Fulvestrant

For research use only.

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

86 publications

Fulvestrant Chemical Structure

CAS No. 129453-61-8

Fulvestrant (ICI-182780, ZD 9238) is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.

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Selleck's Fulvestrant has been cited by 86 publications

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Fulvestrant (ICI-182780, ZD 9238) is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.
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 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7ObnZ3OS5|LUGwNFAhdk1? MWi0PEBp NVLTWIY6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M{n1dFI1QTd7Mkm0
MCF-7/LTED NXvl[4d5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1y0flEvOy1zMECwJI5O MlH0OFghcA>? NYXz[YZVcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXLhPGRWOjR7N{myPVQ>
HCC1428 M3PqUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HoUFEvOy1zMECwJI5O NVTodZhzPDhiaB?= NGHnXZRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXzvdmhWOjR7N{myPVQ>
HCC1428/LTED M4HRfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTlOHFqOS5|LUGwNFAhdk1? NXHsZ29oPDhiaB?= NXTXNo1NcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYn1UJVoOjR7N{myPVQ>
LCC1 Mlq3SpVv[3Srb36gRZN{[Xl? NYTaTpFDOTByIH7N NUTTOYhoPDhvMUS0JIg> M4KzW4FkfGm4YYTld{BWWFJic3nncoFtcW6p M2faXVI1QDV6Mke3
LCC9 MnTTSpVv[3Srb36gRZN{[Xl? MXGxNFAhdk1? MnrnOFguOTR2IHi= NEnofo1i[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= MYiyOFg2QDJ5Nx?=
MCF-7  MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXKxNFAhdk1? MVi1JIQ> Ml20bY5pcWKrdIOgZ4VtdCCpcn;3eIghfG9iMUFvwKU> NUPBPXFEOjR6MUm1OVA>
mesangial  NWT2b3QxTnWwY4Tpc44hSXO|YYm= M3r6d|AvOS1zMECgcm0> Mk\wOFghcA>? M{nDVpN2eHC{ZYPz[ZMhXEeILd8yNU1qdmS3Y3XkJJR6eGViSW[gZ49tdGGpZX6= M4jWXVI1Pzl|NkO5
Mesangial M3zQTGZ2dmO2aX;uJGF{e2G7 NIftTXExNjFvMUCwJI5O NILaTogxNjViaB?= MWHpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRiU33h[FIheGixc4Doc5J6dGG2aX;uJJZq[SCJUFXS M1PpbVI1Pzl|NkO5
ER+ MCF-7/2a MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XVZWlEPTB;MD6wNFQh|ryP MW[xOVMzPDh6NB?=
ER+ MCF-7 MmDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfNVXRiOjByIHi= M3zjWmlEPTB;MD6yNUBvVQ>? NX;UbZRROTV|MkS4PFQ>
MCF-7  NHfOZ21HfW6ldHnvckBCe3OjeR?= M4fhWVExyqCwTdMg MXu3NkBp NUT3NGNWemW4ZYLz[ZMhfGinIHXzeJJw\2WwIHXm[oVkfCiLQ{WwJFEvQSEFlzCxNQKJmjliTTm= NH2yfVUzPDlyOE[1Ni=>
MCF-7  M{C4UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnsc3pKSzVywrDv[kBieHC{b4jpcYF1\Wy7IEKgcm0> NXPmVHF2OjN2NEizOFY>
