Fulvestrant

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

Fulvestrant Chemical Structure

Molecular Weight(MW): 606.77

Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay.

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Cited by 23 Publications

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay.
Targets
ER [1]
(Cell-free assay)
0.94 nM
In vitro

Fulvestrant is an effective inhibitor of the growth of ER-positive MCF-7 (with IC50 of 0.29 nM) but with no effect on the growth of ER-negative BT-20 human breast cancer cells. Fulvestrant causes accumulation of cells in G0/G1 and also reduces the proportion of cells capable of continued DNA synthesis. [1] Fulvestrant competitively inhibits binding of oestradiol to the estrogen receptor. Fulvestrant blocks nuclear localization of the ER through impairing receptor dimerisation, and energy-dependent nucleo-cytoplasmic shuttling. Because of the instability of fulvestrant-ER complex, the binding of Fulvestrant with ER finally results in accelerated degradation of the ER protein. [2] Fulvestrant (10 nM) not only decreases IGF-IR mRNA levels but also decreases the half-life. [3] Treatment with 100 μM Fulvestrant leads to a time dependent increase of TNFR1 and TRADD steady-state mRNA levels in MCF-7 cells. [4] Fulvestrant is capable of down-regulating androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells. Fulvestrant also significantly attenuates R1881-stimulated growth by 70%. [5] Fulvestrant is able to modulate mitosis and cell death in immature cerebellar neurons via rapid activation of MAPK. [6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 MkC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2C5PVEvOy1zMECwJI5O M3P0PFQ5KGh? NWDDWGV[cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4PtV|I1QTd7Mkm0
MCF-7/LTED MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH24NmYyNjNvMUCwNEBvVQ>? MXK0PEBp MYrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4fUTVI1QTd7Mkm0
HCC1428 MkjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEf1dFcyNjNvMUCwNEBvVQ>? NILpT2Q1QCCq MkXGbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M2nrR|I1QTd7Mkm0
HCC1428/LTED NFnz[4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1Pnc|EvOy1zMECwJI5O MmnHOFghcA>? NUHmU5R3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWj4dIV6OjR7N{myPVQ>
LCC1 NIr2U5dHfW6ldHnvckBCe3OjeR?= NGrES3gyODBibl2= NW\K[XViPDhvMUS0JIg> MUThZ5RqfmG2ZYOgWXBTKHOrZ37hcIlv\w>? NGnZW2QzPDh3OEK3Oy=>
LCC9 MmrVSpVv[3Srb36gRZN{[Xl? M1\TdlExOCCwTR?= NYHQTlBtPDhvMUS0JIg> M1O1Z4FkfGm4YYTld{BWWFJic3nncoFtcW6p MkLHNlQ5PTh{N{e=
MCF-7  MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHNRYEyODBibl2= NF;2W4U2KGR? NXm5UYFrcW6qaXLpeJMh[2WubDDndo94fGhidH:gNVDwxIV? M1m4WlI1QDF7NUWw
