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.

Size Price Stock Quantity  
In DMSO USD 64 In stock
USD 70 In stock
USD 270 In stock
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5 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.

     

    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, 2016. 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 Mlu0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVKxMlMuOTByMDDuUS=> NEfZUYg1QCCq NHfOfm1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1zDRlI1QTd7Mkm0
MCF-7/LTED MnfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3u5RlEvOy1zMECwJI5O MlWxOFghcA>? MVXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGTSdWszPDl5OUK5OC=>
HCC1428 NWWySHM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHlNU4{NTFyMECgcm0> NWj4bm5PPDhiaB?= M1XZN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NX7CTY06OjR7N{myPVQ>
HCC1428/LTED MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTPWHYyOS5|LUGwNFAhdk1? NEPiOZk1QCCq M{nJZolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVXPfVRWOjR7N{myPVQ>
LCC1 NVrWeYU{TnWwY4Tpc44hSXO|YYm= M3i4XFExOCCwTR?= MkD5OFguOTR2IHi= NG\Mb5Zi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= Mm\3NlQ5PTh{N{e=
LCC9 NFnkdVJHfW6ldHnvckBCe3OjeR?= MYKxNFAhdk1? NVfpdJcyPDhvMUS0JIg> NUm4WY9X[WO2aY\heIV{KFWSUjDzbYdv[Wyrbne= M1LMfVI1QDV6Mke3
MCF-7  MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTNNVAxKG6P NEfDbFM2KGR? MnvtbY5pcWKrdIOgZ4VtdCCpcn;3eIghfG9iMUFvwKU> MlfmNlQ5OTl3NUC=
mesangial  NInRVYNHfW6ldHnvckBCe3OjeR?= NUPjNI5sOC5zLUGwNEBvVQ>? M{jsWFQ5KGh? NVe4[JhHe3WycILld5NmeyCWR1[t{tIyNWmwZIXj[YQhfHmyZTDJWkBkd2yuYXflci=> MoXwNlQ4QTN4M{m=
Mesangial M4rVdGZ2dmO2aX;uJGF{e2G7 MU[wMlEuOTByIH7N M2H0SVAvPSCq M3nrZolvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDTcYFlOiCyaH;zdIhwenmuYYTpc44hfmmjIFfQSXI> MnPVNlQ4QTN4M{m=
ER+ MCF-7/2a NECwOVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PFV2lEPTB;MD6wNFQh|ryP MnnFNVU{OjR6OES=
ER+ MCF-7 M1LG[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[4NlJoOjByIHi= M2S0UGlEPTB;MD6yNUBvVQ>? MXexOVMzPDh6NB?=
MCF-7  NV[2VYJbTnWwY4Tpc44hSXO|YYm= NIHJPZgyOMLibl5CpC=> NFHROIM4OiCq M1nJbJJmfmW{c3XzJJRp\SCnc4Tyc4dmdiCnZn\lZ5QpUUN3MDCxMlkhy5diMUFijLI6KE1r Mn7QNlQ6ODh4NUK=
MCF-7  MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\LTWM2OMLib3[gZZBxem:6aX3heIVtgSB{IH7N MnfONlM1PDh|NE[=
H1975  M1W2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PMU|PDqM7:TR?= NGDQfWUyKG1? MUTpcoNz\WG|ZYOgeIhmKGenZnn0bY5q[iC|ZX7zbZRqfmm2eTDv[kBJOTl5NTDj[Yxte8Li MofCNlQzPjh6MUC=
H1975 Ml:1SpVv[3Srb36gRZN{[Xl? M13nNlPDqM7:TR?= NIi4dZQyKG1? NF;ERWR2eHKnZ4XsZZRmeyC2aHWgcIV3\Wxib3[gUIV1NTel M{HFSFI1OjZ6OEGw
MCF-7  MUXGeY5kfGmxbjDBd5NigQ>? M375N|ExOOLCiX7NxsA> NIPE[FI4OiCq M3HK[ZJmfmW{c3XzJJRp\SCycn;0[YN1cX[nIHXm[oVkfCCxZjDFNuKhcW5iY3XscEBqdn[jc3nvci=> Mo\YNlM6OzZ5N{O=
MCF-7  MkfzSpVv[3Srb36gRZN{[Xl? MmnRNVAx6oDLbl5CpC=> Mk\GNlQwPDhiaB?= MVrmZYNqdGm2YYTld{Bqdn[jc3nvckB1cHKxdXfoJG1OWHNpIH3v[JVt[XSrb36= M4DhNVI{QTN4N{ez
BT474-tet-shMED1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV22UYw1OC5zLUWg{txO M2Toclch\A>? NFzy[5BqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M4W2dFI{QTN4MkO0
ZR75-1-tet-shMED1  MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{i2dVAvOS13IN88US=> Mlv2O{Bl NGDNVI5qdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M4XLdFI{QTN4MkO0
MCF-7-tet-shMED1 M4r2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUSwMlEuPSEQvF2= NV3TSWh5PyCm M3TUVIlv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MVeyN|k{PjJ|NB?=
HepG2  M1jjeGZ2dmO2aX;uJGF{e2G7 NXXpZ4ViOC5yMT2xNEDPxE1? NY\o[ZpWOThiaNMg M4HqVYFkfGm4YYTld{B1cGViRWLFMY1m\GmjdHXkJJRz[W6|Y4LpdJRqd25ib3[gRWYzTVJ? M2TUZ|I{PzN|MUi4
MCF-7L  NGLoZ21HfW6ldHnvckBCe3OjeR?= MkLZNVAxKG6PwrC= MlKzNVAhdWmwL{K0JIgwPDhiaB?= M2fm[pJme3WudIOgbY4hTUeIUjygTGVTOiCjbnSgTGVTOyCyaH;zdIhwenmuYYTpc44h[XRicILvcI9v\2WmIHX4dI9{fXKn M3zjUVI{Pjh4NEG2
MCF-7L  NGLIV4tHfW6ldHnvckBCe3OjeR?= NVTtd4VZOTByIH7NxsA> NHLJUGw1QCCq NHLE[GpqdmS3Y3XzJJVxemWpdXzheIlwdiCxZjDtVm5CKG:oIFXHSnIhdGmpYX7kJGhDNUWJRh?= NHvDVFIzOzZ6NkSxOi=>
MCF-7L M3TCd2Z2dmO2aX;uJGF{e2G7 M2jqUFExOCCwTdMg MWK0PEBp NIjrSnlqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU MYCyN|Y5PjRzNh?=
C4-12  M1PuNWZ2dmO2aX;uJGF{e2G7 NIfKV2YyODBibl5CpC=> MVS0PEBp NH\leYxqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU MkHzNlM3QDZ2MU[=
MCF-7L NEPZcZJHfW6ldHnvckBCe3OjeR?= MnrlNVAxKG6PwrC= MnOwNlQhcA>? MoX6bY5lfWOnczDFS2ZTKHCqb4PwbI9zgWyjdHnvckBz\XG3aYLl[EBJSi2HR1[g[pVv[3Srb36= M{fTSlI{Pjh4NEG2
MMQ  MYHGeY5kfGmxbjDBd5NigQ>? NF3JR5MxNTZ{NTDuUS=> M4H2RlczKGh? MVPkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCnc4Tyc4dmdiC{ZXPldJRwei4QsTCoSXLPuSl? NHLOdmwzOzV{M{O1Oy=>
H1975  NIPne3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTDNYVYOC5|MUK1MVExKM7:TR?= M{LFfVYh\A>? NVTRe|lScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFL2d4UzOzN7OUm1Oy=>
H1975  M4jOOGFxd3C2b4Ppd{BCe3OjeR?= MYmyNFAhdk1? Moe4O|IhcA>? M{PLTYVvcGGwY3XzJIVzdG:2aX7pZkBqdmS3Y3XkJIFxd3C2b4Ppdy=> MUWyN|M6QTl3Nx?=
MCF-7  MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;TNVAwOTByL{GwNFAhdk1? Ml33Nk81NzZiZB?= MU\EUXNQ MVzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ NHTmR5czOzNzM{WwOi=>
MCF-7  MorZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVyxNFAhdk1? MnexOEBl Mn3RSG1UVw>? MXjpcoR2[2W|IHGgbIlocGW{IIDyc5BwenSrb36gc4Yh[2WubIOgbY4hfGinIFexJJBp[XOnwrC= NH\nTnkzOzNzM{WwOi=>
