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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Cited by 10 Publications

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 Ml\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7aWlAyNjNvMUCwNEBvVQ>? MVi0PEBp NHLzelZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFjwb2szPDl5OUK5OC=>
MCF-7/LTED MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYexMlMuOTByMDDuUS=> NXTrcY1xPDhiaB?= NXrHVWpRcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGnzOVAzPDl5OUK5OC=>
HCC1428 NEfSZmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX36VYw{OS5|LUGwNFAhdk1? MnzyOFghcA>? M1LrbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUSyOFk4QTJ7NB?=
HCC1428/LTED MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnkNU4{NTFyMECgcm0> MnPWOFghcA>? M1fhbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mnv1NlQ6Pzl{OUS=
LCC1 M1TuU2Z2dmO2aX;uJGF{e2G7 MnviNVAxKG6P M1nYdFQ5NTF2NDDo MUDhZ5RqfmG2ZYOgWXBTKHOrZ37hcIlv\w>? Mmf1NlQ5PTh{N{e=
LCC9 NHnqeIRHfW6ldHnvckBCe3OjeR?= Mn;QNVAxKG6P MW[0PE0yPDRiaB?= NULTS2NJ[WO2aY\heIV{KFWSUjDzbYdv[Wyrbne= NVjsenF[OjR6NUiyO|c>
MCF-7  NYmzW5BiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:0[JgyODBibl2= M4HmSlUh\A>? NVr0W4RKcW6qaXLpeJMh[2WubDDndo94fGhidH:gNVDwxIV? NI\mb4IzPDhzOUW1NC=>
mesangial  MknrSpVv[3Srb36gRZN{[Xl? NV7ETXdCOC5zLUGwNEBvVQ>? NW\UdlROPDhiaB?= NGPhSmV{fXCycnXzd4V{KFSJRj5OtlEucW6mdXPl[EB1gXCnIFnWJINwdGyjZ3Xu M1vPelI1Pzl|NkO5
Mesangial NFnXSmtHfW6ldHnvckBCe3OjeR?= NX;je3liOC5zLUGwNEBvVQ>? NGHSU4UxNjViaB?= MkK3bY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIGPtZYQzKHCqb4PwbI9zgWyjdHnvckB3cWFiR2DFVi=> M1;sUlI1Pzl|NkO5
ER+ MCF-7/2a MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoK5TWM2OD1yLkCwOEDPxE1? MUOxOVMzPDh6NB?=
ER+ MCF-7 MnLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnRR4MzODBiaB?= NEjBRnpKSzVyPUCuNlEhdk1? NH\qZVcyPTN{NEi4OC=>
MCF-7  NEnkcZhHfW6ldHnvckBCe3OjeR?= MmK5NVDDqG6PwrC= MXe3NkBp MYHy[ZZmenOnczD0bIUh\XO2cn;n[Y4h\W[oZXP0LGlEPTBiMT65JOOYKDFy4pkSPUBOMQ>? MWGyOFkxQDZ3Mh?=
MCF-7  M{jCcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3iVHBKSzVywrDv[kBieHC{b4jpcYF1\Wy7IEKgcm0> NY\pTZRNOjN2NEizOFY>
H1975  MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnWZmpsO8LizszN NX7kS2lzOSCv M2PPS4lv[3KnYYPld{B1cGViZ3XmbZRqdmmkIIPlcpNqfGm4aYT5JI9nKEhzOUe1JINmdGy|wrC= M1PKeFI1OjZ6OEGw
H1975 MnTDSpVv[3Srb36gRZN{[Xl? NX3UPZJbO8LizszN MX[xJI0> NV7rfmRxfXC{ZXf1cIF1\XNidHjlJIxmfmWuIH;mJGxmfC15Yx?= NHPieGYzPDJ4OEixNC=>