mesangial  MXPGeY5kfGmxbjDBd5NigQ>? NEDyeJUxNjFvMUCwJI5O M1LQd|Q5KGh? NVfablV2e3WycILld5NmeyCWR1[t{tIyNWmwZIXj[YQhfHmyZTDJWkBkd2yuYXflci=> NGLWeY0zPDd7M{[zPS=>
Mesangial M13LfGZ2dmO2aX;uJGF{e2G7 MnjhNE4yNTFyMDDuUS=> NV\OPIliOC53IHi= MWfpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRiU33h[FIheGixc4Doc5J6dGG2aX;uJJZq[SCJUFXS NV;wZppQOjR5OUO2N|k>
ER+ MCF-7/2a Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NISwWXdKSzVyPUCuNFA1KM7:TR?= M{LXXFE2OzJ2OEi0
ER+ MCF-7 Mn;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\DfGQzODBiaB?= NWC4UlJbUUN3ME2wMlIyKG6P MV6xOVMzPDh6NB?=
MCF-7  MmrKSpVv[3Srb36gRZN{[Xl? Ml\FNVDDqG6PwrC= NEf5[ZE4OiCq Mn\CdoV3\XK|ZYOgeIhmKGW|dILv[4VvKGWoZnXjeEhKSzVyIEGuPUDEnyBzMPMIllkhVSl? MXWyOFkxQDZ3Mh?=
MCF-7  MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[yTWM2OMLib3[gZZBxem:6aX3heIVtgSB{IH7N Ml\JNlM1PDh|NE[=
H1975  NFLTeZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWWzxsDPxE1? M{PiVFEhdQ>? MnjJbY5kemWjc3XzJJRp\SCpZX\peIlvcWJic3Xud4l1cX[rdImgc4YhUDF7N{WgZ4VtdHQEoB?= NFvkV3IzPDJ4OEixNC=>
H1975 M1;KW2Z2dmO2aX;uJGF{e2G7 NVTLW3R1O8LizszN M4Phd|EhdQ>? Mny2eZBz\We3bHH0[ZMhfGinIHzleoVtKG:oIFzleE04[w>? NIPRPVYzPDJ4OEixNC=>
MCF-7  NXPYRZhzTnWwY4Tpc44hSXO|YYm= M2CyfVExOOLCiX7NxsA> NWPn[5hPPzJiaB?= NGTudm1z\X[ncoPld{B1cGVicILveIVkfGm4ZTDl[oZm[3Rib3[gSVLDqGmwIHPlcIwhcW64YYPpc44> M3y2blI{QTN4N{ez
MCF-7  NWHWRZlCTnWwY4Tpc44hSXO|YYm= Moi1NVAx6oDLbl5CpC=> MVWyOE81QCCq NWXGS5d{\mGlaXzpeIF1\XNiaX72ZZNqd25idHjyc5VocCCPTWDzK{Bud2S3bHH0bY9v NYPU[oJFOjN7M{[3O|M>
BT474-tet-shMED1 M2jVemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPV[lUxNjFvNTFOwG0> MoD0O{Bl NV;uflFPcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M3zGR|I{QTN4MkO0
ZR75-1-tet-shMED1  NYHnd|BKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLaTlVOOC5zLUWg{txO MnzTO{Bl M1vrNIlv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M4fZZVI{QTN4MkO0
MCF-7-tet-shMED1 NXrSN4pJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:wMlEuPSEQvF2= NXzFPHZ[PyCm NFe5ZZdqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NFizXW8zOzl|NkKzOC=>
HepG2  MlvLSpVv[3Srb36gRZN{[Xl? MlfHNE4xOS1zMDFOwG0> MlWwNVghcMLi MlfyZYN1cX[jdHXzJJRp\SCHUlWtcYVlcWG2ZXSgeJJidnOlcnnweIlwdiCxZjDBSlJGWg>? MXOyN|c{OzF6OB?=
MCF-7L  MYPGeY5kfGmxbjDBd5NigQ>? M3q1fFExOCCwTdMg M2nTWlExKG2rbj:yOEBpNzR6IHi= NGrDWGFz\XO3bITzJIlvKEWJRmKsJGhGWjJiYX7kJGhGWjNicHjvd5Bpd3K7bHH0bY9vKGG2IIDyc4xwdmenZDDlfJBwe3W{ZR?= NYHOR4xwOjN4OE[0NVY>
MCF-7L  MlvVSpVv[3Srb36gRZN{[Xl? NH\LeZUyODBibl5CpC=> NXPQdG9MPDhiaB?= MXzpcoR2[2W|IIXwdoVofWyjdHnvckBw\iCvUl7BJI9nKEWJRmKgcIlo[W6mIFjCMWVITg>? NG\1SogzOzZ6NkSxOi=>
MCF-7L NHLsT4tHfW6ldHnvckBCe3OjeR?= NESweXUyODBibl5CpC=> MWi0PEBp M{fGPIlv\HWlZYOgSWdHWiCoYX3pcJkhdWWvYnXyJIFkfGm4YYTpc44hemWzdXny[YQhTVJ? NFPzNFUzOzZ6NkSxOi=>
C4-12  MYnGeY5kfGmxbjDBd5NigQ>? M2jOTVExOCCwTdMg NGj4fnc1QCCq NGewNG5qdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU M{nxflI{Pjh4NEG2
