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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In DMSO USD 64 In stock
USD 70 In stock
USD 270 In stock
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6 Customer Reviews

  • PTPH1 confers breast cancer cell sensitivity to fulvestrant. E and F, PTPH1 overexpression increases the growth inhibition by fulvestrant. PTPH1 was overexpressed by a Tet-on system or a stable transfection, and resultant cells were incubated with fulvestrant as indicated for about 2 weeks. Colony formed was stained and counted. Results shown are normalized to its own solvent control of Vector and PTPH1-overexpressed cells, respectively (means ± SD; n = 3–5) with insets showing PTPH1 overexpression. *, versus vector or no Tet cells for E and F.

    Mol Cancer Ther 2014 13(1), 230-8. Fulvestrant purchased from Selleck.

    Biochim Biophys Acta, 2018, 1863(6):625-638. Fulvestrant purchased from Selleck.

  •  

    Fulvestrant resistance induced by 6 different ZF-TFs. (A) Drug sensitivity of fulvestrant-selected MCF7 ZF-TF-transduced cells. MCF7 cells transduced with one of six different ZF-TF-expressing retroviruses selected first in puromycin (the transduction selection marker) and then in fulvestrant for 1 month were grown in the absence of fulvestrant for 7 days and then challenged with 100 nM fulvestrant or vehicle (0.1% ethanol) for 21 days followed by crystal violet staining and visualization. Data are representative of triplicate experiments.

    PLoS One 2011 6, e21112. Fulvestrant purchased from Selleck.

    Fulvestrant resistance induced by 6 different ZF-TFs. (B and C) Growth curves of MCF7 and T47D cells in the presence and absence of fulvestrant. Comparison of cell growth rates (cell number, mean +/2 SEM, n = 8; time in days as indicated) of MCF7 and T47D cells stably transduced with control retrovirus or one of six different ZF-TF-expressing retroviruses (7, 19, 64, 70, 83 and 115) in the presence (blue line) or absence (pink line) of fulvestrant.

    PLoS One 2011 6, e21112. Fulvestrant purchased from Selleck.

  • CDK4/6 inhibitor resistance promotes diminished ER expression and activity. (a and b) Proliferation of MCF-7 and MR cells in the presence of different concentrations of ICI (a) or 4-hydroxytamoxifen (4-OHT) (b) was measured by the alamarBlue assay and plotted as % inhibition of proliferation against log concentration of inhibitor. Each data point represents the average value±s.d. of six replicates obtained in three independent experiments. (c) MCF-7 and MR cells were treated with different concentrations of ICI, collected after 24 h and then immunoblotted with the indicated antibodies.

    Oncogene, 2017, 36(16):2255-2264. Fulvestrant purchased from Selleck.

    A: Time dependent loss of MGMT activity in ERα-positive MCF7 and T47D tumor cells but not in ERα-negative MDAMB-468 cells after 1 μmol/L Fulvestrant treatment (upper panel). Concentration dependent inhibition of MGMT activity in MCF7 and T47D cells but not in MDA-MB-468 cells after a 72 hours exposure to fulvestrant (lower panel). The data represents the mean of two independent experiments in duplicate and the last time point (72 hours) as assessed by student's t-test was significant at P < 0.05. B: Decreased MGMT and ER-α protein levels in MCF7 cells after 48 hours and 72 hours fulvestrant exposure. ICI is fulvestrant, also called ICI-182,780. C: Decreased MGMT and ER-α protein levels in T47D cells after 48 hours and 72 hours fulvestrant exposure.

    J Biomed Res, 2016, 30(5):393-410. Fulvestrant purchased from Selleck.

