Fulvestrant (ICI-182780)

For research use only.

Catalog No.S1191 Synonyms: ZD 9238, ZM 182780

99 publications

Fulvestrant (ICI-182780) Chemical Structure

CAS No. 129453-61-8

Fulvestrant (ICI-182780, ZD 9238, ZM 182780) 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.

Selleck's Fulvestrant (ICI-182780) has been cited by 99 publications

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Fulvestrant (ICI-182780, ZD 9238, ZM 182780) 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 NXfXUWRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLlbVIyNjNvMUCwNEBvVQ>? NXHubpdDPDhiaB?= MWfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5OUK5OEc,OjR7N{myPVQ9N2F-
MCF-7/LTED M3npXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDMOmZ[OS5|LUGwNFAhdk1? NFHnW5o1QCCq M2\KdIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{nzV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUe5Nlk1Lz5{NEm3PVI6PDxxYU6=
HCC1428 Mo\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXXWpZkOS5|LUGwNFAhdk1? NXq2ZlBnPDhiaB?= M{PSeolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGS5Z2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3PVI6PCd-MkS5O|kzQTR:L3G+
HCC1428/LTED M1vuWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jpZ|EvOy1zMECwJI5O NFjLcnk1QCCq MXTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFHJO|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3PVI6PCd-MkS5O|kzQTR:L3G+
LCC1 NXzReIVSTnWwY4Tpc44hSXO|YYm= MluyNVAxKG6P M{C1e|Q5NTF2NDDo NXjFdphl[WO2aY\heIV{KFWSUjDzbYdv[Wyrbne= NGPtZWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi1PFI4Pyd-MkS4OVgzPzd:L3G+
LCC9 NELhRYpHfW6ldHnvckBCe3OjeR?= MVexNFAhdk1? NV3rRnVOPDhvMUS0JIg> M2HvRYFkfGm4YYTld{BWWFJic3nncoFtcW6p NF\MN|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi1PFI4Pyd-MkS4OVgzPzd:L3G+
MCF-7  NF7keZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqxNFAhdk1? NVz2VlNYPSCm MXrpcohq[mm2czDj[YxtKGe{b4f0bEB1dyBzMP-8iS=> NWTPbHgyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4NVk2PTBpPkK0PFE6PTVyPD;hQi=>
mesangial  NGi2XIxHfW6ldHnvckBCe3OjeR?= NYnPOnNYOC5zLUGwNEBvVQ>? MmjvOFghcA>? MmXLd5VxeHKnc4Pld{BVT0ZvzsKxMYlv\HWlZXSgeJlx\SCLVjDjc4xt[Wenbh?= NV;RSmpLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3PVM3OzlpPkK0O|k{PjN7PD;hQi=>
Mesangial Mn3uSpVv[3Srb36gRZN{[Xl? M1:wOVAvOS1zMECgcm0> M3fsUFAvPSCq NUPvUXEzcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJHNu[WR{IIDoc5NxcG:{eXzheIlwdiC4aXGgS3BGWg>? NXPZXoJ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3PVM3OzlpPkK0O|k{PjN7PD;hQi=>
ER+ MCF-7/2a NGjrSldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlSzTWM2OD1yLkCwOEDPxE1? NVnFUoM6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWzNlQ5QDRpPkG1N|I1QDh2PD;hQi=>