MCF-7L MYHGeY5kfGmxbjDBd5NigQ>? MXGxNFAhdk4EoB?= NVHFXWRPOjRiaB?= NXz4OHBNcW6mdXPld{BGT0[UIIDoc5NxcG:{eXzheIlwdiC{ZYH1bZJm\CCKQj3FS2Yh\nWwY4Tpc44> NEnGWIszOzZ6NkSxOi=>
MMQ  Mn;0SpVv[3Srb36gRZN{[Xl? MYGwMVYzPSCwTR?= NX2xOHpzPzJiaB?= M1fhcYRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIHXzeJJw\2WwIILlZ4VxfG:{Ld8xJEhGWs7zKR?= M4HNUFI{PTJ|M{W3
H1975  MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWG1fpdbOC5|MUK1MVExKM7:TR?= MkC3OkBl MkPGbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWqyN|M6QTl3Nx?=
H1975  MYrBdI9xfG:|aYOgRZN{[Xl? MkjWNlAxKG6P NG\YZ|I4OiCq MX3lcohidmOnczDldoxwfGmwaXKgbY5lfWOnZDDhdI9xfG:|aYO= MX:yN|M6QTl3Nx?=
MCF-7  MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPNNVAwOTByL{GwNFAhdk1? M{DBWlIwPC94IHS= M4LkeWROW09? NV65cHJzcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> MkXJNlM{OTN3ME[=
MCF-7  M1zFfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jseFExOCCwTR?= NHfNN5c1KGR? NF22[3pFVVOR NW\2fJBZcW6mdXPld{BiKGirZ3jldkBxem:yb4L0bY9vKG:oIHPlcIx{KGmwIITo[UBIOSCyaHHz[eKh Mn;aNlM{OTN3ME[=
MLO-Y4  NF3pbnRHfW6ldHnvckBCe3OjeR?= MWixxsDPxE1? NWfTNnZjOSCq NHLOXHdqdmirYnn0d{BGOi2rbnT1Z4VlKEO6NEOg[ZhxemW|c3nvci=> M3;HVFI{OjR5MEW3
MCF-7 NGjRcZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYOxNFAhdk1? NGHre201QCCq Mo\VZYJzd2ejdHXzJJRp\SCycn;sbYZmemG2aY\lJIVn\mWldDDv[kBud2SncnH0[UBvcXS{b4PheIl3\SC|dILld5M> MljYNlMzOTZ5NES=
TG1-1  NVfNblFoTnWwY4Tpc44hSXO|YYm= MX2xxsDPxE1? MnnNNlQhcA>? NVLjS2E3[WK{b3fheIV{KEV{wrDpcoR2[2WmIHHjZ5VufWyjdHnvckBw\iCKSV[tNe6y NEPtR3EzOzB6OE[wOy=>
TG1-1  MmDySpVv[3Srb36gRZN{[Xl? NFzVUmkyyqEQvF2= M3HoWVI1KGh? MkfPZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBRUTON M13aV|I{ODh6NkC3
MCF7 M{HlfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWKxNFAhdk1? MXS0PEBp MVHs[YFleyC2bzDhJJNqdWmuYYKgcI9{eyCrbjDzeZJ3cX[jbDDhd{B4cXSqIHTvfI9zfWKrY3nuJIFtd26n MVuyN|A4PzJ2OR?=
MCF7 NVPTSpdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV6xNFAhdk1? M2npe|Q5KGh? MU\lcohidmOnczDueZRtcW5vbXXkbYF1\WRiY3XscEBl\WG2aB?= M3jITFI{ODd5MkS5
MCF-7  NGD2WmdHfW6ldHnvckBCe3OjeR?= MXm2JIg> NFzne|NFVVOR M{fVUIF1fGWwdXH0[ZMhfGinIH\seYRqd3ixbnnsMUBweiCoZX7o[ZhidWmmLXnu[JVk\WRiaX7jdoVie2ViaX6gcYlTNTJzIHX4dJJme3Orb36= MluxNlMxPTJyM{[=
MCF-7 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnK1NVAxKG6PL{Gg{txO M4GwdVUh\A>? MlLmbY5pcWKrdIOgeIhmKHO2aX31cIF1cW:wIH;mJFE4|rJvZYP0doFlcW:u NF\FXogzOjl6Mke2OS=>
MCF-7 M4fHbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrUZnMyODBibl2= MVe1JIQ> M{nL[4lvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kBnfXOjcnnlcIlvKEh? NVHqb456OjJ7OEK3OlU>
1471.1 NXL5U5o4TnWwY4Tpc44hSXO|YYm= M2nJS|ExOCCwTR?= MnrqNUBp MlrBSZRQUMLi Mni4eIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu MYmyNlg3QTFyNh?=