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 NWP2SWJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjRPWMyNjNvMUCwNEBvVQ>? MnvhOFghcA>? Mo\zbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MnXkNlQ6Pzl{OUS=
MCF-7/LTED Ml7mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmxMlMuOTByMDDuUS=> MWS0PEBp NGL4W45qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXvzXYUyOjR7N{myPVQ>
HCC1428 MkDqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPiNU4{NTFyMECgcm0> M1e4UFQ5KGh? M1OxNIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXWyOFk4QTJ7NB?=
HCC1428/LTED NH[2XndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vGWVEvOy1zMECwJI5O NUS0cGQ2PDhiaB?= NYXr[3dDcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWHGPWZrOjR7N{myPVQ>
LCC1 NHLsN4FHfW6ldHnvckBCe3OjeR?= NILTc4EyODBibl2= MUG0PE0yPDRiaB?= NYrNS5Z4[WO2aY\heIV{KFWSUjDzbYdv[Wyrbne= M{jC[VI1QDV6Mke3
LCC9 MU\GeY5kfGmxbjDBd5NigQ>? M4iwW|ExOCCwTR?= MVK0PE0yPDRiaB?= MkHTZYN1cX[jdHXzJHVRWiC|aXfuZYxqdmd? NV\hU5pSOjR6NUiyO|c>
MCF-7  Mlj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjLNVAxKG6P M{LrOVUh\A>? M3ruWIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSxIEGw89yG MUOyOFgyQTV3MB?=
mesangial  NVv3RpdXTnWwY4Tpc44hSXO|YYm= NUfp[lRVOC5zLUGwNEBvVQ>? NGe1OVA1QCCq MXfzeZBxemW|c3XzJHRITi4QskGtbY5lfWOnZDD0fZBmKEmYIHPvcIxi\2Ww MWGyOFc6OzZ|OR?=
Mesangial NGXwb5FHfW6ldHnvckBCe3OjeR?= M{j0TVAvOS1zMECgcm0> MmP5NE42KGh? M{H5RolvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDTcYFlOiCyaH;zdIhwenmuYYTpc44hfmmjIFfQSXI> MUmyOFc6OzZ|OR?=
ER+ MCF-7/2a NFji[oZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzTbHJUUUN3ME2wMlAxPCEQvF2= M1jZeVE2OzJ2OEi0
ER+ MCF-7 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGyNFAhcA>? NHTLd2hKSzVyPUCuNlEhdk1? M3\uUFE2OzJ2OEi0
MCF-7  M1TDVmZ2dmO2aX;uJGF{e2G7 NHXBUocyOMLibl5CpC=> MVK3NkBp MWXy[ZZmenOnczD0bIUh\XO2cn;n[Y4h\W[oZXP0LGlEPTBiMT65JOOYKDFy4pkSPUBOMQ>? NULVZ4FNOjR7MEi2OVI>
MCF-7  NXHrSnJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\5TWM2OMLib3[gZZBxem:6aX3heIVtgSB{IH7N NYLUSIRIOjN2NEizOFY>
H1975  NGTqNnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2L3SlPDqM7:TR?= MXSxJI0> NITNcZJqdmO{ZXHz[ZMhfGinIHfl[ol1cW6rYjDz[Y5{cXSrdnn0fUBw\iCKMUm3OUBk\Wyuc9Mg M3HSVlI1OjZ6OEGw
H1975 NUHCe|hYTnWwY4Tpc44hSXO|YYm= M4nVUFPDqM7:TR?= MX[xJI0> M2G1[pVxemWpdXzheIV{KHSqZTDs[ZZmdCCxZjDM[ZQuP2N? NX7XcIhZOjR{Nki4NVA>
MCF-7  M3zLPWZ2dmO2aX;uJGF{e2G7 M3TwRlExOOLCiX7NxsA> MYq3NkBp MlTEdoV3\XK|ZYOgeIhmKHC{b4TlZ5RqfmViZX\m[YN1KG:oIFWyxsBqdiClZXzsJIlvfmG|aX;u M4HjVFI{QTN4N{ez
MCF-7  M2XqU2Z2dmO2aX;uJGF{e2G7 M{HlWlExOOLCiX7NxsA> MYiyOE81QCCq NXvhXW05\mGlaXzpeIF1\XNiaX72ZZNqd25idHjyc5VocCCPTWDzK{Bud2S3bHH0bY9v NHHzVnIzOzl|Nke3Ny=>
BT474-tet-shMED1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLrNE4yNTVizszN MWC3JIQ> NVHndpZ1cW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MUWyN|k{PjJ|NB?=
ZR75-1-tet-shMED1  MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HFeVAvOS13IN88US=> MkDmO{Bl MX;pcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NInyNWEzOzl|NkKzOC=>