ER+ MCF-7 M1PlW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX0SHZIOjByIHi= NIrOXpBKSzVyPUCuNlEhdk1? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTN{NEi4OEc,OTV|MkS4PFQ9N2F-
MCF-7  MXvGeY5kfGmxbjDBd5NigQ>? MmH0NVDDqG6PwrC= MmPyO|IhcA>? MXPy[ZZmenOnczD0bIUh\XO2cn;n[Y4h\W[oZXP0LGlEPTBiMT65JOOYKDFy4pkSPUBOMQ>? NXj5T2htRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFg3PTJpPkK0PVA5PjV{PD;hQi=>
MCF-7  M3\wZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1mzSmlEPTEEoH;mJIFxeHKxeHntZZRmdHliMjDuUS=> NGjFRZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0PFM1Pid-MkO0OFg{PDZ:L3G+
H1975  MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXuzxsDPxE1? NWX6eWU2OSCv MX;pcoNz\WG|ZYOgeIhmKGenZnn0bY5q[iC|ZX7zbZRqfmm2eTDv[kBJOTl5NTDj[Yxte8Li NIntfnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK2PFgyOCd-MkSyOlg5OTB:L3G+
H1975 NH7wPJpHfW6ldHnvckBCe3OjeR?= MlXhN:Kh|ryP NYTrOIR3OSCv MnHFeZBz\We3bHH0[ZMhfGinIHzleoVtKG:oIFzleE04[w>? NIf2bIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK2PFgyOCd-MkSyOlg5OTB:L3G+
MCF-7  MkXNSpVv[3Srb36gRZN{[Xl? M{DDflExOOLCiX7NxsA> M1PZNFczKGh? MnTQdoV3\XK|ZYOgeIhmKHC{b4TlZ5RqfmViZX\m[YN1KG:oIFWyxsBqdiClZXzsJIlvfmG|aX;u MoPpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{[3O|MoRjJ|OUO2O|c{RC:jPh?=
MCF-7  NWeyWGN2TnWwY4Tpc44hSXO|YYm= NWjZVZBUOTBy4pEJcm3DqA>? MYOyOE81QCCq MVTmZYNqdGm2YYTld{Bqdn[jc3nvckB1cHKxdXfoJG1OWHNpIH3v[JVt[XSrb36= M3jJRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO2O|c{Lz5{M{mzOlc4OzxxYU6=
BT474-tet-shMED1 M{HYXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEKw[nQxNjFvNTFOwG0> NGTiUZM4KGR? MmPUbY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NYLJdnAyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|YzOzRpPkKzPVM3OjN2PD;hQi=>
ZR75-1-tet-shMED1  NFzhb4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDFXVM4OC5zLUWg{txO NV[2OXhzPyCm M{fTOolv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NWf0eHB[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|YzOzRpPkKzPVM3OjN2PD;hQi=>
MCF-7-tet-shMED1 NYXsSnNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPwNE4yNTVizszN Ml7UO{Bl Mki3bY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NFK0eY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzOlI{PCd-MkO5N|YzOzR:L3G+
HepG2  Ml3mSpVv[3Srb36gRZN{[Xl? NXLwfVhCOC5yMT2xNEDPxE1? MoDiNVghcMLi M2DJdYFkfGm4YYTld{B1cGViRWLFMY1m\GmjdHXkJJRz[W6|Y4LpdJRqd25ib3[gRWYzTVJ? Mn\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5M{OxPFgoRjJ|N{OzNVg5RC:jPh?=
MCF-7L  MnHnSpVv[3Srb36gRZN{[Xl? NHLuVXIyODBibl5CpC=> NF;iO|QyOCCvaX6vNlQhcC92ODDo M3X2WpJme3WudIOgbY4hTUeIUjygTGVTOiCjbnSgTGVTOyCyaH;zdIhwenmuYYTpc44h[XRicILvcI9v\2WmIHX4dI9{fXKn NIWwUVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[4OlQyPid-MkO2PFY1OTZ:L3G+