MCF-7 NWXhe4ZHTnWwY4Tpc44hSXO|YYm= MWSxNFAhdk1? M4P6cVEhcA>? NH;SSWJGfE:KwrC= NXzkcIZufGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv MlHVNlI5PjlzME[=
HeLa Ml\OSpVv[3Srb36gRZN{[Xl? M1XWZVExOCCwTR?= MWCxJIg> NYfTfGhjTXSRSNMg NYG0d5BZfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv NVX3bZloOjJ6NkmxNFY>
COS-7  NVLkNoNjTnWwY4Tpc44hSXO|YYm= NV33OY5JOTByIH7N NWPGfJRWOSCq MXLFeG9JyqB? M3\Sd5Ric2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> NGrJdGczOjh4OUGwOi=>
BG1L-OHTLT  MVzGeY5kfGmxbjDBd5NigQ>? MlTPNVDDqG6P MYqyOOKhcMLi MWjpcohq[mm2czDFVu6yKGW6cILld5Nqd25? NXLqSY1ZOjJ4NUK1OVg>
BG1L-ICILT MUHGeY5kfGmxbjDBd5NigQ>? M4DMcFExyqCwTR?= M2DkTVI1yqCqwrC= NGPVW2pqdmirYnn0d{BGWs7zIHX4dJJme3Orb36= NXv5fYR[OjJ4NUK1OVg>
PC-9 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LjTlAvODB|LUOwJO69VQ>? MknvOFghcA>? MVnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHW2e4IzOjV4ME[zOC=>
H1650 NIDtXnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWewMlAxOy1|MDFOwG0> M{fhZlQ5KGh? M1rG[olvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{HjO|IzPTZyNkO0
H1975 MlLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPGWGkxNjByMz2zNEDPxE1? MlLVOFghcA>? NFXNVXpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NIDE[ZMzOjV4ME[zOC=>
H1975 MYLGeY5kfGmxbjDBd5NigQ>? M2TUeFPDqM7:TR?= NHzQeVI{KGh? NVSxflBS[WK{b3fheIV{KHSqZTDwbI9{eGixLVXHSnIhcW6mdXP0bY9vKGK7IHXzeJJw\2Ww M1PNZVIzPTZyNkO0
H1975 M2[0NGZ2dmO2aX;uJGF{e2G7 Mki0N:Kh|ryP MVm3JIQ> Ml7XbY5lfWOnczDFS2ZTKGW6cILld5Nqd25? NGnh[lEzOjV4ME[zOC=>
HTR-8 NHjJXGtHfW6ldHnvckBCe3OjeR?= M{HnTFHDqM7:TR?= NELmNHIyNTR6IHi= MnTv[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSVfGRnA4KG2UTlG= MoPoNlI{QDNzMUG=
JEG-3 MnPRSpVv[3Srb36gRZN{[Xl? M3Lqd|HDqM7:TR?= MVGxMVQ5KGh? M2T5OoRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B NH;ZUJYzOjN6M{GxNS=>
Huh7 NV76[WxTTnWwY4Tpc44hSXO|YYm= NUj1eWZ{PTEEoN88US=> NXTGZZZzPDhiaB?= NFTHXGJqdmirYnn0d{Bo\W6rc4TlbY4udWWmaXH0[YQhWE:QMTD0doFve2GldHn2ZZRqd25? MmniNlI{ODR{OU[=
201T MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVi1JO69VQ>? NX;ZUVhHPzJiaB?= NYDXdHFIcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\hcoRmfGGwaXK= M37Z[|IzOjV6NEe2
A549  MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLWOUDPxE1? M2fVd|czKGh? M1f4folvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4YX7k[ZRidmmk MkHuNlIzPTh2N{[=
MCF-7 Ml31SpVv[3Srb36gRZN{[Xl? MXixxsDPxE1? NW\YUY5xOjRiaNMg MVrkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb36gbY5lfWOnZDDifUA1NU:KLWSgxsA> M3ftO|IzODR7M{G2
HCC-1428 NV7vUJk6TnWwY4Tpc44hSXO|YYm= M4TUNlHDqM7:TR?= MnG4NlQhcMLi MVfkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb36gbY5lfWOnZDDifUA1NU:KLWSgxsA> M3yweVIzODR7M{G2
MDA-361 MnTYSpVv[3Srb36gRZN{[Xl? M{fYU|HDqM7:TR?= M4HJWVI1KGkEoB?= MUDkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb36gbY5lfWOnZDDifUA1NU:KLWSgxsA> M37KVVIzODR7M{G2