MCF-7  M3\vfWZ2dmO2aX;uJGF{e2G7 NVvLNVZlOTBy4pEJcm3DqA>? MmGzO|IhcA>? M4TNSpJmfmW{c3XzJJRp\SCycn;0[YN1cX[nIHXm[oVkfCCxZjDFNuKhcW5iY3XscEBqdn[jc3nvci=> M{nBcVI{QTN4N{ez
MCF-7  MXzGeY5kfGmxbjDBd5NigQ>? M{TZdlExOOLCiX7NxsA> M33Sc|I1NzR6IHi= NFzJOpFn[WOrbHn0ZZRmeyCrbo\hd4lwdiC2aILveYdpKE2PUIOnJI1w\HWuYYTpc44> MUmyN|k{Pjd5Mx?=
BT474-tet-shMED1 NG[wZ29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPkU4sxNjFvNTFOwG0> NELhV4w4KGR? NVfBNGxkcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MXGyN|k{PjJ|NB?=
ZR75-1-tet-shMED1  M1nnRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKwMlEuPSEQvF2= MYi3JIQ> NEHMc2pqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NH\TZnAzOzl|NkKzOC=>
MCF-7-tet-shMED1 NUL5ZYJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HOclAvOS13IN88US=> MlPvO{Bl NGT4cGNqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MUmyN|k{PjJ|NB?=
HepG2  MmXTSpVv[3Srb36gRZN{[Xl? MlKzNE4xOS1zMDFOwG0> NEfHSnUyQCCqwrC= MWThZ5RqfmG2ZYOgeIhmKEWURT3t[YRq[XSnZDD0doFve2O{aYD0bY9vKG:oIFHGNmVT MXqyN|c{OzF6OB?=
MCF-7L  NF2xfHdHfW6ldHnvckBCe3OjeR?= M2[5T|ExOCCwTdMg MUWxNEBucW5xMkSgbE81QCCq MYjy[ZN2dHS|IHnuJGVITlJuIFjFVlIh[W6mIFjFVlMheGixc4Doc5J6dGG2aX;uJIF1KHC{b3zvcodm\CCneIDvd5Vz\Q>? MofVNlM3QDZ2MU[=
MCF-7L  MYrGeY5kfGmxbjDBd5NigQ>? MYqxNFAhdk4EoB?= M3u0dVQ5KGh? NV;VTVdlcW6mdXPld{B2eHKnZ4XsZZRqd25ib3[gcXJPSSCxZjDFS2ZTKGyrZ3Hu[EBJSi2HR1[= M3nFOFI{Pjh4NEG2
MCF-7L MXnGeY5kfGmxbjDBd5NigQ>? MXyxNFAhdk4EoB?= MXS0PEBp Mn:zbY5lfWOnczDFS2ZTKG[jbXnsfUBu\W2kZYKgZYN1cX[jdHnvckBz\XG3aYLl[EBGWg>? NEfwUVMzOzZ6NkSxOi=>
C4-12  MVTGeY5kfGmxbjDBd5NigQ>? MYWxNFAhdk4EoB?= NVznVYhTPDhiaB?= NYjWSZZDcW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= NGH5O5IzOzZ6NkSxOi=>
MCF-7L NYXSNmZITnWwY4Tpc44hSXO|YYm= M2f5VFExOCCwTdMg MYmyOEBp MlXYbY5lfWOnczDFS2ZTKHCqb4PwbI9zgWyjdHnvckBz\XG3aYLl[EBJSi2HR1[g[pVv[3Srb36= MlLyNlM3QDZ2MU[=
MMQ  MXLGeY5kfGmxbjDBd5NigQ>? MV[wMVYzPSCwTR?= M1HFXVczKGh? NH;SV4Rld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDld5Rzd2enbjDy[YNmeHSxcj5OtUApTVMQsTm= MVOyN|UzOzN3Nx?=
H1975  M3HwW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVSwMlMyOjVvMUCg{txO MVm2JIQ> MYnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NH65em4zOzN7OUm1Oy=>
H1975  NV3mbGNCSXCxcITvd4l{KEG|c3H5 MYKyNFAhdk1? MlTEO|IhcA>? NFjVbIdmdmijbnPld{BmemyxdHnubYIhcW6mdXPl[EBieG:ydH;zbZM> NGT5bo8zOzN7OUm1Oy=>
MCF-7  MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3v4eFExNzFyMD:xNFAxKG6P NF21Z5ozNzRxNjDk MkHqSG1UVw>? M{\kNYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= M1nlVVI{OzF|NUC2
