Fulvestrant

For research use only.

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

75 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. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.

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Selleck's Fulvestrant has been cited by 75 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. 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 NXnYUlV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTKeGwyNjNvMUCwNEBvVQ>? MYW0PEBp MUPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFuyc5MzPDl5OUK5OC=>
MCF-7/LTED Ml;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmOyNU4{NTFyMECgcm0> NEDYOFI1QCCq MlnibY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NWj4[II4OjR7N{myPVQ>
HCC1428 MoKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWKyZ4hoOS5|LUGwNFAhdk1? MUm0PEBp M4noZolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWnyUZdPOjR7N{myPVQ>
HCC1428/LTED NGfyRnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTaNU4{NTFyMECgcm0> NWqzdHdJPDhiaB?= MUXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NEnjRYwzPDl5OUK5OC=>
LCC1 NE\zVnlHfW6ldHnvckBCe3OjeR?= MYSxNFAhdk1? MkC1OFguOTR2IHi= M4S3N4FkfGm4YYTld{BWWFJic3nncoFtcW6p NXLPW4Q5OjR6NUiyO|c>
LCC9 MnLXSpVv[3Srb36gRZN{[Xl? NYPYVo1XOTByIH7N MUe0PE0yPDRiaB?= NH35ZXVi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= NHiySHIzPDh3OEK3Oy=>
MCF-7  MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV6xNFAhdk1? M2[5O|Uh\A>? NWn2N|dCcW6qaXLpeJMh[2WubDDndo94fGhidH:gNVDwxIV? NWm5UHA{OjR6MUm1OVA>
mesangial  NXT4b5d{TnWwY4Tpc44hSXO|YYm= NIP0UGMxNjFvMUCwJI5O NF3xNJQ1QCCq MYrzeZBxemW|c3XzJHRITi4QskGtbY5lfWOnZDD0fZBmKEmYIHPvcIxi\2Ww NH;DeZEzPDd7M{[zPS=>
Mesangial MVLGeY5kfGmxbjDBd5NigQ>? MV6wMlEuOTByIH7N M4HJPFAvPSCq MmrvbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIGPtZYQzKHCqb4PwbI9zgWyjdHnvckB3cWFiR2DFVi=> MVSyOFc6OzZ|OR?=
ER+ MCF-7/2a NUXTeFBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXBV2hKSzVyPUCuNFA1KM7:TR?= NWOy[pNCOTV|MkS4PFQ>
ER+ MCF-7 NHf5[mlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDF[GIzODBiaB?= NWTn[ng4UUN3ME2wMlIyKG6P MkHkNVU{OjR6OES=
MCF-7  NH7jRYRHfW6ldHnvckBCe3OjeR?= NYrmRVBJOTEEoH7NxsA> NI\XZos4OiCq MoDMdoV3\XK|ZYOgeIhmKGW|dILv[4VvKGWoZnXjeEhKSzVyIEGuPUDEnyBzMPMIllkhVSl? M3LjVlI1QTB6NkWy
MCF-7  NITBV5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELD[5RKSzVywrDv[kBieHC{b4jpcYF1\Wy7IEKgcm0> NUDOUYFbOjN2NEizOFY>
H1975  NFHUcohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWzxsDPxE1? MlK0NUBu NEjqdWJqdmO{ZXHz[ZMhfGinIHfl[ol1cW6rYjDz[Y5{cXSrdnn0fUBw\iCKMUm3OUBk\Wyuc9Mg NGDDdVQzPDJ4OEixNC=>
H1975 MUXGeY5kfGmxbjDBd5NigQ>? NEO2R4w{yqEQvF2= NV;GcJZYOSCv NH\nb2t2eHKnZ4XsZZRmeyC2aHWgcIV3\Wxib3[gUIV1NTel NV\sZ3FSOjR{Nki4NVA>
MCF-7  Mn\SSpVv[3Srb36gRZN{[Xl? NXSwRZFHOTBy4pEJcm3DqA>? NVXUbIhZPzJiaB?= MmHBdoV3\XK|ZYOgeIhmKHC{b4TlZ5RqfmViZX\m[YN1KG:oIFWyxsBqdiClZXzsJIlvfmG|aX;u MUGyN|k{Pjd5Mx?=