ZR75-1 NHmzVmRHfW6ldHnvckBCe3OjeR?= MVixxsDPxE1? MYSyOEBpyqB? NEfKUHVld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? MYKyNlA1QTNzNh?=
MCF-7 NWrVbXFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7GN5YyyqEQvF2= MU[1MVExKGR? MmX2d5VxeHKnc4Pld{BGOi2rbnT1Z4VlKGe{b4f0bEBqdmirYnn0bY9v MUSyNlA1QTNzNh?=
HCC-1428 M1LDSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCxxsDPxE1? MlTaOU0yOCCm MmLxd5VxeHKnc4Pld{BGOi2rbnT1Z4VlKGe{b4f0bEBqdmirYnn0bY9v M1\j[FIzODR7M{G2
MDA-361 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFf6VVUyyqEQvF2= NIWzSHI2NTFyIHS= NYHyOZZie3WycILld5NmeyCHMj3pcoR2[2WmIHfyc5d1cCCrbnjpZol1cW:w M3z4UVIzODR7M{G2
ZR75-1 MorDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWOxxsDPxE1? NUXDbVNZPS1zMDDk M4TYSJN2eHC{ZYPz[ZMhTTJvaX7keYNm\CCpcn;3eIghcW6qaXLpeIlwdg>? MVSyNlA1QTNzNh?=
MCF-7/AC-1 M4\iTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NECySXcxNTBwMjFOwG0> NHvDfWs3KGR? NGTsbYZqdmirYnn0d{Bk\WyuIHfyc5d1cCCvb3Tld5RtgQ>? MlnNNlIxPDJ5OUK=
MCF7 NHTkS25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXGdXJzOTBiwsXN NIX5c3M1QCCq M3XOZ4lv\HWlZYOgZ4VtdCCrbnjpZol1cW:wIIfobYNpKGOjbjDi[UBmdmijbnPl[EBjgSCoaXLyc4Jt[XO2cx?= NHPXUJkzOjB2MUi4Oy=>
MMQ MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTF[4ExNTZ{NTDuUS=> NUPJXZM1PzJiaB?= MonhdJJw\HWlZYOgd5RifGm|dHnjZYxtgSC|aXfubYZq[2GwdDDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdsLi MUOyNlAyPTFyMR?=
MMQ NGHycYZHfW6ldHnvckBCe3OjeR?= MWCwMVYzPSCwTR?= Ml;IO|IhcA>? NH6xWZVxem:mdXPld{BiKHO2YYTpd5Rq[2GubImgd4lodmmoaXPhcpQtKGSxc3Wt[IVx\W6mZX70JJJm\HWldHnvckBqdiCSUlygd4VkemW2aX;u M3v3WFIzODF3MUCx
MCF7 NEDQVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjlZ2txOC1zIN88US=> NIGxUowzPC1zMkCgbC=> M1HqbYlvcGmkaYTzJJRp\SCpcn;3eIghd2ZiTVPGO{1[Si1zwrC= NW\Kd3c3OjF6NkOyOVg>
HepG2 M4Kw[2Fxd3C2b4Ppd{BCe3OjeR?= NWXZPYdTOC5zwrFOwG0> NGr0SIszPCCq NWDPfZkz[WKxbHnzbIV{KHSqZTDld5Rzd2enbj3pcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZiYYDvRWkh[W6mIHHwc20> MXKyNVgyPjJ|Mx?=
MCF7–iFR3 NF[5fpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXFNlAuOTByIH7N M4XleFk3KGh? NEnFb2pmdmijbnPld{BCWC2rbnT1Z4VlKGOnbHyg[5Jwf3SqIHnubIljcXSrb36= M{\We|IyPzl{OEi5
MCF7S NYHFW3hLTnWwY4Tpc44hSXO|YYm= NVPzeVhqOcLizszN M4TYblQ5KGh? M176OYRwf26{ZXf1cIF1\XNib4\ldoFtdCCHUt8xJJBzd3SnaX6gcIV3\Wy| MV[yNVU{OzF7NR?=
MCF7 NH;DWmJHfW6ldHnvckBCe3OjeR?= MV:xxsDPxE1? Mn6zOFghcA>? MlX4[I94dnKnZ4XsZZRmeyCxdnXyZYxtKEWUzsGgdJJwfGWrbjDs[ZZmdHN? NIjnTJQzOTV|M{G5OS=>
MCF7S NWjj[2ZjTnWwY4Tpc44hSXO|YYm= MUixxsDPxE1? NI\LdJc4KGR? MmTSZZR1\W63YYTld{B1fW2xcoPwbIVz\SCob4LtZZRqd25iYX7kJJBzd2yrZnXyZZRqd25? NHrpVJkzOTV|M{G5OS=>
MCF7S MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTzdWdjOC53L{Gg{txO NES2R4s4KGR? MnG0SG1UVw>? M4ToOoRm[3KnYYPld{Bk\WyuIHX4dIFve2mxbh?= NGXSfokzOTV|M{G5OS=>
