Fulvestrant

For research use only.

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

90 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 90 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 NW\GXJROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fXN|EvOy1zMECwJI5O NVmzNotkPDhiaB?= MX;pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXn3Uot{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O|kzQTRpPkK0PVc6Ojl2PD;hQi=>
MCF-7/LTED NH\R[JdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCxMlMuOTByMDDuUS=> MXK0PEBp NEXNbZpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MmSzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{myPVQoRjJ2OUe5Nlk1RC:jPh?=
HCC1428 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2Dsc|EvOy1zMECwJI5O NEXCPVE1QCCq NEn6[phqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M2nKelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUe5Nlk1Lz5{NEm3PVI6PDxxYU6=
HCC1428/LTED NFLZPXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofBNU4{NTFyMECgcm0> NVT0d2JvPDhiaB?= NXTSW|U5cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{myPVQoRjJ2OUe5Nlk1RC:jPh?=
LCC1 M1GwV2Z2dmO2aX;uJGF{e2G7 NFf1WIUyODBibl2= NUXqc|BqPDhvMUS0JIg> NF3YN5Fi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= NV\NUJFoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OVgzPzdpPkK0PFU5Ojd5PD;hQi=>
LCC9 NETTWGJHfW6ldHnvckBCe3OjeR?= NUK5e4Z7OTByIH7N NXnrbpdMPDhvMUS0JIg> Mo\3ZYN1cX[jdHXzJHVRWiC|aXfuZYxqdmd? M4fqVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEW4Nlc4Lz5{NEi1PFI4PzxxYU6=
MCF-7  M3;hPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvUTY1XOTByIH7N M{jXdVUh\A>? MYTpcohq[mm2czDj[YxtKGe{b4f0bEB1dyBzMP-8iS=> MkGxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6MUm1OVAoRjJ2OEG5OVUxRC:jPh?=
mesangial  MnHZSpVv[3Srb36gRZN{[Xl? MkDzNE4yNTFyMDDuUS=> NYHIUZY6PDhiaB?= MYPzeZBxemW|c3XzJHRITi4QskGtbY5lfWOnZDD0fZBmKEmYIHPvcIxi\2Ww MlHTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5OUO2N|koRjJ2N{mzOlM6RC:jPh?=
Mesangial NGC5T2JHfW6ldHnvckBCe3OjeR?= NGjjdWUxNjFvMUCwJI5O NX;XOItbOC53IHi= MVnpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRiU33h[FIheGixc4Doc5J6dGG2aX;uJJZq[SCJUFXS MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd7M{[zPUc,OjR5OUO2N|k9N2F-
ER+ MCF-7/2a M{j1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi1VY5KSzVyPUCuNFA1KM7:TR?= NGfSNY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUOyOFg5PCd-MUWzNlQ5QDR:L3G+
ER+ MCF-7 NW\GfGdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PTNlIxOCCq Moq0TWM2OD1yLkKxJI5O NIewO|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUOyOFg5PCd-MUWzNlQ5QDR:L3G+
MCF-7  NGPCXYNHfW6ldHnvckBCe3OjeR?= NXzJfHRmOTEEoH7NxsA> Ml3XO|IhcA>? NXnMTG1QemW4ZYLz[ZMhfGinIHXzeJJw\2WwIHXm[oVkfCiLQ{WwJFEvQSEFlzCxNQKJmjliTTm= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyOE[1Nkc,OjR7MEi2OVI9N2F-
MCF-7  M13sOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MomzTWM2OMLib3[gZZBxem:6aX3heIVtgSB{IH7N MnXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEizOFYoRjJ|NES4N|Q3RC:jPh?=
H1975  Mm\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLCN4I{yqEQvF2= MofyNUBu MknybY5kemWjc3XzJJRp\SCpZX\peIlvcWJic3Xud4l1cX[rdImgc4YhUDF7N{WgZ4VtdHQEoB?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ4OEixNEc,OjR{Nki4NVA9N2F-
H1975 M2G5ZmZ2dmO2aX;uJGF{e2G7 NUOzeoRGO8LizszN MmGxNUBu M2nzUZVxemWpdXzheIV{KHSqZTDs[ZZmdCCxZjDM[ZQuP2N? NVnBPVNzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOlg5OTBpPkK0NlY5QDFyPD;hQi=>
MCF-7  NHHKS4tHfW6ldHnvckBCe3OjeR?= NGTrblkyODEkgJnuUeKh NH;jVFM4OiCq NG\WTWZz\X[ncoPld{B1cGVicILveIVkfGm4ZTDl[oZm[3Rib3[gSVLDqGmwIHPlcIwhcW64YYPpc44> NWTHeIl3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|Y4PzNpPkKzPVM3Pzd|PD;hQi=>
MCF-7  NFflT2VHfW6ldHnvckBCe3OjeR?= MojRNVAx6oDLbl5CpC=> NYTmcWNnOjRxNEigbC=> MXnmZYNqdGm2YYTld{Bqdn[jc3nvckB1cHKxdXfoJG1OWHNpIH3v[JVt[XSrb36= MnnnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{[3O|MoRjJ|OUO2O|c{RC:jPh?=
BT474-tet-shMED1 M3y2OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\5elAvOS13IN88US=> MojCO{Bl MlTlbY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MkTmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{[yN|QoRjJ|OUO2NlM1RC:jPh?=
ZR75-1-tet-shMED1  M4nEWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkf0NE4yNTVizszN NXrr[YFKPyCm M17DTYlv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NEfpSpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzOlI{PCd-MkO5N|YzOzR:L3G+
MCF-7-tet-shMED1 NUfvZWpDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\hOFAvOS13IN88US=> NGjZUFg4KGR? NF;Mc2lqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M3LFdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO2NlM1Lz5{M{mzOlI{PDxxYU6=
HepG2  MV7GeY5kfGmxbjDBd5NigQ>? NXftbnpzOC5yMT2xNEDPxE1? M1;LelE5KGkEoB?= M{XS[oFkfGm4YYTld{B1cGViRWLFMY1m\GmjdHXkJJRz[W6|Y4LpdJRqd25ib3[gRWYzTVJ? M3;UUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{OzNVg5Lz5{M{ezN|E5QDxxYU6=
MCF-7L  NWrMbJRZTnWwY4Tpc44hSXO|YYm= NFr3dpEyODBibl5CpC=> Mli2NVAhdWmwL{K0JIgwPDhiaB?= M13mbJJme3WudIOgbY4hTUeIUjygTGVTOiCjbnSgTGVTOyCyaH;zdIhwenmuYYTpc44h[XRicILvcI9v\2WmIHX4dI9{fXKn NHvQVok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[4OlQyPid-MkO2PFY1OTZ:L3G+
MCF-7L  MlyxSpVv[3Srb36gRZN{[Xl? MXuxNFAhdk4EoB?= NETlZXE1QCCq NHLYT|JqdmS3Y3XzJJVxemWpdXzheIlwdiCxZjDtVm5CKG:oIFXHSnIhdGmpYX7kJGhDNUWJRh?= MlHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4OE[0NVYoRjJ|Nki2OFE3RC:jPh?=
MCF-7L NY\IVphuTnWwY4Tpc44hSXO|YYm= MnnENVAxKG6PwrC= MmOxOFghcA>? NF32TpdqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ6NkSxOkc,OjN4OE[0NVY9N2F-
C4-12  MWjGeY5kfGmxbjDBd5NigQ>? MW[xNFAhdk4EoB?= NULSOVVIPDhiaB?= MVvpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT MlfqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4OE[0NVYoRjJ|Nki2OFE3RC:jPh?=
MCF-7L M{fpT2Z2dmO2aX;uJGF{e2G7 M3zKXVExOCCwTdMg MlTpNlQhcA>? MkLFbY5lfWOnczDFS2ZTKHCqb4PwbI9zgWyjdHnvckBz\XG3aYLl[EBJSi2HR1[g[pVv[3Srb36= MnLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4OE[0NVYoRjJ|Nki2OFE3RC:jPh?=
MMQ  MorMSpVv[3Srb36gRZN{[Xl? NFvXT2UxNTZ{NTDuUS=> Ml21O|IhcA>? NYLkOFV1\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[g[ZN1em:pZX6gdoVk\XC2b4Kt{tEhMEWUzsGp MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV{M{O1O{c,OjN3MkOzOVc9N2F-
H1975  NVzTOXAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPDVHcxNjNzMkWtNVAh|ryP NULTdlR5PiCm NHPTNG5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4\wbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m5PVU4Lz5{M{O5PVk2PzxxYU6=
H1975  NYHneppwSXCxcITvd4l{KEG|c3H5 MlHYNlAxKG6P NUjNPXZjPzJiaB?= MlHD[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz NGHI[Wo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5PVk2Pyd-MkOzPVk6PTd:L3G+
MCF-7  NXPSUGx1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3q4[FExNzFyMD:xNFAxKG6P NHn0NZAzNzRxNjDk Mn:4SG1UVw>? MVLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ NIXENYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OxN|UxPid-MkOzNVM2ODZ:L3G+
MCF-7  MnnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr2dnkyODBibl2= MoruOEBl MkTrSG1UVw>? NIrtRWpqdmS3Y3XzJIEhcGmpaHXyJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5idHjlJGcyKHCqYYPlxsA> MmLmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|MUO1NFYoRjJ|M{GzOVA3RC:jPh?=
MLO-Y4  MnrQSpVv[3Srb36gRZN{[Xl? M4TuPFHDqM7:TR?= MkDVNUBp M1PQcYlvcGmkaYTzJGUzNWmwZIXj[YQhS3h2MzDlfJBz\XO|aX;u NX3kVnY{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOFcxPTdpPkKzNlQ4ODV5PD;hQi=>
MCF-7 MmK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[xNFAhdk1? NIP2eXI1QCCq MkW3ZYJzd2ejdHXzJJRp\SCycn;sbYZmemG2aY\lJIVn\mWldDDv[kBud2SncnH0[UBvcXS{b4PheIl3\SC|dILld5M> Mn3tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{MU[3OFQoRjJ|MkG2O|Q1RC:jPh?=
TG1-1  MXLGeY5kfGmxbjDBd5NigQ>? MWqxxsDPxE1? NGf0bI8zPCCq M{nIcoFjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhUEmILUJOtS=> MmH6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyOEi2NFcoRjJ|MEi4OlA4RC:jPh?=
TG1-1  M2DMe2Z2dmO2aX;uJGF{e2G7 MWSxxsDPxE1? MW[yOEBp MnH0ZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBRUTON M{fJVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEi4OlA4Lz5{M{C4PFYxPzxxYU6=
MCF7 Mn;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXKxNFAhdk1? MoPjOFghcA>? NGXzdmht\WGmczD0c{BiKHOrbXnsZZIhdG:|czDpckB{fXK4aY\hcEBieyC5aYToJIRwgG:{dXLpZ4lvKGGub37l M3f0eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEe3NlQ6Lz5{M{C3O|I1QTxxYU6=
MCF7 MnrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHP5UmkyODBibl2= MYe0PEBp Mlrj[Y5p[W6lZYOgcpV1dGmwLX3l[IlifGWmIHPlcIwh\GWjdHi= MkfCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyN{eyOFkoRjJ|MEe3NlQ6RC:jPh?=
MCF-7  MVvGeY5kfGmxbjDBd5NigQ>? NULkVFdoPiCq NUnCRXFiTE2VTx?= MUfheJRmdnWjdHXzJJRp\SCobIXkbY95d26rbD2gc5Ih\mWwaHX4ZY1q\C2rbnT1Z4VlKGmwY4LlZZNmKGmwIH3pVk0zOSCneIDy[ZN{cW:w M3nze|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEWyNFM3Lz5{M{C1NlA{PjxxYU6=
MCF-7 MkXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2G5[|ExOCCwTT:xJO69VQ>? NHzBb4k2KGR? NHjsNJVqdmirYnn0d{B1cGVic4TpcZVt[XSrb36gc4YhOTgQsj3ld5Rz[WSrb3y= NHT3eGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mkm4Nlc3PSd-MkK5PFI4PjV:L3G+
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MCF7 NX2xbIFKTnWwY4Tpc44h[XO|YYm= MYeyOEBpenN? NITBclRFd3ewIILl[5Vt[XSrb36gc4Yh\XO2cn;n[Y4hemWlZYD0c5Ih[WyyaHGg[ZhxemW|c3nvckBqdiCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTF|M{e3O{c,OTlzM{O3O|c9N2F-
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HEK293 M17pUWZ2dmO2aX;uJIF{e2G7 M1PyTlEhfU1? NVrDRYVVSW62YXfvcol{fCCjY4Tpeol1gSCjdDDFVoJmfGFiaX6gTGVMOjl|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhTVKHLXTldIVv\GWwdDDseYNq\mW{YYPlJIV5eHKnc4Ppc44h[XRiMTD1US=> NYXoUZE1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4OFU{QDZpPkG5PFQ2Ozh4PD;hQi=>
Ishikawa NW\1VZBDTnWwY4Tpc44h[XO|YYm= NGHNenUyKHWP M4fmOmFvfGGpb37pd5Qh[WO2aY\peJkh[XRiZYP0do9o\W5icnXj[ZB1d3JiaX6gbJVu[W5iSYPobYtif2FiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBGWkVvZHXw[Y5l\W62IHHsb4FtcW6nIIDoc5NxcGG2YYPlJIxmfmWuczDheEAyKHWP NV6yWHk6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4OFU{QDZpPkG5PFQ2Ozh4PD;hQi=>
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HeLa NHL3N25HfW6ldHnvckBie3OjeR?= M{myflExOCCwTR?= M3npT|IxKHSxIEK0JIhzew>? NIPW[|lCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFzCSEBw\iCHUnHsdIhiKHKnY3XweI9zKGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgZoxw[2ujZHWgc4YhW1KFLUGgZolv\GmwZzD0c{Bz\WOncITvdkBifCBzMECgcm0h[W[2ZYKgNlAhfG9iMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> NXji[VBiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OFg{PDZpPkKzOFQ5OzR4PD;hQi=>