MCF-7  MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2npZVExOCCwTR?= NYPuNpRLPCCm M1fhVmROW09? NIDsUJRqdmS3Y3XzJIEhcGmpaHXyJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5idHjlJGcyKHCqYYPlxsA> NWTUd5BrOjN|MUO1NFY>
MLO-Y4  MUXGeY5kfGmxbjDBd5NigQ>? Mn:0NeKh|ryP MmfaNUBp MWrpcohq[mm2czDFNk1qdmS3Y3XkJGN5PDNiZYjwdoV{e2mxbh?= NX3MZ3I{OjN{NEewOVc>
MCF-7 NWfuVGNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYKxNFAhdk1? MWO0PEBp NEDvWopi[nKxZ3H0[ZMhfGinIIDyc4xq\mW{YYTpeoUh\W[oZXP0JI9nKG2xZHXyZZRmKG6rdILvd4F1cX[nIIP0doV{ew>? NIL3NnMzOzJzNke0OC=>
TG1-1  NYPrW|hETnWwY4Tpc44hSXO|YYm= Mnq5NeKh|ryP M1XNZVI1KGh? MoToZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x NETiclkzOzB6OE[wOy=>
TG1-1  MnH1SpVv[3Srb36gRZN{[Xl? NHzvTHYyyqEQvF2= MojJNlQhcA>? M{jzV4Fjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhWEl|Sx?= M4n5R|I{ODh6NkC3
MCF7 NH7OT5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUCxNFAhdk1? NEf5RYI1QCCq M2X1boxm[WS|IITvJIEhe2mvaXzhdkBtd3O|IHnuJJN2en[rdnHsJIF{KHerdHig[I95d3K3YnnjbY4h[WyxbnW= NYj3R|lrOjNyN{eyOFk>
MCF7 M{\ITmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOxNFAhdk1? MmPhOFghcA>? MnXK[Y5p[W6lZYOgcpV1dGmwLX3l[IlifGWmIHPlcIwh\GWjdHi= MnX3NlMxPzd{NEm=
MCF-7  MlHUSpVv[3Srb36gRZN{[Xl? MkDUOkBp NXTYTpNNTE2VTx?= NV\MOXFN[XS2ZX71ZZRmeyC2aHWg[ox2\GmxeH;ubYwuKG:{IH\lcohmgGGvaXStbY5lfWOnZDDpcoNz\WG|ZTDpckBucVJvMkGg[ZhxemW|c3nvci=> Mkm2NlMxPTJyM{[=
MCF-7 M{fFcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXixNFAhdk1xMTFOwG0> M3K0dlUh\A>? M2fHTIlvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kAyP87{LXXzeJJi\GmxbB?= MWGyNlk5Ojd4NR?=
MCF-7 NWjXSJJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTEPGcyOTByIH7N MnzTOUBl Mn[1bY5pcWKrdIOgeIhmKHO2aX31cIF1cW:wIH;mJIZ2e2G{aXXsbY4hUA>? NGrWb3EzOjl6Mke2OS=>
1471.1 MoTBSpVv[3Srb36gRZN{[Xl? MVuxNFAhdk1? Ml\hNUBp MkS5SZRQUMLi NGnWR3d1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> NUXTS4VkOjJ6NkmxNFY>
MCF-7 NFTaV|VHfW6ldHnvckBCe3OjeR?= NYfIcFd{OTByIH7N NFPYWI8yKGh? NYDNXnppTXSRSNMg M4nF[5Ric2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> NYTETldROjJ6NkmxNFY>
HeLa Ml:2SpVv[3Srb36gRZN{[Xl? MXqxNFAhdk1? M3nOeFEhcA>? M{HObmV1V0kEoB?= NVflVYIzfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv M4[2[lIzQDZ7MUC2
COS-7  NWH1T3NPTnWwY4Tpc44hSXO|YYm= MnzKNVAxKG6P NHnVWIwyKGh? M4i3Z2V1V0kEoB?= MnnReIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu M{K3VFIzQDZ7MUC2
BG1L-OHTLT  MnHPSpVv[3Srb36gRZN{[Xl? MYCxNOKhdk1? NXPPOWU4OjUEoHlCpC=> MYLpcohq[mm2czDFVu6yKGW6cILld5Nqd25? NVvOfYw6OjJ4NUK1OVg>
BG1L-ICILT MUHGeY5kfGmxbjDBd5NigQ>? MVmxNOKhdk1? M2HFWlI1yqCqwrC= NGHwWlFqdmirYnn0d{BGWs7zIHX4dJJme3Orb36= MYOyNlY2OjV3OB?=
PC-9 MnrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV6wMlAxOy1|MDFOwG0> NEnnepg1QCCq NVriOVZScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Ml\nNlI2PjB4M{S=
H1650 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7zeVIxNjByMz2zNEDPxE1? M1P1[VQ5KGh? NX;Z[I5ZcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MUeyNlU3ODZ|NB?=
H1975 M{j3Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moe5NE4xODNvM{Cg{txO M3fLTlQ5KGh? NVzuepQycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGfobYYzOjV4ME[zOC=>
H1975 M4THU2Z2dmO2aX;uJGF{e2G7 NYXEPVk2O8LizszN NES3cGc{KGh? Mn;KZYJzd2ejdHXzJJRp\SCyaH;zdIhwNUWJRmKgbY5lfWO2aX;uJIJ6KGW|dILv[4Vv M1Syd|IzPTZyNkO0
H1975 NX\UfHRmTnWwY4Tpc44hSXO|YYm= M3XIblPDqM7:TR?= Ml7SO{Bl M4npeIlv\HWlZYOgSWdHWiCneIDy[ZN{cW:w MmSwNlI2PjB4M{S=
HTR-8 M1LFTWZ2dmO2aX;uJGF{e2G7 MV6xxsDPxE1? MkLFNU01QCCq MoTj[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSVfGRnA4KG2UTlG= MonGNlI{QDNzMUG=
JEG-3 MYLGeY5kfGmxbjDBd5NigQ>? Mn2zNeKh|ryP M2rxNVEuPDhiaB?= NGDFR3Zld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDJS2ZDWDdibWLORS=> NGTaXZYzOjN6M{GxNS=>
Huh7 MV7GeY5kfGmxbjDBd5NigQ>? M{PoNVUxyqEQvF2= MWi0PEBp M2rLWYlvcGmkaYTzJIdmdmm|dHXpck1u\WSrYYTl[EBRV05zIITyZY5{[WO2aY\heIlwdg>? M2jzfFIzOzB2Mkm2
201T MmrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljvOUDPxE1? NGrBXlE4OiCq MkOxbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? MWCyNlI2QDR5Nh?=
A549  MoTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PhTFUh|ryP NGn0PXA4OiCq NGLr[|FqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnHu[IV1[W6rYh?= NV3DS2JmOjJ{NUi0O|Y>
MCF-7 NE\OPZZHfW6ldHnvckBCe3OjeR?= NH[1RpQyyqEQvF2= M1jv[|I1KGkEoB?= NWTDSlBs\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi NVLOWmxCOjJyNEmzNVY>
HCC-1428 M2TZfmZ2dmO2aX;uJGF{e2G7 MnPDNeKh|ryP Mkn1NlQhcMLi MoTS[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh MUmyNlA1QTNzNh?=
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MDAMB361 Ml\BSpVv[3Srb36gRZN{[Xl? MlLSNVAxKG6P NW\0bGM3PyCm M{LWcZJm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> NGfofW0zOTN7NkC5OC=>
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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):
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

If you have any other enquiries, please leave a message.

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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