T47D  MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrPdXNsPCCwTR?= MYq0NEBp M2\xPJN2eHC{ZYPz[ZMh[2WubDDndo94fGhibX;k[ZJifGWueR?= MoXZNlE1QDB|OUG=
BT474  M1jpWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVK0JI5O MVK0NEBp M1vEUpN2eHC{ZYPz[ZMh[2WubDDndo94fGhibX;k[ZJifGWueR?= NV3v[HJUOjF2OECzPVE>
T47D  M3[1Z2Z2dmO2aX;uJGF{e2G7 MornNVAhdk1? M2\KVVQxKGh? NI\wXJBld3ewcnXneYxifGW|IFXS{tEheHKxdHXpci=> M3LwVVIyPDhyM{mx
BT474  NHzRXGVHfW6ldHnvckBCe3OjeR?= MWKxNEBvVQ>? MlfGOFAhcA>? NWX6OmNt\G:5boLl[5Vt[XSnczDFVu6yKHC{b4TlbY4> NVqzeYZYOjF2OECzPVE>
MCF7 NHy2coJHfW6ldHnvckBCe3OjeR?= NVjkWmF5OTByIH7N NYPSdY1LPyCm MX\y[YR2[2W|IFXS{tEh\XiycnXzd4lwdiC|aXfubYZq[2GwdHz5 M{LmXVIyOzl4MEm0
T47D  NFTieIdHfW6ldHnvckBCe3OjeR?= NXmzWVdVOTByIH7N NGe5WHQ4KGR? MlfjdoVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> NWjEfG1rOjF|OU[wPVQ>
BT474  M{\BfWZ2dmO2aX;uJGF{e2G7 MoXVNVAxKG6P NW\ZRnVqPyCm MVHy[YR2[2W|IFXS{tEh\XiycnXzd4lwdiC|aXfubYZq[2GwdHz5 M3;oSFIyOzl4MEm0
MDAMB361 MXPGeY5kfGmxbjDBd5NigQ>? NFr3ZpoyODBibl2= MmDVO{Bl MnTkdoVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> NIX3cYEzOTN7NkC5OC=>
MCF7 M1\EVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXyVoh5OC5yMT2xJO69VQ>? MXG3JIQ> M2DQdZJm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M3\zXlIyOzl4MEm0
T47D  Mo\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPBdnpWOC5yMT2xJO69VQ>? Mn\0O{Bl M{izZpJm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MlP2NlE{QTZyOUS=
BT474  NUfhWZQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfVe4ExNjBzLUGg{txO M{fZeVch\A>? NXzCcoJtemWmdXPld{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NGXOOJAzOTN7NkC5OC=>
MDAMB361 NEH2e25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2wMlAyNTFizszN NVLaRY9iPyCm NFvoS5Rz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3;kblIyOzl4MEm0
MCF7 NVPNNG1QTnWwY4Tpc44hSXO|YYm= MUSxNFAhdk1? Mm\pO{Bl M3jUWolv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= NHLmVVMzOTN7NkC5OC=>
T47D  NFn0eGtHfW6ldHnvckBCe3OjeR?= MYexNFAhdk1? NUHxbohmPyCm NHPybINqdmS3Y3XzJI9nKEW{YlKzJIFv\CCHcnLCOEBz\WOncITvdkBmgHC{ZYPzbY9vKGGwZDDzbYdv[WyuaX7n MXOyNVM6PjB7NB?=
BT474  NIm3Z5ZHfW6ldHnvckBCe3OjeR?= NWja[IhxOTByIH7N MYK3JIQ> MXnpcoR2[2W|IH;mJGVz[kJ|IHHu[EBGemKENDDy[YNmeHSxcjDlfJBz\XO|aX;uJIFv\CC|aXfuZYxtcW6p M{jKO|IyOzl4MEm0
MDAMB361 MXnGeY5kfGmxbjDBd5NigQ>? NEWxSXMyODBibl2= NXT6VmVEPyCm NFPy[45qdmS3Y3XzJI9nKEW{YlKzJIFv\CCHcnLCOEBz\WOncITvdkBmgHC{ZYPzbY9vKGGwZDDzbYdv[WyuaX7n MXmyNVM6PjB7NB?=
MCF7 MojYSpVv[3Srb36gRZN{[Xl? NXq0ZY91OTBibl2= NGHvXHM6PiCq NXTkZpk3\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vyqB? Mki2NlE{Pzh|M{O=
MDA-MB-231 Mn\SSpVv[3Srb36gRZN{[Xl? NEDEN3oyOCCwTR?= MoLhPVYhcA>? MYjkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb39CpC=> MU[yNVM4QDN|Mx?=