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MCF7 M1fCPGZ2dmO2aX;uJIF{e2G7 MkOxNUB2VQ>? Mni2NlAhcHK| MU\JcoR2[3Srb36gc4Yh\XO2cn;n[Y4hemWlZYD0c5Iu[WyyaHGg[IVoemGmYYTpc44hcW5iaIXtZY4hVUOINzDj[YxteyCjdDCxJJVOKGGodHXyJFIxKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NEDxOHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi3PVQ5PSd-MkW4O|k1QDV:L3G+
MCF7 MmnvSpVv[3Srb36gZZN{[Xl? NXuyd3ljOC5yMTD0c{A{ODBibl2= NWPwNolZPDhiaILz MXXE[Ydz[WSjdHnvckBi[3Srdnn0fUBw\iCHUnHsdIhiKHKnY3XweI9zKGmwIHj1cYFvKE2FRkegZ4VtdHNiYYSgNE4xOSC2bzCzNFAhdk1iYX\0[ZIhPDhiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjRyN{CxNkc,OjZ2MEewNVI9N2F-
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MCF-7 NVrO[IZzTnWwY4Tpc44h[XO|YYm= MVOzJI5ONCB|MDDuUUwhOzByIH7NMEA{KHWP NUCwdXloOjRiaILz NGrUdpRFd3ewcnXneYxifGmxbjDv[kBGWmGucHjhJIlvKGi3bXHuJG1ETi15IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBme3S{YXTpc4wucW6mdXPl[EBR\1JibWLORUBt\X[nbIOgZZQhOyC6IEGwK{06KE1uIEOgfEAyOCdvODDNMEA{KHhiMUCnMVchVSxiMzD4JFExLy14IF2gZYZ1\XJiMkSgbJJ{KGK7IGLUMXBEWiCvZYToc4Q> NWH1[3NzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2OVc{OjBpPkK4OlU4OzJyPD;hQi=>
MCF-7 NWX1VnZITnWwY4Tpc44h[XO|YYm= MonTN{BvVSxiM{Cgcm0tKDNyMDDuUUwhOyC3TR?= MUWyOEBpenN? M1TaS2Rwf26{ZXf1cIF1cW:wIH;mJGVT[WyyaHGgbY4hcHWvYX6gUWNHNTdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJIV{fHKjZHnvcE1qdmS3Y3XkJJBUOiCvUl7BJIxmfmWuczDheEA{KHhiMUCnMVkhVSxiMzD4JFExLy16IF2sJFMhgCBzMDetO{BONCB|IIigNVAoNTZiTTDh[pRmeiB{NDDodpMh[nliUmStVGNTKG2ndHjv[C=> NIfLNGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1O|MzOCd-Mki2OVc{OjB:L3G+
MCF7 NFfDOGtHfW6ldHnvckBie3OjeR?= Mm\yNVAhfU1? NHjzRWUzPCCqcoO= NHqyOWtKdmS3Y4Tpc44hd2Zic3Xs[YN1cX[nIHXzeJJw\2WwIILlZ4VxfG:{IHHsdIhiKGSnZ4Lh[IF1cW:wIHnuJIh2dWGwIF3DSlch[2WubIOgZZQhOTBidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NIXoPG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW2Nlc{Pyd-Mkm1OlI4Ozd:L3G+

... 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)
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)

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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Bio Calculators

Molarity Calculator

Molarity Calculator

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

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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The Serial Dilution Calculator Equation

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04544189 Not yet recruiting Drug: Alpelisib|Drug: Fulvestrant|Drug: Placebo Breast Neoplasms Novartis Pharmaceuticals|Novartis December 31 2020 Phase 2
NCT04567420 Not yet recruiting Drug: Palbociclib|Drug: Fulvestrant|Drug: Adjuvant Therapy Breast Cancer Criterium Inc. December 15 2020 Phase 2
NCT04524000 Recruiting Drug: Alpelisib|Drug: Fulvestrant Advanced Breast Cancer Novartis Pharmaceuticals|Novartis November 20 2020 Phase 2
NCT04483505 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. November 25 2020 Phase 1
NCT04572295 Recruiting Drug: E7090|Drug: Fulvestrant|Drug: Exemestane Breast Neoplasms Eisai Co. Ltd.|Eisai Inc. October 9 2020 Phase 1
NCT04300790 Recruiting Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant Breast Cancer MedSIR|Novartis October 23 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