MCF-7  M1vaTWZ2dmO2aX;uJGF{e2G7 Mn\jNVAx6oDLbl5CpC=> NILWO3kzPC92ODDo MU\mZYNqdGm2YYTld{Bqdn[jc3nvckB1cHKxdXfoJG1OWHNpIH3v[JVt[XSrb36= NYXwSFBLOjN7M{[3O|M>
BT474-tet-shMED1 M33kNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmwMlEuPSEQvF2= NGC3dmg4KGR? MU\pcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MmTkNlM6OzZ{M{S=
ZR75-1-tet-shMED1  NVmyU45pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIX4XFgxNjFvNTFOwG0> MWm3JIQ> NF;OT5lqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M13qNVI{QTN4MkO0
MCF-7-tet-shMED1 NEHWXZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXGwMlEuPSEQvF2= MonoO{Bl NETFTnlqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= Mme0NlM6OzZ{M{S=
HepG2  MVPGeY5kfGmxbjDBd5NigQ>? MmOxNE4xOS1zMDFOwG0> NGTJTWMyQCCqwrC= MlrIZYN1cX[jdHXzJJRp\SCHUlWtcYVlcWG2ZXSgeJJidnOlcnnweIlwdiCxZjDBSlJGWg>? NYfHWoZPOjN5M{OxPFg>
MCF-7L  NEe4dYxHfW6ldHnvckBCe3OjeR?= NG\HW2EyODBibl5CpC=> NGnrSJoyOCCvaX6vNlQhcC92ODDo MnfQdoV{fWy2czDpckBGT0[ULDDISXIzKGGwZDDISXI{KHCqb4PwbI9zgWyjdHnvckBifCCycn;sc45o\WRiZYjwc5N2emV? Mki5NlM3QDZ2MU[=
MCF-7L  NXPXTXcyTnWwY4Tpc44hSXO|YYm= M4fPcVExOCCwTdMg NXjMeI0{PDhiaB?= M{jOS4lv\HWlZYOgeZBz\We3bHH0bY9vKG:oIH3SUmEhd2ZiRVfGVkBtcWejbnSgTGIuTUeI MUiyN|Y5PjRzNh?=
MCF-7L NVTHTINvTnWwY4Tpc44hSXO|YYm= NXvpeWM4OTByIH7NxsA> NWTL[FZpPDhiaB?= MWTpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT NHrnepEzOzZ6NkSxOi=>
C4-12  MUPGeY5kfGmxbjDBd5NigQ>? MUWxNFAhdk4EoB?= NWDGcZR[PDhiaB?= NIrXc2hqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU MlPjNlM3QDZ2MU[=
MCF-7L NIj4[25HfW6ldHnvckBCe3OjeR?= M{LRXFExOCCwTdMg NWjtZZEyOjRiaB?= NYPkS5c{cW6mdXPld{BGT0[UIIDoc5NxcG:{eXzheIlwdiC{ZYH1bZJm\CCKQj3FS2Yh\nWwY4Tpc44> Mo[3NlM3QDZ2MU[=
MMQ  MlzpSpVv[3Srb36gRZN{[Xl? MXewMVYzPSCwTR?= M3vBdlczKGh? M3iweYRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIHXzeJJw\2WwIILlZ4VxfG:{Ld8xJEhGWs7zKR?= MWCyN|UzOzN3Nx?=
H1975  MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUC5Tlh4OC5|MUK1MVExKM7:TR?= NWHOPXROPiCm Mn7hbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFHGW|MzOzN7OUm1Oy=>
H1975  NV;PWllSSXCxcITvd4l{KEG|c3H5 MoLyNlAxKG6P NWHKUmRlPzJiaB?= Mm\X[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz MVmyN|M6QTl3Nx?=
MCF-7  MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHTW5EyOC9zMECvNVAxOCCwTR?= NFjjO2kzNzRxNjDk M1fiUWROW09? NITGdXpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy NWjo[mptOjN|MUO1NFY>
MCF-7  NIq0WGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzTR3VOOTByIH7N Mke1OEBl MYjEUXNQ NH:2fYJqdmS3Y3XzJIEhcGmpaHXyJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5idHjlJGcyKHCqYYPlxsA> MorUNlM{OTN3ME[=
MLO-Y4  NWrOZnQxTnWwY4Tpc44hSXO|YYm= MUWxxsDPxE1? NXfSPWxyOSCq M4nL[4lvcGmkaYTzJGUzNWmwZIXj[YQhS3h2MzDlfJBz\XO|aX;u NHzXR5EzOzJ2N{C1Oy=>
MCF-7 M{jjWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH60NnkyODBibl2= NGXkVXQ1QCCq MmfIZYJzd2ejdHXzJJRp\SCycn;sbYZmemG2aY\lJIVn\mWldDDv[kBud2SncnH0[UBvcXS{b4PheIl3\SC|dILld5M> MWWyN|IyPjd2NB?=
TG1-1  NX7lNoxWTnWwY4Tpc44hSXO|YYm= MX2xxsDPxE1? NXG0eYl{OjRiaB?= MoHTZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x M{Xv[|I{ODh6NkC3
TG1-1  NGm5T49HfW6ldHnvckBCe3OjeR?= NH7wOFkyyqEQvF2= NIDsO4czPCCq M{PadoFjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhWEl|Sx?= M3fZXVI{ODh6NkC3
MCF7 Mnj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU[1OYk{OTByIH7N MUi0PEBp NWHoZ4d5dGWjZIOgeI8h[SC|aX3pcIFzKGyxc4OgbY4he3W{dnn2ZYwh[XNid3n0bEBld3ixcoXibYNqdiCjbH;u[S=> Mnu0NlMxPzd{NEm=
MCF7 NV\ONXpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHi2OXoyODBibl2= NFOxd3k1QCCq MlXF[Y5p[W6lZYOgcpV1dGmwLX3l[IlifGWmIHPlcIwh\GWjdHi= Ml\zNlMxPzd{NEm=
MCF-7  MVHGeY5kfGmxbjDBd5NigQ>? NGLTVmU3KGh? NGHDSWVFVVOR MVTheJRmdnWjdHXzJJRp\SCobIXkbY95d26rbD2gc5Ih\mWwaHX4ZY1q\C2rbnT1Z4VlKGmwY4LlZZNmKGmwIH3pVk0zOSCneIDy[ZN{cW:w MV[yN|A2OjB|Nh?=
MCF-7 NWTjbFd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HVTlExOCCwTT:xJO69VQ>? MYm1JIQ> NU\qdIJncW6qaXLpeJMhfGinIIP0bY12dGG2aX;uJI9nKDF5zsKt[ZN1emGmaX;s NYnxV2JbOjJ7OEK3OlU>
MCF-7 NEDBUYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYS0c2ExOTByIH7N M3Wy[|Uh\A>? Mo\3bY5pcWKrdIOgeIhmKHO2aX31cIF1cW:wIH;mJIZ2e2G{aXXsbY4hUA>? M1TxUlIzQTh{N{[1
1471.1 NH\FfXhHfW6ldHnvckBCe3OjeR?= MXSxNFAhdk1? MU[xJIg> MmLTSZRQUMLi MnP5eIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu M{DGRVIzQDZ7MUC2
MCF-7 NFTDWWRHfW6ldHnvckBCe3OjeR?= MXyxNFAhdk1? NGPx[XMyKGh? NFzRVXlGfE:KwrC= NV7ib4RpfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv MnG5NlI5PjlzME[=
HeLa NELGNGNHfW6ldHnvckBCe3OjeR?= NUO0OoliOTByIH7N NV;JNGNrOSCq NVLLRXc4TXSRSNMg MVP0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= MVyyNlg3QTFyNh?=
COS-7  NWT3NWZXTnWwY4Tpc44hSXO|YYm= NIfuTocyODBibl2= MWCxJIg> MoC1SZRQUMLi NWfGOmFPfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv NGPVdHkzOjh4OUGwOi=>
BG1L-OHTLT  NHLvToRHfW6ldHnvckBCe3OjeR?= MWGxNOKhdk1? NGHxN2ozPMLiaNMg NX;ac49JcW6qaXLpeJMhTVMQsTDlfJBz\XO|aX;u MlnTNlI3PTJ3NUi=
BG1L-ICILT NELGU|JHfW6ldHnvckBCe3OjeR?= MWOxNOKhdk1? NUHkZopyOjUEoHlCpC=> M2LvWolvcGmkaYTzJGVT|rFiZYjwdoV{e2mxbh?= M1fQbFIzPjV{NUW4
PC-9 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGwMlAxOy1|MDFOwG0> MlLlOFghcA>? M2ixcolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnOyNlI2PjB4M{S=
H1650 M1\ORmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTsRZQxNjByMz2zNEDPxE1? MWS0PEBp MYrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1y3fFIzPTZyNkO0
H1975 NV7kfJdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPJUVE4OC5yMEOtN|Ah|ryP Mn3MOFghcA>? MWnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NH\GbWQzOjV4ME[zOC=>
H1975 NUXYcXRlTnWwY4Tpc44hSXO|YYm= MXmzxsDPxE1? M4rkVFMhcA>? NYfRW4t1[WK{b3fheIV{KHSqZTDwbI9{eGixLVXHSnIhcW6mdXP0bY9vKGK7IHXzeJJw\2Ww NXGzVXRvOjJ3NkC2N|Q>
H1975 NWTIRW41TnWwY4Tpc44hSXO|YYm= M1zWVlPDqM7:TR?= M3XwOVch\A>? NXXMepNrcW6mdXPld{BGT0[UIHX4dJJme3Orb36= MYWyNlU3ODZ|NB?=
HTR-8 MmnMSpVv[3Srb36gRZN{[Xl? MlTDNeKh|ryP NEizO4wyNTR6IHi= NX[5TnFM\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gTWdHSlB5IH3SUmE> NH3VXpczOjN6M{GxNS=>
JEG-3 MXLGeY5kfGmxbjDBd5NigQ>? M3;hfVHDqM7:TR?= MoDYNU01QCCq M323XIRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B NFrXU5ozOjN6M{GxNS=>
Huh7 M{PFfmZ2dmO2aX;uJGF{e2G7 MlXxOVDDqM7:TR?= NIPue3M1QCCq NFvkO2NqdmirYnn0d{Bo\W6rc4TlbY4udWWmaXH0[YQhWE:QMTD0doFve2GldHn2ZZRqd25? Mnj6NlI{ODR{OU[=
201T M1jWNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX21JO69VQ>? NX3j[Y5XPzJiaB?= Mk[5bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? M1n4OFIzOjV6NEe2
A549  MmXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTmfZI2KM7:TR?= MYS3NkBp NFW1[WNqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnHu[IV1[W6rYh?= MnvkNlIzPTh2N{[=
MCF-7 MX\GeY5kfGmxbjDBd5NigQ>? NU\5dVBWOcLizszN NVf1R2I{OjRiaNMg NG\Hb4pld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? NXPzRlJ2OjJyNEmzNVY>
HCC-1428 Mm\mSpVv[3Srb36gRZN{[Xl? NVXuepQ3OcLizszN M2LmVVI1KGkEoB?= NYfvRWVn\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi MkTwNlIxPDl|MU[=
MDA-361 NEfvdXVHfW6ldHnvckBCe3OjeR?= Mni0NeKh|ryP M4jLcFI1KGkEoB?= Mn;j[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh M1rqZlIzODR7M{G2
ZR75-1 M{n1emZ2dmO2aX;uJGF{e2G7 NXTzXFNjOcLizszN Mo\aNlQhcMLi NIjFco9ld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? M{faUVIzODR7M{G2
MCF-7 M2DzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;u[3FVOcLizszN MXG1MVExKGR? MkTYd5VxeHKnc4Pld{BGOi2rbnT1Z4VlKGe{b4f0bEBqdmirYnn0bY9v NITvb2IzOjB2OUOxOi=>
HCC-1428 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1u5fVHDqM7:TR?= M2q3bVUuOTBiZB?= MUDzeZBxemW|c3XzJGUzNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> NHzseYwzOjB2OUOxOi=>
MDA-361 Mny0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnke4kyyqEQvF2= NYPzbY4xPS1zMDDk NEXNXpp{fXCycnXzd4V{KEV{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? NGTVfmQzOjB2OUOxOi=>
ZR75-1 NVzIboFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzERZBsOcLizszN NX\UUGh7PS1zMDDk M1vmSpN2eHC{ZYPz[ZMhTTJvaX7keYNm\CCpcn;3eIghcW6qaXLpeIlwdg>? NEnzdZkzOjB2OUOxOi=>
MCF-7/AC-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[zNE0xNjJizszN NIWwRWU3KGR? NX;HUGVqcW6qaXLpeJMh[2WubDDndo94fGhibX;k[ZN1dHl? NFWye|czOjB2Mke5Ni=>
MCF7 M2e3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTRNVAhyrWP NUj4XWh4PDhiaB?= MnrXbY5lfWOnczDj[YxtKGmwaHnibZRqd25id3jpZ4gh[2GwIHLlJIVvcGGwY3XkJIJ6KG[rYoLvZoxie3S| NU\kdY1SOjJyNEG4PFc>
MMQ NVTSR2I{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHixeJUxNTZ{NTDuUS=> Mo[zO|IhcA>? MmXjdJJw\HWlZYOgd5RifGm|dHnjZYxtgSC|aXfubYZq[2GwdDDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdsLi NWLnSmtrOjJyMUWxNFE>
MMQ MX7GeY5kfGmxbjDBd5NigQ>? NGDwW|MxNTZ{NTDuUS=> NITSbWo4OiCq M1\ibZBzd2S3Y3XzJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEwh\G:|ZT3k[ZBmdmSnboSgdoVlfWO2aX;uJIlvKFCUTDDz[YNz\XSrb36= NXjWZ4VmOjJyMUWxNFE>
MCF7 NIDjNnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MViwMVEh|ryP M{LENlI1NTF{MDDo M1\xbolvcGmkaYTzJJRp\SCpcn;3eIghd2ZiTVPGO{1[Si1zwrC= Mn3aNlE5PjN{NUi=
HepG2 M365WGFxd3C2b4Ppd{BCe3OjeR?= MUKwMlHDqM7:TR?= MkDpNlQhcA>? M1;D[YFjd2yrc3jld{B1cGViZYP0do9o\W5vaX7keYNm\CC3cD3y[Yd2dGG2aX;uJI9nKGGyb1HJJIFv\CCjcH;N NFnFZoEzOThzNkKzNy=>
MCF7–iFR3 NV3TVY9wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PpXVIxNTFyMDDuUS=> MXS5OkBp NEnsSGdmdmijbnPld{BCWC2rbnT1Z4VlKGOnbHyg[5Jwf3SqIHnubIljcXSrb36= M4\ZTFIyPzl{OEi5
MCF7S M13PPWZ2dmO2aX;uJGF{e2G7 NEn3eGcyyqEQvF2= M3G2UVQ5KGh? NYTWVolk\G:5boLl[5Vt[XSnczDveoVz[WyuIFXS{tEheHKxdHXpckBt\X[nbIO= MnvkNlE2OzNzOUW=
MCF7 NHnZcppHfW6ldHnvckBCe3OjeR?= NVPoS2xXOcLizszN NUTWdnE4PDhiaB?= NF3uTZhld3ewcnXneYxifGW|IH;2[ZJidGxiRWNOtUBxem:2ZXnuJIxmfmWucx?= MX[yNVU{OzF7NR?=
MCF7S MYDGeY5kfGmxbjDBd5NigQ>? MU[xxsDPxE1? NUL1d|k1PyCm M3TN[IF1fGWwdXH0[ZMhfHWvb4LzdIhmemViZn;ycYF1cW:wIHHu[EBxem:uaX\ldoF1cW:w MoPSNlE2OzNzOUW=
MCF7S M1vl[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1X6fVAvPS9zIN88US=> NFP6SXc4KGR? NX\lcXR4TE2VTx?= NXzMRnZN\GWlcnXhd4V{KGOnbHyg[Zhx[W6|aX;u NUjKbXpOOjF3M{OxPVU>
T47D  MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvPOIhpPCCwTR?= MVS0NEBp NWjDSoU6e3WycILld5NmeyClZXzsJIdzd3e2aDDtc4RmemG2ZXz5 NWK5Z5ltOjF2OECzPVE>
BT474  NIHSU49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\mOEBvVQ>? MmT2OFAhcA>? NWmydIZKe3WycILld5NmeyClZXzsJIdzd3e2aDDtc4RmemG2ZXz5 M1nNV|IyPDhyM{mx
T47D  NULjV2x4TnWwY4Tpc44hSXO|YYm= NXLzVnNrOTBibl2= MmXqOFAhcA>? NHXzdZBld3ewcnXneYxifGW|IFXS{tEheHKxdHXpci=> MV:yNVQ5ODN7MR?=
BT474  NX[3V2NITnWwY4Tpc44hSXO|YYm= NYjYUmt[OTBibl2= MW[0NEBp Mm\P[I94dnKnZ4XsZZRmeyCHUt8xJJBzd3SnaX6= MlLaNlE1QDB|OUG=
MCF7 NXPpcWVoTnWwY4Tpc44hSXO|YYm= NITYU4cyODBibl2= NGD5Noc4KGR? Mnn2doVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> MofnNlE{QTZyOUS=
T47D  NXvXNnFJTnWwY4Tpc44hSXO|YYm= NGTVd24yODBibl2= NXnlO|BnPyCm NGn4XmRz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 M1KybVIyOzl4MEm0
BT474  M3LyU2Z2dmO2aX;uJGF{e2G7 MXqxNFAhdk1? NETVPFM4KGR? NWK4[m5vemWmdXPld{BGWs7zIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? MmLJNlE{QTZyOUS=
MDAMB361 M3jGRmZ2dmO2aX;uJGF{e2G7 NXjmTIxjOTByIH7N NYDubFVjPyCm NGK2fI9z\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 NIPOfFUzOTN7NkC5OC=>
MCF7 NGLC[lJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUf4b29ZOC5yMT2xJO69VQ>? MVi3JIQ> M{jHcpJm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MUeyNVM6PjB7NB?=