SK-BR-3 NFXKVHVHfW6ldHnvckBCe3OjeR?= NX32e5dzOTBibl2= MmHJPVYhcA>? NX;NbnpO\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vyqB? M3O2SVIyOzd6M{Oz
MCF-7 M4K4R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[4NVAxKG6P Mn3lO|IwQTZiaB?= MkPwZ4F2e2W|IHPlcIwh[3mlbHWgZZJz\XO2 MlTXNlEzQTl6NkK=
MMQ M3L0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTkWIgxNjByOD22NlUhdk1? NV7zeWVzPzJiaB?= MVnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFnOOZczODdyMEe1OS=>
MMQ MnvnSpVv[3Srb36gRZN{[Xl? MVOwMlAxQC14MkWgcm0> Mli3O|IhcA>? M{nreYlvcGmkaYTzJHBTVCC|ZXPy[ZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NF7PXWQzODdyMEe1OS=>
MMQ MmX4SpVv[3Srb36gRZN{[Xl? M{DoblAvODRvNkK1JI5O NUjZTnFOPzJiaB?= M{nJcYlvcGmkaYTzJGVT|rFiZYjwdoV{e2mxbh?= MXSyNFcxODd3NR?=
MMQ NUDLNoJQTnWwY4Tpc44hSXO|YYm= NEXJdVYxNjB2LU[yOUBvVQ>? NEjmOYU4OiCq MnT5eZBz\We3bHH0[ZMhXEeIzsKzJIFv\CCWR1dOtnJKUSCneIDy[ZN{cW:w NXnvT|VGOjB5MEC3OVU>

... 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]
+ Expand
  • 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]
+ Expand
  • Animal Models: The human breast cancer xenografts MCF-7 in nude mice
  • Formulation: 50 mg/mL in arachis oil
  • Dosages: 5 mg/mouse
  • Administration: s.c. injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (164.8 mM)
Ethanol 100 mg/mL warmed (164.8 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
0.4mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 606.77
Formula

C32H47F5O3S

CAS No. 129453-61-8
Storage powder
in solvent
Synonyms ICI-182780, ZD 9238

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03531645 Not yet recruiting Malignant Neoplasms of Female Genital Organs M.D. Anderson Cancer Center|AstraZeneca|Pfizer April 1 2019 Phase 2
NCT03531645 Not yet recruiting Malignant Neoplasms of Female Genital Organs M.D. Anderson Cancer Center|AstraZeneca|Pfizer April 1 2019 Phase 2
NCT03854903 Not yet recruiting Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer Georgetown University|Pfizer March 2019 Phase 1
NCT03854903 Not yet recruiting Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer Georgetown University|Pfizer March 2019 Phase 1
NCT03691493 Recruiting Anatomic Stage IV Breast Cancer AJCC v8|Estrogen Receptor Positive|HER2/Neu Negative|Metastatic Breast Carcinoma|Metastatic Malignant Neoplasm in the Bone|Progesterone Receptor Positive|Prognostic Stage IV Breast Cancer AJCC v8 Emory University|Pfizer February 8 2019 Phase 2
NCT03803761 Not yet recruiting Anatomic Stage IV Breast Cancer AJCC v8|Breast Carcinoma Metastatic in the Brain|Estrogen Receptor Positive|HER2/Neu Negative|Metastatic Breast Carcinoma|Postmenopausal|Prognostic Stage IV Breast Cancer AJCC v8 National Cancer Institute (NCI) February 12 2019 Phase 1|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.

Estrogen/progestogen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID