIV{KGmwdnHzbY9vKHSqcn;1[4ghVU2SczegcY9lfWyjdHnvci=> NHWzcpMzOzl|Nke3Ny=>
BT474-tet-shMED1 M3LNV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPGNE4yNTVizszN NX\ITmlKPyCm MVPpcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWLNNHkxOjN7M{[yN|Q>
ZR75-1-tet-shMED1  MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrTengxNjFvNTFOwG0> NUWxeGRpPyCm NWTCOI5kcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M3rMW|I{QTN4MkO0
MCF-7-tet-shMED1 NF;ydZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHXe3gxNjFvNTFOwG0> MnPTO{Bl MmLDbY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MnTZNlM6OzZ{M{S=
HepG2  MY\GeY5kfGmxbjDBd5NigQ>? MUGwMlAyNTFyIN88US=> NGKwZ4syQCCqwrC= M3qyR4FkfGm4YYTld{B1cGViRWLFMY1m\GmjdHXkJJRz[W6|Y4LpdJRqd25ib3[gRWYzTVJ? MWqyN|c{OzF6OB?=
MCF-7L  MX3GeY5kfGmxbjDBd5NigQ>? MWCxNFAhdk4EoB?= NHjoWVQyOCCvaX6vNlQhcC92ODDo M4jjPZJme3WudIOgbY4hTUeIUjygTGVTOiCjbnSgTGVTOyCyaH;zdIhwenmuYYTpc44h[XRicILvcI9v\2WmIHX4dI9{fXKn MWKyN|Y5PjRzNh?=
MCF-7L  MXPGeY5kfGmxbjDBd5NigQ>? M1jkeFExOCCwTdMg Moi1OFghcA>? NGXSXYdqdmS3Y3XzJJVxemWpdXzheIlwdiCxZjDtVm5CKG:oIFXHSnIhdGmpYX7kJGhDNUWJRh?= MnnuNlM3QDZ2MU[=
MCF-7L M2LhN2Z2dmO2aX;uJGF{e2G7 Mo[zNVAxKG6PwrC= MXm0PEBp M4fKO4lv\HWlZYOgSWdHWiCoYX3pcJkhdWWvYnXyJIFkfGm4YYTpc44hemWzdXny[YQhTVJ? NWP3RodCOjN4OE[0NVY>
C4-12  MlfUSpVv[3Srb36gRZN{[Xl? MVqxNFAhdk4EoB?= NVnI[nBEPDhiaB?= NVu4T4dZcW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= NW\uTFJGOjN4OE[0NVY>
MCF-7L M1\MUWZ2dmO2aX;uJGF{e2G7 NX\1cm5HOTByIH7NxsA> Mn6zNlQhcA>? M3HXdYlv\HWlZYOgSWdHWiCyaH;zdIhwenmuYYTpc44hemWzdXny[YQhUEJvRVfGJIZ2dmO2aX;u MnznNlM3QDZ2MU[=
MMQ  NWDY[WZITnWwY4Tpc44hSXO|YYm= NHS4SFcxNTZ{NTDuUS=> NWnvdlR6PzJiaB?= NHfMS4Zld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDld5Rzd2enbjDy[YNmeHSxcj5OtUApTVMQsTm= NWfrdnZDOjN3MkOzOVc>
H1975  NYHJNFFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnRNE4{OTJ3LUGwJO69VQ>? NVXGUYZUPiCm NX7BNpVlcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4iyTlI{Ozl7OUW3
H1975  NFTzd3JCeG:ydH;zbZMhSXO|YYm= NYC0fpZiOjByIH7N NGfXeFc4OiCq Mlr0[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz M4XmWFI{Ozl7OUW3
MCF-7  NEnRN4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvHNVAwOTByL{GwNFAhdk1? MYOyM|QwPiCm MkPySG1UVw>? M1e0S4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= MY[yN|MyOzVyNh?=
MCF-7  NHfqV41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU[xNFAhdk1? NWrJc3p1PCCm NXX2c45yTE2VTx?= NIjjbGhqdmS3Y3XzJIEhcGmpaHXyJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5idHjlJGcyKHCqYYPlxsA> MniyNlM{OTN3ME[=
MLO-Y4  M4m2bmZ2dmO2aX;uJGF{e2G7 Mlj1NeKh|ryP M2ToeFEhcA>? NFi5dVdqdmirYnn0d{BGOi2rbnT1Z4VlKEO6NEOg[ZhxemW|c3nvci=> Mk\yNlMzPDdyNUe=
MCF-7 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWxNFAhdk1? NXy1N3FQPDhiaB?= M{DoSoFjem:pYYTld{B1cGVicILvcIln\XKjdHn2[UBm\m[nY4Sgc4YhdW:mZYLheIUhdmm2cn;zZZRqfmVic4Ty[ZN{ MUiyN|IyPjd2NB?=
TG1-1  M{fYbWZ2dmO2aX;uJGF{e2G7 MXexxsDPxE1? NFmyXoIzPCCq NXq1SIFZ[WK{b3fheIV{KEV{wrDpcoR2[2WmIHHjZ5VufWyjdHnvckBw\iCKSV[tNe6y M2\VfFI{ODh6NkC3
TG1-1  MU\GeY5kfGmxbjDBd5NigQ>? MWOxxsDPxE1? MWWyOEBp NXfBRoxz[WK{b3fheIV{KEV{wrDpcoR2[2WmIHHjZ5VufWyjdHnvckBw\iCSSUPL MXmyN|A5QDZyNx?=
MCF7 NUDBeGtuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[zWIQyODBibl2= NELLb2o1QCCq M{nKU4xm[WS|IITvJIEhe2mvaXzhdkBtd3O|IHnuJJN2en[rdnHsJIF{KHerdHig[I95d3K3YnnjbY4h[WyxbnW= M4HL[|I{ODd5MkS5
MCF7 M3O0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HWUVExOCCwTR?= NVe0ZlRUPDhiaB?= MmPx[Y5p[W6lZYOgcpV1dGmwLX3l[IlifGWmIHPlcIwh\GWjdHi= NUnZ[mpbOjNyN{eyOFk>
MCF-7  NUXweI44TnWwY4Tpc44hSXO|YYm= M1vsOlYhcA>? NV;nVW5mTE2VTx?= NHHQUnRifHSnboXheIV{KHSqZTDmcJVlcW:6b37pcE0hd3JiZnXubIV5[W2rZD3pcoR2[2WmIHnuZ5Jm[XOnIHnuJI1qWi1{MTDlfJBz\XO|aX;u M2Xx[lI{ODV{MEO2
MCF-7 NIS2bZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfrT4l2OTByIH7NM|Eh|ryP NU[5bWVjPSCm M{LDVolvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kAyP87{LXXzeJJi\GmxbB?= MXmyNlk5Ojd4NR?=
MCF-7 NIPNdJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVv0UWdXOTByIH7N NUnN[JRuPSCm Mlz1bY5pcWKrdIOgeIhmKHO2aX31cIF1cW:wIH;mJIZ2e2G{aXXsbY4hUA>? M33qPFIzQTh{N{[1
1471.1 NXOwepplTnWwY4Tpc44hSXO|YYm= NVe2RW5QOTByIH7N NGDlWoYyKGh? NWnJTWhNTXSRSNMg M4rZUZRic2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> NHnwZnEzOjh4OUGwOi=>
MCF-7 MUXGeY5kfGmxbjDBd5NigQ>? NYLxN4hSOTByIH7N NIXxPWIyKGh? NFnHeVlGfE:KwrC= NHjmeHl1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> M2nmVFIzQDZ7MUC2
HeLa MnnuSpVv[3Srb36gRZN{[Xl? MVexNFAhdk1? MnfXNUBp NGjrWo1GfE:KwrC= NEfnWJJ1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> M2HWT|IzQDZ7MUC2
COS-7  NGexXmRHfW6ldHnvckBCe3OjeR?= NGP0R4QyODBibl2= MVOxJIg> MkSxSZRQUMLi MVj0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= MVKyNlg3QTFyNh?=
BG1L-OHTLT  NUDUc2pETnWwY4Tpc44hSXO|YYm= NYPRSnJSOTEEoH7N MWGyOOKhcMLi M37VOIlvcGmkaYTzJGVT|rFiZYjwdoV{e2mxbh?= M1HNTFIzPjV{NUW4
BG1L-ICILT NVjuXVRPTnWwY4Tpc44hSXO|YYm= NEPGS4QyOMLibl2= MY[yOOKhcMLi NHjzdIhqdmirYnn0d{BGWs7zIHX4dJJme3Orb36= MWOyNlY2OjV3OB?=
PC-9 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYewMlAxOy1|MDFOwG0> MU[0PEBp M2XWeYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1;DPFIzPTZyNkO0
H1650 NYT0b2pMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPLNE4xODNvM{Cg{txO MX20PEBp MVXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4rrdFIzPTZyNkO0
H1975 NX7tT2tLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqwMlAxOy1|MDFOwG0> MYO0PEBp NGnDZZFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NH:3[5kzOjV4ME[zOC=>
H1975 NUDNNYl5TnWwY4Tpc44hSXO|YYm= NVnYVZBqO8LizszN NUH0WoptOyCq NIHkT5Fi[nKxZ3H0[ZMhfGinIIDoc5NxcG9vRVfGVkBqdmS3Y4Tpc44h[nliZYP0do9o\W5? M4TzZlIzPTZyNkO0
H1975 MWLGeY5kfGmxbjDBd5NigQ>? NFPMUoU{yqEQvF2= NFnmSHc4KGR? M{DWT4lv\HWlZYOgSWdHWiCneIDy[ZN{cW:w M33Qb|IzPTZyNkO0
HTR-8 M3X6RWZ2dmO2aX;uJGF{e2G7 MYqxxsDPxE1? NYTDUIlZOS12ODDo MoLt[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSVfGRnA4KG2UTlG= MkDuNlI{QDNzMUG=
JEG-3 MVvGeY5kfGmxbjDBd5NigQ>? NGTVNnUyyqEQvF2= NVPNToRVOS12ODDo Mo[x[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSVfGRnA4KG2UTlG= MViyNlM5OzFzMR?=
Huh7 M2nCOGZ2dmO2aX;uJGF{e2G7 MYK1NOKh|ryP M3fVVFQ5KGh? NFOzdJdqdmirYnn0d{Bo\W6rc4TlbY4udWWmaXH0[YQhWE:QMTD0doFve2GldHn2ZZRqd25? MXOyNlMxPDJ7Nh?=
201T MlLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjhZos2KM7:TR?= MkL1O|IhcA>? M3nCV4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4YX7k[ZRidmmk NYfnVGFFOjJ{NUi0O|Y>
A549  NFe3bXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fQ[FUh|ryP NGfyNHA4OiCq NFnWVpdqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnHu[IV1[W6rYh?= Mk\aNlIzPTh2N{[=
MCF-7 NEK5RnBHfW6ldHnvckBCe3OjeR?= NFfSeHcyyqEQvF2= NWPw[YVGOjRiaNMg NEPXfohld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? Mln6NlIxPDl|MU[=
HCC-1428 M2SyU2Z2dmO2aX;uJGF{e2G7 MUmxxsDPxE1? MnqwNlQhcMLi Mn;Z[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh NETBW|EzOjB2OUOxOi=>
MDA-361 MWHGeY5kfGmxbjDBd5NigQ>? NEn0RoEyyqEQvF2= NUHzfHc1OjRiaNMg MnLD[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh NVXrOHdOOjJyNEmzNVY>
ZR75-1 M3j3d2Z2dmO2aX;uJGF{e2G7 MnizNeKh|ryP NYr0R3RYOjRiaNMg MmK0[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh Mlv3NlIxPDl|MU[=
MCF-7 M1HMeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWOxxsDPxE1? NX\ud2hDPS1zMDDk MX7zeZBxemW|c3XzJGUzNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> M1W1WlIzODR7M{G2
HCC-1428 M1zFRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXmwZXlqOcLizszN M3HRelUuOTBiZB?= Mnnid5VxeHKnc4Pld{BGOi2rbnT1Z4VlKGe{b4f0bEBqdmirYnn0bY9v NIXId5AzOjB2OUOxOi=>
MDA-361 NWTiR5dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqxxsDPxE1? M2r0XlUuOTBiZB?= NWnwcYc4e3WycILld5NmeyCHMj3pcoR2[2WmIHfyc5d1cCCrbnjpZol1cW:w NIHnT3czOjB2OUOxOi=>
ZR75-1 NFLkdHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D1VlHDqM7:TR?= M2TjeVUuOTBiZB?= M{PHdZN2eHC{ZYPz[ZMhTTJvaX7keYNm\CCpcn;3eIghcW6qaXLpeIlwdg>? MlXpNlIxPDl|MU[=
MCF-7/AC-1 NFfKdFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnSVI5SOC1yLkKg{txO MUm2JIQ> NVPIOFBkcW6qaXLpeJMh[2WubDDndo94fGhibX;k[ZN1dHl? NYXXe2JIOjJyNEK3PVI>
MCF7 NYDue2FTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKxNEDDvU1? NF7uVoM1QCCq MVzpcoR2[2W|IHPlcIwhcW6qaXLpeIlwdiC5aHnjbEBk[W5iYnWg[Y5p[W6lZXSgZpkh\mmkcn;icIF{fHN? MX6yNlA1OTh6Nx?=
MMQ M2n3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVywMVYzPSCwTR?= MnP6O|IhcA>? M1rjUZBzd2S3Y3XzJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd28EoB?= NUfFVHdXOjJyMUWxNFE>
MMQ NXzaVY1GTnWwY4Tpc44hSXO|YYm= M4C4[VAuPjJ3IH7N NWnOemNwPzJiaB?= NVX1c3NOeHKxZIXj[ZMh[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51NCCmb4PlMYRmeGWwZHXueEBz\WS3Y4Tpc44hcW5iUGLMJJNm[3KndHnvci=> Ml\hNlIxOTVzMEG=
MCF7 M4\rRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHwNE0yKM7:TR?= M{C4OVI1NTF{MDDo NF7oUVNqdmirYnn0d{B1cGViZ4Lve5RpKG:oIF3DSlcuYUJvMdMg NVrlVIVOOjF6NkOyOVg>
HepG2 NXvkUmNZSXCxcITvd4l{KEG|c3H5 NXrVRZl6OC5zwrFOwG0> MkDRNlQhcA>? MnXQZYJwdGm|aHXzJJRp\SCnc4Tyc4dmdi2rbnT1Z4VlKHWyLYLl[5Vt[XSrb36gc4Yh[XCxQVmgZY5lKGGyb12= MYCyNVgyPjJ|Mx?=
MCF7–iFR3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYOyNE0yODBibl2= M3PtUVk3KGh? M36wboVvcGGwY3XzJGFRNWmwZIXj[YQh[2WubDDndo94fGhiaX7obYJqfGmxbh?= MUiyNVc6Ojh6OR?=
MCF7S MUfGeY5kfGmxbjDBd5NigQ>? MkTUNeKh|ryP M2nDbFQ5KGh? NHfqflVld3ewcnXneYxifGW|IH;2[ZJidGxiRWNOtUBxem:2ZXnuJIxmfmWucx?= MmnQNlE2OzNzOUW=
MCF7 M1;6ZWZ2dmO2aX;uJGF{e2G7 MYixxsDPxE1? NULEU4dVPDhiaB?= MYfkc5dvemWpdXzheIV{KG:4ZYLhcIwhTVMQsTDwdo91\WmwIHzleoVtew>? MmjnNlE2OzNzOUW=
MCF7S M37qWWZ2dmO2aX;uJGF{e2G7 MXSxxsDPxE1? NIDtfYs4KGR? MYTheJRmdnWjdHXzJJR2dW:{c4Do[ZJmKG[xcn3heIlwdiCjbnSgdJJwdGmoZYLheIlwdg>? NFTqS3ozOTV|M{G5OS=>
MCF7S NGqxdoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPRNE42NzFizszN M1nlT|ch\A>? MVrEUXNQ NIfXTI1l\WO{ZXHz[ZMh[2WubDDlfJBidnOrb36= MnmxNlE2OzNzOUW=
T47D  M4D4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jyTVQhdk1? NYnlS|FpPDBiaB?= NG\LcWt{fXCycnXzd4V{KGOnbHyg[5Jwf3SqIH3v[IVz[XSnbIm= M4jDflIyPDhyM{mx
BT474  MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3DOEBvVQ>? MWe0NEBp MXvzeZBxemW|c3XzJINmdGxiZ4Lve5RpKG2xZHXyZZRmdHl? M2jLclIyPDhyM{mx
T47D  MXnGeY5kfGmxbjDBd5NigQ>? NUL3O3Y2OTBibl2= NEnQWHY1OCCq NFT5VXBld3ewcnXneYxifGW|IFXS{tEheHKxdHXpci=> MWSyNVQ5ODN7MR?=
BT474  NW\2OZI5TnWwY4Tpc44hSXO|YYm= MXixNEBvVQ>? NFWyZmI1OCCq NX;V[3BZ\G:5boLl[5Vt[XSnczDFVu6yKHC{b4TlbY4> M1HrfVIyPDhyM{mx
MCF7 MUTGeY5kfGmxbjDBd5NigQ>? Mn2zNVAxKG6P MVS3JIQ> NIS4enJz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 MlT4NlE{QTZyOUS=
T47D  NFH2Ro1HfW6ldHnvckBCe3OjeR?= MXOxNFAhdk1? MYC3JIQ> NFzXZmtz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 NH7LeFAzOTN7NkC5OC=>
BT474  Ml;RSpVv[3Srb36gRZN{[Xl? M1Tt[lExOCCwTR?= NWrHfGkxPyCm NHvhVo1z\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 MYqyNVM6PjB7NB?=
MDAMB361 MlLISpVv[3Srb36gRZN{[Xl? MoLsNVAxKG6P NXnEbnR4PyCm Mn\idoVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> MkPmNlE{QTZyOUS=
MCF7 M1HDbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjHNE4xOS1zIN88US=> NWqxZYhLPyCm NGfXWXNz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NFXzOI0zOTN7NkC5OC=>
T47D  MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7YSFljOC5yMT2xJO69VQ>? Ml7TO{Bl M4rSU5Jm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NGTLZ|czOTN7NkC5OC=>
BT474  NWX0d3d2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWwMlAyNTFizszN NVzob2lOPyCm NGfIRmNz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M124SFIyOzl4MEm0
MDAMB361 NWC5fJd1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\F[mlbOC5yMT2xJO69VQ>? NHiyS2Q4KGR? MnvQdoVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NFrl[pQzOTN7NkC5OC=>
MCF7 NFXFfGNHfW6ldHnvckBCe3OjeR?= MlHFNVAxKG6P NW\v[4FmPyCm M2HqcIlv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= NHTZSIczOTN7NkC5OC=>
T47D  M3f1cGZ2dmO2aX;uJGF{e2G7 NFK1WnEyODBibl2= NEjpZnk4KGR? M2HjRolv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= NUPlWppXOjF|OU[wPVQ>
BT474  MWDGeY5kfGmxbjDBd5NigQ>? MoSwNVAxKG6P MkGwO{Bl MoPObY5lfWOnczDv[kBGemKEMzDhcoQhTXKkQkSgdoVk\XC2b4Kg[ZhxemW|c3nvckBidmRic3nncoFtdGmwZx?= MnrmNlE{QTZyOUS=
MDAMB361 M{LPOWZ2dmO2aX;uJGF{e2G7 NYnJcIk1OTByIH7N NEDq[3E4KGR? M2jvc4lv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= NUjS[W5UOjF|OU[wPVQ>
MCF7 M2HDdmZ2dmO2aX;uJGF{e2G7 MU[xNEBvVQ>? Mn\GPVYhcA>? MXjkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb39CpC=> NWnaWmM{OjF|N{izN|M>
MDA-MB-231 NFq1WHRHfW6ldHnvckBCe3OjeR?= NWOzOoFjOTBibl2= NIPJdYQ6PiCq NYjMPJcy\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vyqB? M{Ho[VIyOzd6M{Oz
SK-BR-3 MnuwSpVv[3Srb36gRZN{[Xl? MWSxNEBvVQ>? MlWwPVYhcA>? NE\IO|Fld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc47DqA>? MmLXNlE{Pzh|M{O=
MCF-7 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSxNFAhdk1? M3i2OFczNzl4IHi= M2O1VoNifXOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MYeyNVI6QTh4Mh?=
MMQ M3jqUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTYZW9JOC5yMEitOlI2KG6P NEL4Wmo4OiCq NWW1N5l1cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lMUBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MUKyNFcxODd3NR?=
MMQ NUXuWGNqTnWwY4Tpc44hSXO|YYm= NXnaRZJKOC5yMEitOlI2KG6P NYjlbYJzPzJiaB?= MVnpcohq[mm2czDQVmwhe2WlcnX0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWfx[FBTOjB5MEC3OVU>
MMQ M3myeWZ2dmO2aX;uJGF{e2G7 NWDyR3F6OC5yND22NlUhdk1? M1G5[lczKGh? MnPwbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w Ml7MNlA4ODB5NUW=
MMQ NEfi[5dHfW6ldHnvckBCe3OjeR?= MXOwMlA1NTZ{NTDuUS=> NXrudGtpPzJiaB?= NGHCOYR2eHKnZ4XsZZRmeyCWR1dOtlMh[W6mIGTHSu6zWkmLIHX4dJJme3Orb36= M3XKXFIxPzByN{W1

... 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]
- Collapse
  • 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]
- Collapse
  • 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
Smiles CC12CCC3C(C(CCCCCCCCC[S](=O)CCCC(F)(F)C(F)(F)F)CC4=C3C=CC(=C4)O)C1CCC2O

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Mass Concentration Volume Molecular Weight

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