MCF-7-tet-shMED1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPtNE4yNTVizszN Ml;FO{Bl MUTpcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4G5cVI{QTN4MkO0
HepG2  MU\GeY5kfGmxbjDBd5NigQ>? NHm2N28xNjBzLUGwJO69VQ>? NYW0XZpZOThiaNMg MUPhZ5RqfmG2ZYOgeIhmKEWURT3t[YRq[XSnZDD0doFve2O{aYD0bY9vKG:oIFHGNmVT M3:2UVI{PzN|MUi4
MCF-7L  MV;GeY5kfGmxbjDBd5NigQ>? M1r6[FExOCCwTdMg M4K5[|ExKG2rbj:yOEBpNzR6IHi= NYm5OlA4emW|dXz0d{BqdiCHR1\SMEBJTVJ{IHHu[EBJTVJ|IIDoc5NxcG:{eXzheIlwdiCjdDDwdo9td26pZXSg[Zhxd3O3cnW= NFn3bI0zOzZ6NkSxOi=>
MCF-7L  M{j1dGZ2dmO2aX;uJGF{e2G7 MUWxNFAhdk4EoB?= MYG0PEBp MofQbY5lfWOnczD1dJJm\3WuYYTpc44hd2ZibWLORUBw\iCHR1\SJIxq\2GwZDDIRk1GT0Z? MYWyN|Y5PjRzNh?=
MCF-7L NGjYVZRHfW6ldHnvckBCe3OjeR?= NV7OcGpyOTByIH7NxsA> MnHEOFghcA>? MUjpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT NIj0S24zOzZ6NkSxOi=>
C4-12  M2PicWZ2dmO2aX;uJGF{e2G7 NVG3R4h1OTByIH7NxsA> MVm0PEBp NFPsXHVqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU M3TwZVI{Pjh4NEG2
MCF-7L NHvOPGxHfW6ldHnvckBCe3OjeR?= NX;1SGVxOTByIH7NxsA> M1nGdFI1KGh? MnXEbY5lfWOnczDFS2ZTKHCqb4PwbI9zgWyjdHnvckBz\XG3aYLl[EBJSi2HR1[g[pVv[3Srb36= M3nDR|I{Pjh4NEG2
MMQ  MX3GeY5kfGmxbjDBd5NigQ>? M1rIflAuPjJ3IH7N NEmxNFU4OiCq NIfibnlld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDld5Rzd2enbjDy[YNmeHSxcj5OtUApTVMQsTm= MVqyN|UzOzN3Nx?=
H1975  M1S4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLnNE4{OTJ3LUGwJO69VQ>? NGPTfHo3KGR? NVrYVFhDcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHzmc4szOzN7OUm1Oy=>
H1975  MnXTRZBweHSxc3nzJGF{e2G7 NGXHcm0zODBibl2= MmexO|IhcA>? NGnOToxmdmijbnPld{BmemyxdHnubYIhcW6mdXPl[EBieG:ydH;zbZM> MVeyN|M6QTl3Nx?=
MCF-7  NVTVfoExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofsNVAwOTByL{GwNFAhdk1? M1nUT|IwPC94IHS= MlfBSG1UVw>? MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ Ml;RNlM{OTN3ME[=
MCF-7  MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjPNVAxKG6P NIjleVY1KGR? NFLiS3lFVVOR MnTTbY5lfWOnczDhJIhq\2incjDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKHSqZTDHNUBxcGG|ZdMg Mm\xNlM{OTN3ME[=
MLO-Y4  MVfGeY5kfGmxbjDBd5NigQ>? NEXXbYEyyqEQvF2= M{fkNFEhcA>? M3XSS4lvcGmkaYTzJGUzNWmwZIXj[YQhS3h2MzDlfJBz\XO|aX;u M2PtdlI{OjR5MEW3
MCF-7 M2Dofmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn2zNVAxKG6P M3HiNlQ5KGh? MniwZYJzd2ejdHXzJJRp\SCycn;sbYZmemG2aY\lJIVn\mWldDDv[kBud2SncnH0[UBvcXS{b4PheIl3\SC|dILld5M> NIPoVZMzOzJzNke0OC=>
TG1-1  M4jubmZ2dmO2aX;uJGF{e2G7 MVOxxsDPxE1? MVeyOEBp MoXjZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x NWXyXXIzOjNyOEi2NFc>
TG1-1  NVW0bXdNTnWwY4Tpc44hSXO|YYm= Mon5NeKh|ryP MmnMNlQhcA>? NIq2Ro9i[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKFCLM1u= NUOzXlQ4OjNyOEi2NFc>
MCF7 NI\D[WJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjxRY5XOTByIH7N NVftcJB4PDhiaB?= NWTYeZUxdGWjZIOgeI8h[SC|aX3pcIFzKGyxc4OgbY4he3W{dnn2ZYwh[XNid3n0bEBld3ixcoXibYNqdiCjbH;u[S=> NULN[FVLOjNyN{eyOFk>
MCF7 M3TnZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWqxNFAhdk1? M4HodVQ5KGh? NX7RNJNE\W6qYX7j[ZMhdnW2bHnuMY1m\GmjdHXkJINmdGxiZHXheIg> M3nUeVI{ODd5MkS5
MCF-7  NFfWWmFHfW6ldHnvckBCe3OjeR?= MknDOkBp NUXtfXo{TE2VTx?= NVjrWXZC[XS2ZX71ZZRmeyC2aHWg[ox2\GmxeH;ubYwuKG:{IH\lcohmgGGvaXStbY5lfWOnZDDpcoNz\WG|ZTDpckBucVJvMkGg[ZhxemW|c3nvci=> NGXTO|gzOzB3MkCzOi=>
MCF-7 NIXUUINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPSSW1DOTByIH7NM|Eh|ryP NWPWWXg1PSCm M1exSIlvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kAyP87{LXXzeJJi\GmxbB?= NVHk[olPOjJ7OEK3OlU>
MCF-7 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\4elQyODBibl2= NX;DbZQ4PSCm MnXRbY5pcWKrdIOgeIhmKHO2aX31cIF1cW:wIH;mJIZ2e2G{aXXsbY4hUA>? MYGyNlk5Ojd4NR?=
1471.1 MknvSpVv[3Srb36gRZN{[Xl? M3vYNFExOCCwTR?= M2ftW|EhcA>? M3TST2V1V0kEoB?= MX\0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= M2e1TFIzQDZ7MUC2
MCF-7 M{X3OmZ2dmO2aX;uJGF{e2G7 MXKxNFAhdk1? NIDwXZgyKGh? MVzFeG9JyqB? NFz1XW91[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> MkLrNlI5PjlzME[=
HeLa MVfGeY5kfGmxbjDBd5NigQ>? NYnOO3Y3OTByIH7N M2\pbVEhcA>? MmHsSZRQUMLi Mnj3eIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu MWGyNlg3QTFyNh?=
COS-7  NGjPbVhHfW6ldHnvckBCe3OjeR?= M{K0V|ExOCCwTR?= NHnU[m0yKGh? MnjESZRQUMLi NInPPZN1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> MYeyNlg3QTFyNh?=
BG1L-OHTLT  M{jMO2Z2dmO2aX;uJGF{e2G7 NVfU[JdXOTEEoH7N NXe2RVg2OjUEoHlCpC=> NIPSPI5qdmirYnn0d{BGWs7zIHX4dJJme3Orb36= NGnIWVczOjZ3MkW1PC=>
BG1L-ICILT M1jo[GZ2dmO2aX;uJGF{e2G7 M3G3OlExyqCwTR?= Mnq1NlTDqGkEoB?= MXjpcohq[mm2czDFVu6yKGW6cILld5Nqd25? MVuyNlY2OjV3OB?=
PC-9 M{e0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDGSYMxNjByMz2zNEDPxE1? NYXS[mVRPDhiaB?= NIjLNW1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1vFe|IzPTZyNkO0
H1650 NUPEeHdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4n3NFAvODB|LUOwJO69VQ>? NH\aZpU1QCCq MY\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4XMblIzPTZyNkO0
H1975 NYLzd2pzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnxZlI6OC5yMEOtN|Ah|ryP M1;xWlQ5KGh? NH3aboxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MmHkNlI2PjB4M{S=
H1975 MUnGeY5kfGmxbjDBd5NigQ>? MorGN:Kh|ryP MoLTN{Bp NU\ROJBY[WK{b3fheIV{KHSqZTDwbI9{eGixLVXHSnIhcW6mdXP0bY9vKGK7IHXzeJJw\2Ww M2fufVIzPTZyNkO0
H1975 NFHFOnRHfW6ldHnvckBCe3OjeR?= MkfkN:Kh|ryP MVi3JIQ> MVXpcoR2[2W|IFXHSnIh\XiycnXzd4lwdg>? NV7Ndo9bOjJ3NkC2N|Q>
HTR-8 MXrGeY5kfGmxbjDBd5NigQ>? M1vjRVHDqM7:TR?= MoL0NU01QCCq NXvoSWJj\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gTWdHSlB5IH3SUmE> MXyyNlM5OzFzMR?=
JEG-3 M3HXUWZ2dmO2aX;uJGF{e2G7 MoG5NeKh|ryP M33qXFEuPDhiaB?= MV7kc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCLR1\CVFchdVKQQR?= NFPIVW0zOjN6M{GxNS=>
Huh7 MVLGeY5kfGmxbjDBd5NigQ>? MVK1NOKh|ryP NIHqZ4s1QCCq NXfteYZ4cW6qaXLpeJMh\2WwaYP0[YlvNW2nZHnheIVlKFCRTkGgeJJidnOjY4TpeoF1cW:w MYWyNlMxPDJ7Nh?=
201T MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjVS|Z2PSEQvF2= NFzPeIY4OiCq NFLzVFRqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnHu[IV1[W6rYh?= MnLYNlIzPTh2N{[=
A549  MoTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYK1JO69VQ>? MnXnO|IhcA>? NHP6SYFqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnHu[IV1[W6rYh?= MUCyNlI2QDR5Nh?=
MCF-7 MY\GeY5kfGmxbjDBd5NigQ>? NFXSc3oyyqEQvF2= NHL5XmgzPCCqwrC= NXjq[205\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi NU\HOJkyOjJyNEmzNVY>
HCC-1428 MUDGeY5kfGmxbjDBd5NigQ>? NFnzU3kyyqEQvF2= NXnSdVhUOjRiaNMg MnXl[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh NHvQeGszOjB2OUOxOi=>
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MCF7S M3G4NGZ2dmO2aX;uJGF{e2G7 NFvST3oyyqEQvF2= MYm3JIQ> M1vRUIF1fGWwdXH0[ZMhfHWvb4LzdIhmemViZn;ycYF1cW:wIHHu[EBxem:uaX\ldoF1cW:w M3LDSFIyPTN|MUm1
MCF7S MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zBV|AvPS9zIN88US=> MXS3JIQ> NUf0RmhYTE2VTx?= M4DHTYRm[3KnYYPld{Bk\WyuIHX4dIFve2mxbh?= M2nicFIyPTN|MUm1
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BT474  NWmzN3R3TnWwY4Tpc44hSXO|YYm= NGLwPFMyOCCwTR?= Ml6yOFAhcA>? Mn;u[I94dnKnZ4XsZZRmeyCHUt8xJJBzd3SnaX6= M3G3WlIyPDhyM{mx
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T47D  NUPuSmM1TnWwY4Tpc44hSXO|YYm= M3;2TVExOCCwTR?= MYO3JIQ> NXzldVI4emWmdXPld{BGWs7zIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? MkHJNlE{QTZyOUS=
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MDAMB361 Mlf0SpVv[3Srb36gRZN{[Xl? MX6xNFAhdk1? MYK3JIQ> NXzBRWtzemWmdXPld{BGWs7zIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? NHXxdYUzOTN7NkC5OC=>
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BT474  MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[wMlAyNTFizszN MVm3JIQ> MmrYdoVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M4nYfFIyOzl4MEm0
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MCF7 MXfGeY5kfGmxbjDBd5NigQ>? NWOxWlIyOTByIH7N NYH0Z3JjPyCm M4jlXYlv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= MmLyNlE{QTZyOUS=
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... Click to View More Cell Line Experimental Data

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):
5% DMSO+95% Corn oil
For best results, use promptly after mixing.
30mg/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

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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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02340221 Active not recruiting Breast Cancer Hoffmann-La Roche April 9 2015 Phase 3
NCT01597388 Active not recruiting Advanced Metastatic Breast Cancer AstraZeneca May 8 2012 Phase 1
NCT00099437 Active not recruiting Breast Cancer AstraZeneca February 8 2005 Phase 3
NCT03377101 Withdrawn Estrogen Receptor Positive|HER2/Neu Negative|Progesterone Receptor Positive|Stage IV Breast Cancer AJCC v6 and v7 National Cancer Institute (NCI) August 7 2018 Phase 2
NCT01610284 Active not recruiting Breast Cancer Novartis Pharmaceuticals|Novartis August 7 2012 Phase 3
NCT02953860 Recruiting Breast Cancer University of Colorado Denver|United States Department of Defense July 6 2017 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