H1975  MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDlXZFEO8LizszN NIHEe2IyKG1? M1SycYlv[3KnYYPld{B1cGViZ3XmbZRqdmmkIIPlcpNqfGm4aYT5JI9nKEhzOUe1JINmdGy|wrC= NIizUJQzPDJ4OEixNC=>
H1975 NVLaUGx3TnWwY4Tpc44hSXO|YYm= NEnqfmY{yqEQvF2= NXrGNFNtOSCv NVjnS4E4fXC{ZXf1cIF1\XNidHjlJIxmfmWuIH;mJGxmfC15Yx?= NHvjTVkzPDJ4OEixNC=>
MCF-7  MXnGeY5kfGmxbjDBd5NigQ>? NFrzRoYyODEkgJnuUeKh NFP6TYQ4OiCq M1jkepJmfmW{c3XzJJRp\SCycn;0[YN1cX[nIHXm[oVkfCCxZjDFNuKhcW5iY3XscEBqdn[jc3nvci=> MnTjNlM6OzZ5N{O=
MCF-7  NVr4T3Q1TnWwY4Tpc44hSXO|YYm= MkWwNVAx6oDLbl5CpC=> MXqyOE81QCCq NFeyflBn[WOrbHn0ZZRmeyCrbo\hd4lwdiC2aILveYdpKE2PUIOnJI1w\HWuYYTpc44> NIrBfnYzOzl|Nke3Ny=>
BT474-tet-shMED1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7vdo0xNjFvNTFOwG0> MWK3JIQ> M4HJSIlv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MVeyN|k{PjJ|NB?=
ZR75-1-tet-shMED1  NHrmfVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF34bmMxNjFvNTFOwG0> NXjnTZFmPyCm NXXCXG1lcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NXLVdFlbOjN7M{[yN|Q>
MCF-7-tet-shMED1 M{DINmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\RN|AvOS13IN88US=> MlSxO{Bl NVfH[4V{cW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MkPJNlM6OzZ{M{S=
HepG2  MUXGeY5kfGmxbjDBd5NigQ>? M2PFW|AvODFvMUCg{txO MYCxPEBpyqB? M2S3cIFkfGm4YYTld{B1cGViRWLFMY1m\GmjdHXkJJRz[W6|Y4LpdJRqd25ib3[gRWYzTVJ? NGLsdVUzOzd|M{G4PC=>
MCF-7L  MUHGeY5kfGmxbjDBd5NigQ>? NHHNPYEyODBibl5CpC=> NVGwUHJOOTBibXnuM|I1KGhxNEigbC=> NVvmXoJxemW|dXz0d{BqdiCHR1\SMEBJTVJ{IHHu[EBJTVJ|IIDoc5NxcG:{eXzheIlwdiCjdDDwdo9td26pZXSg[Zhxd3O3cnW= M17BT|I{Pjh4NEG2
MCF-7L  M1O4TWZ2dmO2aX;uJGF{e2G7 NYDRSJp{OTByIH7NxsA> Mli1OFghcA>? M2DoRYlv\HWlZYOgeZBz\We3bHH0bY9vKG:oIH3SUmEhd2ZiRVfGVkBtcWejbnSgTGIuTUeI NHP6ZogzOzZ6NkSxOi=>
MCF-7L M3nrTGZ2dmO2aX;uJGF{e2G7 Mnm2NVAxKG6PwrC= MYO0PEBp M2CzZYlv\HWlZYOgSWdHWiCoYX3pcJkhdWWvYnXyJIFkfGm4YYTpc44hemWzdXny[YQhTVJ? M1qzO|I{Pjh4NEG2
C4-12  M1S4V2Z2dmO2aX;uJGF{e2G7 MYqxNFAhdk4EoB?= MXm0PEBp NVzuW242cW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= M2HCfFI{Pjh4NEG2
MCF-7L MUHGeY5kfGmxbjDBd5NigQ>? M1XQc|ExOCCwTdMg M1\Y[lI1KGh? MXLpcoR2[2W|IFXHSnIheGixc4Doc5J6dGG2aX;uJJJmeXWrcnXkJGhDNUWJRjDmeY5kfGmxbh?= M1jsZVI{Pjh4NEG2
MMQ  NU\C[ndKTnWwY4Tpc44hSXO|YYm= NGrwNmoxNTZ{NTDuUS=> NVjsNGNrPzJiaB?= MXPkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCnc4Tyc4dmdiC{ZXPldJRwei4QsTCoSXLPuSl? NXLJPINYOjN3MkOzOVc>
H1975  NHrqXWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKwMlMyOjVvMUCg{txO MWK2JIQ> M3jmPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4iw[|I{Ozl7OUW3
H1975  MmL6RZBweHSxc3nzJGF{e2G7 MWeyNFAhdk1? NVy2eHdWPzJiaB?= MlLF[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz NU\ZeZBCOjN|OUm5OVc>
MCF-7  M2TGbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLiNVAwOTByL{GwNFAhdk1? NWn4c4s{Oi92L{[g[C=> NI\PZmdFVVOR M4LIbYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= MkmyNlM{OTN3ME[=
MCF-7  MkLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXexNFAhdk1? M{j2SlQh\A>? NXTGT3NETE2VTx?= NVHyfXBHcW6mdXPld{BiKGirZ3jldkBxem:yb4L0bY9vKG:oIHPlcIx{KGmwIITo[UBIOSCyaHHz[eKh M3zid|I{OzF|NUC2
MLO-Y4  MUfGeY5kfGmxbjDBd5NigQ>? MkjINeKh|ryP M4nrPVEhcA>? MnznbY5pcWKrdIOgSVIucW6mdXPl[EBEgDR|IHX4dJJme3Orb36= NIDZUHIzOzJ2N{C1Oy=>
MCF-7 NFO5b5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGxNFAhdk1? MYq0PEBp MYPhZpJw\2G2ZYOgeIhmKHC{b3zp[oVz[XSrdnWg[YZn\WO2IH;mJI1w\GW{YYTlJI5qfHKxc3H0bZZmKHO2cnXzdy=> NUHVeGhlOjN{MU[3OFQ>
TG1-1  NEXBWpNHfW6ldHnvckBCe3OjeR?= MkntNeKh|ryP MmizNlQhcA>? MmH1ZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x NWnReWp4OjNyOEi2NFc>
TG1-1  M1nk[WZ2dmO2aX;uJGF{e2G7 NWjDemRoOcLizszN NVzsWW1ROjRiaB?= MmDmZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBRUTON MXOyN|A5QDZyNx?=
MCF7 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[xNFAhdk1? Ml\3OFghcA>? NUH3eW1[dGWjZIOgeI8h[SC|aX3pcIFzKGyxc4OgbY4he3W{dnn2ZYwh[XNid3n0bEBld3ixcoXibYNqdiCjbH;u[S=> MYGyN|A4PzJ2OR?=
MCF7 MnPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjXeZNyOTByIH7N Moj2OFghcA>? NGLZ[mhmdmijbnPld{BvfXSuaX6tcYVlcWG2ZXSgZ4VtdCCmZXH0bC=> MoDwNlMxPzd{NEm=
MCF-7  M1m2VmZ2dmO2aX;uJGF{e2G7 NGPWdWo3KGh? NWLwb4RKTE2VTx?= NXfDWIZ1[XS2ZX71ZZRmeyC2aHWg[ox2\GmxeH;ubYwuKG:{IH\lcohmgGGvaXStbY5lfWOnZDDpcoNz\WG|ZTDpckBucVJvMkGg[ZhxemW|c3nvci=> MWmyN|A2OjB|Nh?=
MCF-7 NHvse4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLxRZV[OTByIH7NM|Eh|ryP M3nkVFUh\A>? NYfDUnBXcW6qaXLpeJMhfGinIIP0bY12dGG2aX;uJI9nKDF5zsKt[ZN1emGmaX;s M4fDbVIzQTh{N{[1
MCF-7 M3\kcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOxNFAhdk1? NYLzSXVsPSCm NWnUcXNmcW6qaXLpeJMhfGinIIP0bY12dGG2aX;uJI9nKG[3c3HybYVtcW5iSB?= M4T1WVIzQTh{N{[1
1471.1 NHfNU5RHfW6ldHnvckBCe3OjeR?= NXTabHhkOTByIH7N NGLjbmoyKGh? NGDXNoFGfE:KwrC= M3XLcJRic2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> NHTzO|EzOjh4OUGwOi=>
MCF-7 NHu1O5JHfW6ldHnvckBCe3OjeR?= NYTEdmRFOTByIH7N MnG4NUBp MYnFeG9JyqB? MV30ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= NXTHUXgzOjJ6NkmxNFY>
HeLa MoKySpVv[3Srb36gRZN{[Xl? NWjjcFNTOTByIH7N MX2xJIg> M4TUfWV1V0kEoB?= MV;0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= MmPINlI5PjlzME[=
COS-7  NE\ud2RHfW6ldHnvckBCe3OjeR?= M1zvclExOCCwTR?= NFHVd|kyKGh? NXnlWHV6TXSRSNMg MYr0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= MUKyNlg3QTFyNh?=
BG1L-OHTLT  NUnIdpNETnWwY4Tpc44hSXO|YYm= MXKxNOKhdk1? MnLVNlTDqGkEoB?= MoXybY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w M2e1UFIzPjV{NUW4
BG1L-ICILT M4DVN2Z2dmO2aX;uJGF{e2G7 NHzm[okyOMLibl2= NYDuZoFOOjUEoHlCpC=> NUDOfWRNcW6qaXLpeJMhTVMQsTDlfJBz\XO|aX;u NXi3WlB4OjJ4NUK1OVg>
PC-9 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TCXVAvODB|LUOwJO69VQ>? NGXaVWo1QCCq MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mn3LNlI2PjB4M{S=
H1650 M37rcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPhTnQxNjByMz2zNEDPxE1? NIP3doU1QCCq NVTISnRWcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4qzfVIzPTZyNkO0
H1975 NXXNVIN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PrblAvODB|LUOwJO69VQ>? NWrjUWJ1PDhiaB?= M4H6XolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXSyNlU3ODZ|NB?=
H1975 NWPkS2J7TnWwY4Tpc44hSXO|YYm= NFnlWJU{yqEQvF2= M1nQXFMhcA>? NVnyXmtV[WK{b3fheIV{KHSqZTDwbI9{eGixLVXHSnIhcW6mdXP0bY9vKGK7IHXzeJJw\2Ww M1zGXFIzPTZyNkO0
H1975 MnPpSpVv[3Srb36gRZN{[Xl? MV2zxsDPxE1? Ml62O{Bl MlznbY5lfWOnczDFS2ZTKGW6cILld5Nqd25? MmXUNlI2PjB4M{S=
HTR-8 Ml3ySpVv[3Srb36gRZN{[Xl? Ml23NeKh|ryP NXT1fJhqOS12ODDo NEi5VHJld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDJS2ZDWDdibWLORS=> M363[|IzOzh|MUGx
JEG-3 M1;HdGZ2dmO2aX;uJGF{e2G7 M2[0blHDqM7:TR?= MUmxMVQ5KGh? NE\kdVRld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDJS2ZDWDdibWLORS=> MnH0NlI{QDNzMUG=
Huh7 NGHRZmxHfW6ldHnvckBCe3OjeR?= NGHXVJM2OMLizszN NWPrO20zPDhiaB?= MmjvbY5pcWKrdIOg[4VvcXO2ZXnuMY1m\GmjdHXkJHBQVjFidILhcpNi[3SrdnH0bY9v NVfCe4E2OjJ|MESyPVY>
201T NVTNZ2o{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV61JO69VQ>? MX:3NkBp M1\kWolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4YX7k[ZRidmmk NIDQO48zOjJ3OES3Oi=>
A549  NF\m[YRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVi1JO69VQ>? M2HPe|czKGh? NHHo[4NqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnHu[IV1[W6rYh?= NV22T41nOjJ{NUi0O|Y>
MCF-7 MmfsSpVv[3Srb36gRZN{[Xl? M3fJVVHDqM7:TR?= NF7FV5AzPCCqwrC= M{TiNoRwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvckBqdmS3Y3XkJIJ6KDRvT1itWEDDqA>? NX;rcmdVOjJyNEmzNVY>
HCC-1428 M{nSNmZ2dmO2aX;uJGF{e2G7 NITFXIMyyqEQvF2= M1nL[|I1KGkEoB?= NXjCZ4RQ\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi Mn7iNlIxPDl|MU[=
MDA-361 M1PjdGZ2dmO2aX;uJGF{e2G7 MVyxxsDPxE1? NHLre40zPCCqwrC= M{XRdYRwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvckBqdmS3Y3XkJIJ6KDRvT1itWEDDqA>? NFXhPZUzOjB2OUOxOi=>
ZR75-1 NH\pdVRHfW6ldHnvckBCe3OjeR?= NHvwSpQyyqEQvF2= MUeyOEBpyqB? NFThOlFld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? MYqyNlA1QTNzNh?=
MCF-7 NV7nSFVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlv2NeKh|ryP MmDtOU0yOCCm MlPyd5VxeHKnc4Pld{BGOi2rbnT1Z4VlKGe{b4f0bEBqdmirYnn0bY9v NFXlRmQzOjB2OUOxOi=>
HCC-1428 M3fKUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jre|HDqM7:TR?= MoXtOU0yOCCm NWjUSGZXe3WycILld5NmeyCHMj3pcoR2[2WmIHfyc5d1cCCrbnjpZol1cW:w MoO1NlIxPDl|MU[=
MDA-361 M4\QeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4L4ZVHDqM7:TR?= NEXD[lA2NTFyIHS= MXrzeZBxemW|c3XzJGUzNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> NXHxbnRZOjJyNEmzNVY>
ZR75-1 NVTHUHFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHMNeKh|ryP NWnLTGRGPS1zMDDk M3OybJN2eHC{ZYPz[ZMhTTJvaX7keYNm\CCpcn;3eIghcW6qaXLpeIlwdg>? MnLvNlIxPDl|MU[=
MCF-7/AC-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVuwMVAvOiEQvF2= MUi2JIQ> Mnj1bY5pcWKrdIOgZ4VtdCCpcn;3eIghdW:mZYP0cJk> NV\ubpplOjJyNEK3PVI>
MCF7 NIruSZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XGVlExKML3TR?= MnryOFghcA>? MXzpcoR2[2W|IHPlcIwhcW6qaXLpeIlwdiC5aHnjbEBk[W5iYnWg[Y5p[W6lZXSgZpkh\mmkcn;icIF{fHN? M{jreFIzODRzOEi3
MMQ M3;HSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H4bFAuPjJ3IH7N NVHFb|hkPzJiaB?= NU\obYtIeHKxZIXj[ZMhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbtMg MXqyNlAyPTFyMR?=
MMQ NFPRSHZHfW6ldHnvckBCe3OjeR?= Mo\0NE03OjVibl2= MYS3NkBp MWPwdo9lfWOnczDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSsJIRwe2VvZHXw[Y5l\W62IILl[JVkfGmxbjDpckBRWkxic3XjdoV1cW:w M2TSSlIzODF3MUCx
MCF7 M3vrWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4T4XVAuOSEQvF2= Mk\INlQuOTJyIHi= M3PpT4lvcGmkaYTzJJRp\SCpcn;3eIghd2ZiTVPGO{1[Si1zwrC= NWW3PFZjOjF6NkOyOVg>
HepG2 MlPJRZBweHSxc3nzJGF{e2G7 MknkNE4yyqEQvF2= M{jKfVI1KGh? MUDhZo9tcXOqZYOgeIhmKGW|dILv[4VvNWmwZIXj[YQhfXBvcnXneYxifGmxbjDv[kBieG:DSTDhcoQh[XCxTR?= M3ziTFIyQDF4MkOz
MCF7–iFR3 NGqxb|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWyNE0yODBibl2= NVHhTIJyQTZiaB?= Mn;Q[Y5p[W6lZYOgRXAucW6mdXPl[EBk\WyuIHfyc5d1cCCrbnjpZol1cW:w NVK2XmNTOjF5OUK4PFk>
MCF7S NFO2OotHfW6ldHnvckBCe3OjeR?= M{jCVlHDqM7:TR?= MYq0PEBp NYP1bJR5\G:5boLl[5Vt[XSnczDveoVz[WyuIFXS{tEheHKxdHXpckBt\X[nbIO= NVvQTVJHOjF3M{OxPVU>
MCF7 MofLSpVv[3Srb36gRZN{[Xl? MYixxsDPxE1? MUi0PEBp NFXWNFNld3ewcnXneYxifGW|IH;2[ZJidGxiRWNOtUBxem:2ZXnuJIxmfmWucx?= Mmn2NlE2OzNzOUW=
MCF7S M2rsOGZ2dmO2aX;uJGF{e2G7 NFT0W2QyyqEQvF2= Mor4O{Bl M1;4XoF1fGWwdXH0[ZMhfHWvb4LzdIhmemViZn;ycYF1cW:wIHHu[EBxem:uaX\ldoF1cW:w M3vPcVIyPTN|MUm1
MCF7S MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DjVVAvPS9zIN88US=> NEnGZXU4KGR? MW\EUXNQ M1O3WYRm[3KnYYPld{Bk\WyuIHX4dIFve2mxbh?= NGjnRoozOTV|M{G5OS=>
T47D  M{DJT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\sNVQhdk1? NV\obmdoPDBiaB?= MY\zeZBxemW|c3XzJINmdGxiZ4Lve5RpKG2xZHXyZZRmdHl? NYLCWmU3OjF2OECzPVE>
BT474  NXzRR5cxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIj1fpI1KG6P M3[yVlQxKGh? NUX2ZpVme3WycILld5NmeyClZXzsJIdzd3e2aDDtc4RmemG2ZXz5 M1\3PVIyPDhyM{mx
T47D  MYPGeY5kfGmxbjDBd5NigQ>? M1XrWFExKG6P MUm0NEBp NI[0Vmhld3ewcnXneYxifGW|IFXS{tEheHKxdHXpci=> NFHrdY0zOTR6MEO5NS=>
BT474  M2nibGZ2dmO2aX;uJGF{e2G7 NX\oOJFoOTBibl2= NIfxUIs1OCCq NWTmPGxr\G:5boLl[5Vt[XSnczDFVu6yKHC{b4TlbY4> MoLENlE1QDB|OUG=
MCF7 Mo\PSpVv[3Srb36gRZN{[Xl? NUjydnFmOTByIH7N MnPaO{Bl NXf3dHZ5emWmdXPld{BGWs7zIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? NWLFfWhTOjF|OU[wPVQ>
T47D  MmLtSpVv[3Srb36gRZN{[Xl? MVSxNFAhdk1? MnOzO{Bl M2X5c5Jm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> M2DEdVIyOzl4MEm0
BT474  NGHXdm9HfW6ldHnvckBCe3OjeR?= M{LtVVExOCCwTR?= M1;HbVch\A>? MX;y[YR2[2W|IFXS{tEh\XiycnXzd4lwdiC|aXfubYZq[2GwdHz5 M3O2blIyOzl4MEm0
MDAMB361 NUmwem54TnWwY4Tpc44hSXO|YYm= NWfZVJh5OTByIH7N Mn23O{Bl NETQV4tz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 NF3ZVnMzOTN7NkC5OC=>
MCF7 NGnQOW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvJR5gxNjBzLUGg{txO NEjUWJI4KGR? MmLUdoVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NE\oenkzOTN7NkC5OC=>
T47D  NUHyfHJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOwMlAyNTFizszN NF\wd2E4KGR? M3v5V5Jm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NUG0SWl4OjF|OU[wPVQ>
BT474  M4TPZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DGT|AvODFvMTFOwG0> NVjPeHY6PyCm MYPy[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? NFz5dogzOTN7NkC5OC=>
MDAMB361 M1vzXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLCPFcxNjBzLUGg{txO NFnqU|M4KGR? M{WwdZJm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MmWzNlE{QTZyOUS=
MCF7 MnTYSpVv[3Srb36gRZN{[Xl? NFLONo0yODBibl2= NI\ve4Q4KGR? Ml36bY5lfWOnczDv[kBGemKEMzDhcoQhTXKkQkSgdoVk\XC2b4Kg[ZhxemW|c3nvckBidmRic3nncoFtdGmwZx?= NH\TdnEzOTN7NkC5OC=>
T47D  NV7mcW9HTnWwY4Tpc44hSXO|YYm= NWrBT|EzOTByIH7N NHnpZ2s4KGR? MoLjbY5lfWOnczDv[kBGemKEMzDhcoQhTXKkQkSgdoVk\XC2b4Kg[ZhxemW|c3nvckBidmRic3nncoFtdGmwZx?= MX:yNVM6PjB7NB?=
BT474  NHr4OnVHfW6ldHnvckBCe3OjeR?= MmWyNVAxKG6P NWTCe|B5PyCm M3HaUolv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= M{i1WVIyOzl4MEm0
MDAMB361 MWnGeY5kfGmxbjDBd5NigQ>? NVvh[5E3OTByIH7N MoD5O{Bl NWDVRmdLcW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=> Mm\ONlE{QTZyOUS=
MCF7 M2rzbGZ2dmO2aX;uJGF{e2G7 NXjJUXhYOTBibl2= M{jQcFk3KGh? NGHvOYtld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc47DqA>? NF3uPFQzOTN5OEOzNy=>
MDA-MB-231 MYTGeY5kfGmxbjDBd5NigQ>? MYKxNEBvVQ>? NYjsRnVRQTZiaB?= NYT0OHpw\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vyqB? MXSyNVM4QDN|Mx?=
SK-BR-3 NVPrfWhRTnWwY4Tpc44hSXO|YYm= M3;C[lExKG6P M3\hN|k3KGh? MkTS[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uxsA> NYLvbFNbOjF|N{izN|M>
MCF-7 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWixNFAhdk1? MX[3Nk86PiCq NHuw[Ihk[XW|ZYOgZ4VtdCCleXPs[UBienKnc4S= M33WXFIyOjl7OE[y
MMQ NEKwUIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELzPXcxNjByOD22NlUhdk1? M{W2[FczKGh? M2XQXYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZT2gZY5lKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NVnTO21QOjB5MEC3OVU>
MMQ MY\GeY5kfGmxbjDBd5NigQ>? NVnlclVROC5yMEitOlI2KG6P MVW3NkBp NIXJV5VqdmirYnn0d{BRWkxic3XjdoV1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M1LjUVIxPzByN{W1
MMQ NHvLSHFHfW6ldHnvckBCe3OjeR?= NFzKUngxNjB2LU[yOUBvVQ>? NE\Lfmw4OiCq MoLBbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w MmnwNlA4ODB5NUW=
MMQ NGjveWVHfW6ldHnvckBCe3OjeR?= NIDS[nAxNjB2LU[yOUBvVQ>? Mk\CO|IhcA>? MWf1dJJm\3WuYYTld{BVT0cQskOgZY5lKFSJRt8yVmlKKGW6cILld5Nqd25? NFHRNo8zODdyMEe1OS=>

... 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
  • 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(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F

In vivo Formulation Calculator (Clear solution)

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Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04524000 Not yet recruiting Drug: Alpelisib|Drug: Fulvestrant Advanced Breast Cancer Novartis Pharmaceuticals|Novartis October 1 2020 Phase 2
NCT04483505 Not yet recruiting Drug: Combination Rogaratinib + palbociclib + fulvestrant Breast Cancer Metastatic|Hormone Receptor Positive Malignant Neoplasm of Breast Fundacion CRIS de Investigación para Vencer el Cáncer|Bayer|Pfizer|Apices Soluciones S.L. October 1 2020 Phase 1
NCT04300790 Not yet recruiting Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant Breast Cancer MedSIR|Novartis June 30 2020 Phase 2
NCT04024436 Recruiting Drug: TAS-120|Drug: Fulvestrant Metastatic Breast Cancer|FGFR2 Amplification Taiho Oncology Inc. December 15 2019 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