T47D  NUf3bXNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzsXHMxNjBzLUGg{txO MUC3JIQ> NFHEPWtz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NHfvXVIzOTN7NkC5OC=>
BT474  NIDTdZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnYN3hbOC5yMT2xJO69VQ>? MUi3JIQ> M1TwSpJm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NE\QcYkzOTN7NkC5OC=>
MDAMB361 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDZPFExNjBzLUGg{txO NHjm[2w4KGR? Ml:zdoVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NFLkc|MzOTN7NkC5OC=>
MCF7 NIXCbpVHfW6ldHnvckBCe3OjeR?= NVrkTI5SOTByIH7N Mlu5O{Bl NULLbYgxcW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=> NF7kRZIzOTN7NkC5OC=>
T47D  MWjGeY5kfGmxbjDBd5NigQ>? M1j0dlExOCCwTR?= M4LCZ|ch\A>? M3Gy[4lv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= NFf6T4YzOTN7NkC5OC=>
BT474  M4P1bmZ2dmO2aX;uJGF{e2G7 M3XaNFExOCCwTR?= M2ToPFch\A>? NFPBeG1qdmS3Y3XzJI9nKEW{YlKzJIFv\CCHcnLCOEBz\WOncITvdkBmgHC{ZYPzbY9vKGGwZDDzbYdv[WyuaX7n NXLjNJNyOjF|OU[wPVQ>
MDAMB361 NGHGO4ZHfW6ldHnvckBCe3OjeR?= MnG4NVAxKG6P NXXBWm5pPyCm NIfqTphqdmS3Y3XzJI9nKEW{YlKzJIFv\CCHcnLCOEBz\WOncITvdkBmgHC{ZYPzbY9vKGGwZDDzbYdv[WyuaX7n NYm3OYRbOjF|OU[wPVQ>
MCF7 M4K4SGZ2dmO2aX;uJGF{e2G7 MVOxNEBvVQ>? MX:5OkBp MV7kc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb39CpC=> MV[yNVM4QDN|Mx?=
MDA-MB-231 MkT0SpVv[3Srb36gRZN{[Xl? NF;0TFEyOCCwTR?= NFW4NYs6PiCq MXPkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb39CpC=> MnLVNlE{Pzh|M{O=
SK-BR-3 NFzyUoxHfW6ldHnvckBCe3OjeR?= NGj4clAyOCCwTR?= M4niVFk3KGh? MVTkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb39CpC=> MnnBNlE{Pzh|M{O=
MCF-7 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13P[VExOCCwTR?= NIjDSZQ4Oi97NjDo Ml;4Z4F2e2W|IHPlcIwh[3mlbHWgZZJz\XO2 NHKx[oQzOTJ7OUi2Ni=>
MMQ M1q2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXq3SYZUOC5yMEitOlI2KG6P NFXi[4o4OiCq NYrtdY1vcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lMUBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Moq5NlA4ODB5NUW=
MMQ MoLhSpVv[3Srb36gRZN{[Xl? NVHaVYNtOC5yMEitOlI2KG6P MknUO|IhcA>? NH3yOnhqdmirYnn0d{BRWkxic3XjdoV1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NFLGWnYzODdyMEe1OS=>
MMQ NHzHeGlHfW6ldHnvckBCe3OjeR?= MXywMlA1NTZ{NTDuUS=> NV74c5pCPzJiaB?= M1GyZolvcGmkaYTzJGVT|rFiZYjwdoV{e2mxbh?= M33vfFIxPzByN{W1
MMQ NYG0fFlYTnWwY4Tpc44hSXO|YYm= M3LqSFAvODRvNkK1JI5O MYS3NkBp MWj1dJJm\3WuYYTld{BVT0cQskOgZY5lKFSJRt8yVmlKKGW6cILld5Nqd25? MW[yNFcxODd3NR?=

... 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)
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 ICI-182780, ZD 9238
Smiles CC12CCC3C(C(CCCCCCCCC[S](=O)CCCC(F)(F)C(F)(F)F)CC4=C3C=CC(=C4)O)C1CCC2O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT04318223 Recruiting Drug: Palbociclib Metastatic Breast Cancer|Locally Advanced Breast Cancer Consorzio Oncotech July 16 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