MCF-7L  M3PsXmZ2dmO2aX;uJGF{e2G7 MnmwNVAxKG6PwrC= NVTJN5BDPDhiaB?= MUjpcoR2[2W|IIXwdoVofWyjdHnvckBw\iCvUl7BJI9nKEWJRmKgcIlo[W6mIFjCMWVITg>? NFPRR3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[4OlQyPid-MkO2PFY1OTZ:L3G+
MCF-7L MmW0SpVv[3Srb36gRZN{[Xl? MUSxNFAhdk4EoB?= M3qwfVQ5KGh? MX7pcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT M{[0TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nki2OFE3Lz5{M{[4OlQyPjxxYU6=
C4-12  MVzGeY5kfGmxbjDBd5NigQ>? MV[xNFAhdk4EoB?= NWPuWHZqPDhiaB?= MX3pcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ6NkSxOkc,OjN4OE[0NVY9N2F-
MCF-7L MXPGeY5kfGmxbjDBd5NigQ>? MVuxNFAhdk4EoB?= MoHFNlQhcA>? NX;0bZR6cW6mdXPld{BGT0[UIIDoc5NxcG:{eXzheIlwdiC{ZYH1bZJm\CCKQj3FS2Yh\nWwY4Tpc44> NU\6cVdERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2PFY1OTZpPkKzOlg3PDF4PD;hQi=>
MMQ  M1O5O2Z2dmO2aX;uJGF{e2G7 MWGwMVYzPSCwTR?= MnvtO|IhcA>? M2r4O4Rwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIHXzeJJw\2WwIILlZ4VxfG:{Ld8xJEhGWs7zKR?= NED6O5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WyN|M2Pyd-MkO1NlM{PTd:L3G+
H1975  NE\kS|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2ezOVAvOzF{NT2xNEDPxE1? NX;ac4hEPiCm Mn\2bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWO4OJFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzPVk6PTdpPkKzN|k6QTV5PD;hQi=>
H1975  NEP1NYlCeG:ydH;zbZMhSXO|YYm= MmLnNlAxKG6P M13nTVczKGh? MkLO[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz NX\0VI5SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzPVk6PTdpPkKzN|k6QTV5PD;hQi=>
MCF-7  MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHsS|IyOC9zMECvNVAxOCCwTR?= NXK3bGh[Oi92L{[g[C=> MnrESG1UVw>? M3jYd4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= NF;acYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OxN|UxPid-MkOzNVM2ODZ:L3G+
MCF-7  NVrCRmtlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\PcHJkOTByIH7N NWPubJlrPCCm NWX2fY5UTE2VTx?= MVTpcoR2[2W|IHGgbIlocGW{IIDyc5BwenSrb36gc4Yh[2WubIOgbY4hfGinIFexJJBp[XOnwrC= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzNzM{WwOkc,OjN|MUO1NFY9N2F-
MLO-Y4  MWLGeY5kfGmxbjDBd5NigQ>? MVGxxsDPxE1? MYexJIg> NH\5WZhqdmirYnn0d{BGOi2rbnT1Z4VlKEO6NEOg[ZhxemW|c3nvci=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ2N{C1O{c,OjN{NEewOVc9N2F-
MCF-7 M{KwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXNe3o3OTByIH7N NX3RbYp5PDhiaB?= MXjhZpJw\2G2ZYOgeIhmKHC{b3zp[oVz[XSrdnWg[YZn\WO2IH;mJI1w\GW{YYTlJI5qfHKxc3H0bZZmKHO2cnXzdy=> MojtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{MU[3OFQoRjJ|MkG2O|Q1RC:jPh?=
TG1-1  MlzzSpVv[3Srb36gRZN{[Xl? MXGxxsDPxE1? MnrLNlQhcA>? NHzsR|Fi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKEiLRj2x{tE> M3fCTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEi4OlA4Lz5{M{C4PFYxPzxxYU6=
TG1-1  MV\GeY5kfGmxbjDBd5NigQ>? NVrmWpplOcLizszN MV2yOEBp NHLsPWxi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKFCLM1u= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB6OE[wO{c,OjNyOEi2NFc9N2F-
MCF7 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[1WlExOCCwTR?= M123SlQ5KGh? MWrs[YFleyC2bzDhJJNqdWmuYYKgcI9{eyCrbjDzeZJ3cX[jbDDhd{B4cXSqIHTvfI9zfWKrY3nuJIFtd26n MmqzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyN{eyOFkoRjJ|MEe3NlQ6RC:jPh?=
MCF7 MkfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIj2WWkyODBibl2= NIPFNng1QCCq MV\lcohidmOnczDueZRtcW5vbXXkbYF1\WRiY3XscEBl\WG2aB?= NHn5XVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C3O|I1QSd-MkOwO|czPDl:L3G+
MCF-7  NUeyWohlTnWwY4Tpc44hSXO|YYm= NGHvdYw3KGh? NGqzN3NFVVOR MnPKZZR1\W63YYTld{B1cGViZnz1[IlwgG:waXytJI9zKG[nbnjlfIFucWRvaX7keYNm\CCrbnPy[YF{\SCrbjDtbXIuOjFiZYjwdoV{e2mxbh?= NWflbYk5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwOVIxOzZpPkKzNFUzODN4PD;hQi=>
MCF-7 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXReFEyODBibl2vNUDPxE1? M4W1U|Uh\A>? MVXpcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[gNVfPui2nc4TyZYRqd2x? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl6Mke2OUc,OjJ7OEK3OlU9N2F-
MCF-7 NYPLVnNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjVNVAxKG6P MnHUOUBl MVTpcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[g[pV{[XKrZXzpckBJ M4XjbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUiyO|Y2Lz5{Mkm4Nlc3PTxxYU6=
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MCF7 MWfGeY5kfGmxbjDhd5NigQ>? M1;0fVI1KGi{cx?= M4HndWRwf25icnXneYxifGmxbjDv[kBme3S{b3flckBz\WOncITvdkBidHCqYTDlfJBz\XO|aX;uJIlvKGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTF|M{e3O{c,OTlzM{O3O|c9N2F-
MCF7 M3j5dGZ2dmO2aX;uJIF{e2G7 NXn3dFdIOTByIH7N NYTHUJBWOjRiaILz NX7hfI1ZTG:5bjDy[Yd2dGG2aX;uJI9nKGW|dILv[4VvKHKnY3XweI9zKGGucHjhJIV5eHKnc4Ppc44hcW5iaIXtZY4hVUOINzDj[YxteyCjdDCxNFAhdk1iYX\0[ZIhOjRiaILzJIJ6KGmvbYXuc4ZtfW:{ZYPj[Y5k\SC|dHHpcolv\w>? NUGxU41ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxN|M4PzdpPkG5NVM{Pzd5PD;hQi=>
MCF7:D5L MXHGeY5kfGmxbjDhd5NigQ>? MVexJJVO M1n4WGFvfGGpb37pd5Qh[WO2aY\peJkh[XRiRWLhcJBp[SCrbjDoeY1idiCPQ1[3PmQ2VCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGVTTS2mZYDlcoRmdnRibIXjbYZmemG|ZTDlfJBz\XO|aX;uJIF1KDFidV2= NUfpWlg3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4OFU{QDZpPkG5PFQ2Ozh4PD;hQi=>
HEK293 MkfSSpVv[3Srb36gZZN{[Xl? NIXRbZoyKHWP NFHkdHhCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFXSZoV1[SCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBGWkVvZHXw[Y5l\W62IHz1Z4ln\XKjc3Wg[ZhxemW|c3nvckBifCBzIIXN NUnFXZJ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4OFU{QDZpPkG5PFQ2Ozh4PD;hQi=>
Ishikawa MXHGeY5kfGmxbjDhd5NigQ>? MVqxJJVO NFPvPVNCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IHXzeJJw\2WwIILlZ4VxfG:{IHnuJIh2dWGwIFnzbIls[XejIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTVKHLXTldIVv\GWwdDDhcItidGmwZTDwbI9{eGijdHHz[UBt\X[nbIOgZZQhOSC3TR?= NVTicIp1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4OFU{QDZpPkG5PFQ2Ozh4PD;hQi=>
HeLa NIDXd|FHfW6ldHnvckBie3OjeR?= NWLqT204OSC3TR?= MUO0PEBpenN? Ml3qRY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBGWmGucHjhJIV5eHKnc4Pl[EBqdiCqdX3hckBJ\UyjIHPlcIx{KGOxZYjwdoV{e2mwZzDFVmUuTTGkLVz1Z{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIV{fHKjZHnvcE1qdmS3Y3XkJJRz[W6|Y4LpdJRqd26jbDDhZ5RqfmG2aX;uJIF1KDFidV2gZYZ1\XJiNEigbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> MlPuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4MkG0PVIoRjJyNkKxOFkzRC:jPh?=
HeLa MXnGeY5kfGmxbjDhd5NigQ>? NF3CeVUyODBibl2= M2LYZlIxKHSxIEK0JIhzew>? NFLHdlNCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFzCSEBw\iCHUnHsdIhiKHKnY3XweI9zKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgZoxw[2ujZHWgc4YhW1KFLUGgZolv\GmwZzD0c{Bz\WOncITvdkBifCBzMECgcm0h[W[2ZYKgNlAhfG9iMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> NWKwZ253RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OFg{PDZpPkKzOFQ5OzR4PD;hQi=>
MCF7 NX\rSWcxTnWwY4Tpc44h[XO|YYm= NUHmbVVCOTBibl2= NYjP[mVqPzJiaILz NH6x[XhKdmirYnn0bY9vKG:oIEG3ZoV1[S2nc4TyZYRqd2xvaX7keYNm\CCrbjDFVoFteGijIIDvd4l1cX[nIHj1cYFvKE2FRkegZ4VtdHNicILvcIln\XKjdHnvckBie3Onc4Pl[EBieyCdM1jdMZRpgW2rZHnu[UBqdmOxcoDvdoF1cW:wIHH0JFExKG6PIHHmeIVzKDd{IHjyd{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZx?= NXP3S2d2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFg3PTJpPkK0PVA5PjV{PD;hQi=>
MCF7 MlX1SpVv[3Srb36gZZN{[Xl? NWnmS4d{OSC3TR?= M1mzOVIxKGi{cx?= M4TLSWlv\HWldHnvckBw\iCnc4Tyc4dmdiC{ZXPldJRwei2jbIDoZUBl\We{YXTheIlwdiCrbjDoeY1idiCPQ1[3JINmdGy|IHH0JFEhfU1iYX\0[ZIhOjBiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh5OUS4OUc,OjV6N{m0PFU9N2F-
MCF7 NH:xXmxHfW6ldHnvckBie3OjeR?= NUeyN494OC5yMTD0c{A{ODBibl2= M1XoTFQ5KGi{cx?= NGrTeY1F\We{YXTheIlwdiCjY4Tpeol1gSCxZjDFVoFteGijIILlZ4VxfG:{IHnuJIh2dWGwIF3DSlch[2WubIOgZZQhOC5yMTD0c{A{ODBibl2gZYZ1\XJiNEigbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NHzwVJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkSwO|AyOid-Mk[0NFcxOTJ:L3G+
Neuro2a NVqyWYdnTnWwY4Tpc44h[XO|YYm= NH7NZmYyKHWP NUnpdpY2UW6qaXLpeIlwdiCxZjDEVlI1KGmwIFToZ5I4NWSnZnnjbYVvfCCvb4Xz[UBP\XW{b{LhJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKDdvRFjDJIxmfmWuczDheEAyKHWPIHL5JGxENU2VL1fDMW1UKGGwYXz5d4l{ NYXUc2J6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3PFk3PTdpPkK2O|g6PjV5PD;hQi=>
MCF-7 NWLkPIVrTnWwY4Tpc44h[XO|YYm= MV2zJI5ONCB|MDDuUUwhOzByIH7NMEA{KHWP M1TGT|I1KGi{cx?= M1TCPGRwf26{ZXf1cIF1cW:wIH;mJGVT[WyyaHGgbY4hcHWvYX6gUWNHNTdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJIV{fHKjZHnvcE1qdmS3Y3XkJGdTTUJzIH3SUmEhdGW4ZXzzJIF1KDNieDCxNEcuQSCPLDCzJJghOTBpLUigUUwhOyC6IEGwK{04KE1uIEOgfEAyOCdvNjDNJIFnfGW{IEK0JIhzeyCkeTDSWE1RS1JibXX0bI9l NHrvWlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1O|MzOCd-Mki2OVc{OjB:L3G+
MCF-7 MUPGeY5kfGmxbjDhd5NigQ>? NHzFVmE{KG6PLDCzNEBvVSxiM{CwJI5ONCB|IIXN MVmyOEBpenN? NE\rb5BFd3ewcnXneYxifGmxbjDv[kBGWmGucHjhJIlvKGi3bXHuJG1ETi15IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBme3S{YXTpc4wucW6mdXPl[EBR\1JibWLORUBt\X[nbIOgZZQhOyC6IEGwK{06KE1uIEOgfEAyOCdvODDNMEA{KHhiMUCnMVchVSxiMzD4JFExLy14IF2gZYZ1\XJiMkSgbJJ{KGK7IGLUMXBEWiCvZYToc4Q> NEn6cnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1O|MzOCd-Mki2OVc{OjB:L3G+
MCF-7 NXW0dlM5TnWwY4Tpc44h[XO|YYm= M1\UZ|Mhdk1uIEOwJI5ONCB|MECgcm0tKDNidV2= NHjjWWozPCCqcoO= MkfTSI94dnKnZ4XsZZRqd25ib3[gSXJidHCqYTDpckBpfW2jbjDNR2YuPyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[g[ZN1emGmaX;sMYlv\HWlZXSgdHMzKG2UTlGgcIV3\Wy|IHH0JFMhgCBzMDetPUBONCB|IIigNVAoNThiTTygN{B5KDFyJz23JG0tKDNieDCxNEcuPiCPIHHmeIVzKDJ2IHjyd{BjgSCUVD3QR3IhdWW2aH;k MnzkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4NUezNlAoRjJ6NkW3N|IxRC:jPh?=
MCF7 NF7qbXNHfW6ldHnvckBie3OjeR?= NV:2VXVUOTBidV2= M{fVeFI1KGi{cx?= M3S3XWlv\HWldHnvckBw\iC|ZXzlZ5RqfmViZYP0do9o\W5icnXj[ZB1d3JiYXzwbIEh\GWpcnHkZZRqd25iaX6gbJVu[W5iTVPGO{Bk\WyuczDheEAyOCC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NX;rSWx7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1OlI4OzdpPkK5OVYzPzN5PD;hQi=>

... 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]
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  • 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]
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  • 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)
Water Insoluble
Ethanol ''100 mg/mL warmed
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 ZD 9238, ZM 182780
Smiles CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05022342 Not yet recruiting Other: alpelisib plus fulvestrant Breast Cancer Novartis Pharmaceuticals|Novartis September 15 2021 --
NCT04762979 Recruiting Drug: Alpelisib|Drug: Fulvestrant|Drug: Aromatase inhibitor Hormone Receptor Positive Breast Carcinoma|HER2-negative Breast Cancer|PIK3CA Mutant Metastatic Breast Cancer Amanda Parkes|Novartis|University of Wisconsin Madison|Big Ten Cancer Research Consortium February 12 2021 Phase 2
NCT04567420 Recruiting Drug: Palbociclib|Drug: Fulvestrant|Drug: Adjuvant Therapy Breast Cancer Criterium Inc. February 9 2021 Phase 2
NCT04544189 Recruiting Drug: Alpelisib|Drug: Fulvestrant|Drug: Placebo Breast Neoplasms Novartis Pharmaceuticals|Novartis January 20 2021 Phase 2
NCT04524000 Recruiting Drug: Alpelisib|Drug: Fulvestrant Advanced Breast Cancer Novartis Pharmaceuticals|Novartis November 20 2020 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