MLO-Y4  MVPGeY5kfGmxbjDBd5NigQ>? MUmxxsDPxE1? NInzTpMyKGh? MkewbY5pcWKrdIOgSVIucW6mdXPl[EBEgDR|IHX4dJJme3Orb36= MVGyN|I1PzB3Nx?=
MCF-7 M3;kPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7lNVAxKG6P MoOzOFghcA>? M4\XOYFjem:pYYTld{B1cGVicILvcIln\XKjdHn2[UBm\m[nY4Sgc4YhdW:mZYLheIUhdmm2cn;zZZRqfmVic4Ty[ZN{ MljSNlMzOTZ5NES=
TG1-1  NUTaNFVsTnWwY4Tpc44hSXO|YYm= MWWxxsDPxE1? NXXCcoxQOjRiaB?= NITjToVi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKEiLRj2x{tE> MlHnNlMxQDh4MEe=
TG1-1  NFHCZ|VHfW6ldHnvckBCe3OjeR?= NUfxTW5rOcLizszN M13wVVI1KGh? NFHmeYFi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKFCLM1u= NEXWZ4QzOzB6OE[wOy=>
MCF7 M2nDR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS2UHdSOTByIH7N MlzKOFghcA>? NF\Rd5Ft\WGmczD0c{BiKHOrbXnsZZIhdG:|czDpckB{fXK4aY\hcEBieyC5aYToJIRwgG:{dXLpZ4lvKGGub37l Ml7rNlMxPzd{NEm=
MCF7 Mne0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\DVYMyODBibl2= NHyzeHA1QCCq NG\GOoVmdmijbnPld{BvfXSuaX6tcYVlcWG2ZXSgZ4VtdCCmZXH0bC=> MoHxNlMxPzd{NEm=
MCF-7  MnS4SpVv[3Srb36gRZN{[Xl? MoK2OkBp MkfNSG1UVw>? NHG0T21ifHSnboXheIV{KHSqZTDmcJVlcW:6b37pcE0hd3JiZnXubIV5[W2rZD3pcoR2[2WmIHnuZ5Jm[XOnIHnuJI1qWi1{MTDlfJBz\XO|aX;u M{TxUFI{ODV{MEO2
MCF-7 M4P3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYWxNFAhdk1xMTFOwG0> NX3aeII1PSCm MYPpcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[gNVfPui2nc4TyZYRqd2x? M3rWdFIzQTh{N{[1
MCF-7 NYHpZ2c4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3oNVAxKG6P NYTPNpI5PSCm NInv[o5qdmirYnn0d{B1cGVic4TpcZVt[XSrb36gc4Yh\nW|YYLp[YxqdiCK NYfJN|hrOjJ7OEK3OlU>
1471.1 M1;2dWZ2dmO2aX;uJGF{e2G7 NVrKXoxtOTByIH7N NES4RoQyKGh? Mk\jSZRQUMLi M{PmNZRic2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> MnmxNlI5PjlzME[=
MCF-7 NFHobpVHfW6ldHnvckBCe3OjeR?= NFn3ZnQyODBibl2= NXrOWZRUOSCq NYXnXFdoTXSRSNMg NF[z[2N1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> M2S1V|IzQDZ7MUC2
HeLa MlXwSpVv[3Srb36gRZN{[Xl? NYHSUo5jOTByIH7N M{PGTlEhcA>? M2qyT2V1V0kEoB?= M{iyXZRic2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> M1m2VlIzQDZ7MUC2
COS-7  MnyzSpVv[3Srb36gRZN{[Xl? M{jxeVExOCCwTR?= M2TNW|EhcA>? Mln1SZRQUMLi MVv0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= MUCyNlg3QTFyNh?=
BG1L-OHTLT  Mn\iSpVv[3Srb36gRZN{[Xl? MnuwNVDDqG6P MkXYNlTDqGkEoB?= NI\r[HBqdmirYnn0d{BGWs7zIHX4dJJme3Orb36= NXLTWGd2OjJ4NUK1OVg>
BG1L-ICILT MUnGeY5kfGmxbjDBd5NigQ>? M2XrNlExyqCwTR?= M3Xub|I1yqCqwrC= MmOzbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w NXXM[|JpOjJ4NUK1OVg>
PC-9 M3fR[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfic3MxNjByMz2zNEDPxE1? NVLjSXIxPDhiaB?= MnnvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MV[yNlU3ODZ|NB?=
H1650 M4PYcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\oSmE5OC5yMEOtN|Ah|ryP MnraOFghcA>? MVXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWqyNlU3ODZ|NB?=
H1975 MmfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnw[m0xNjByMz2zNEDPxE1? NIHxVIc1QCCq MnnjbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVzYNFJyOjJ3NkC2N|Q>
H1975 M4XaOGZ2dmO2aX;uJGF{e2G7 MmL1N:Kh|ryP MYizJIg> M2nsZoFjem:pYYTld{B1cGVicHjvd5Bpdy2HR1\SJIlv\HWldHnvckBjgSCnc4Tyc4dmdg>? MWKyNlU3ODZ|NB?=
H1975 MofpSpVv[3Srb36gRZN{[Xl? NIP5foU{yqEQvF2= NGTKfGg4KGR? M4LPOYlv\HWlZYOgSWdHWiCneIDy[ZN{cW:w MXOyNlU3ODZ|NB?=
HTR-8 MUPGeY5kfGmxbjDBd5NigQ>? MYCxxsDPxE1? NIjY[HcyNTR6IHi= NF;LR3hld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDJS2ZDWDdibWLORS=> NEfsbWwzOjN6M{GxNS=>
JEG-3 MWnGeY5kfGmxbjDBd5NigQ>? NEHlb4oyyqEQvF2= NXrneYFrOS12ODDo M2LiToRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B NXX4b5VCOjJ|OEOxNVE>
Huh7 NWXDcZNHTnWwY4Tpc44hSXO|YYm= MVe1NOKh|ryP MmTJOFghcA>? M3r1colvcGmkaYTzJIdmdmm|dHXpck1u\WSrYYTl[EBRV05zIITyZY5{[WO2aY\heIlwdg>? MoHLNlI{ODR{OU[=
201T MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;XPVUh|ryP M2j3VVczKGh? Mnz0bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? M{nU[|IzOjV6NEe2
A549  M4[x[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTxcpExPSEQvF2= MWe3NkBp M3m5b4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4YX7k[ZRidmmk NF2zTWMzOjJ3OES3Oi=>
MCF-7 M3T3Z2Z2dmO2aX;uJGF{e2G7 Mlj0NeKh|ryP NWnKWIh4OjRiaNMg NUDIXm5v\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi Mle1NlIxPDl|MU[=
HCC-1428 MmDmSpVv[3Srb36gRZN{[Xl? MkjtNeKh|ryP M2LxTVI1KGkEoB?= NWewcnBT\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi MVOyNlA1QTNzNh?=
MDA-361 MVfGeY5kfGmxbjDBd5NigQ>? NUf1b3NSOcLizszN MlXLNlQhcMLi MYXkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb36gbY5lfWOnZDDifUA1NU:KLWSgxsA> NVzV[YF{OjJyNEmzNVY>
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MCF-7 Ml3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHXNeKh|ryP M{nkclUuOTBiZB?= M2\NZpN2eHC{ZYPz[ZMhTTJvaX7keYNm\CCpcn;3eIghcW6qaXLpeIlwdg>? MlzLNlIxPDl|MU[=
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MDA-361 NIG1Sm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXGxxsDPxE1? Ml21OU0yOCCm NFO4cI1{fXCycnXzd4V{KEV{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? MX2yNlA1QTNzNh?=
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HepG2 MVjBdI9xfG:|aYOgRZN{[Xl? MUWwMlHDqM7:TR?= NXv6VmdSOjRiaB?= NVXyWXRV[WKxbHnzbIV{KHSqZTDld5Rzd2enbj3pcoR2[2WmIIXwMZJm\3WuYYTpc44hd2ZiYYDvRWkh[W6mIHHwc20> MUeyNVgyPjJ|Mx?=
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MCF7 MnXUSpVv[3Srb36gRZN{[Xl? M1XzVVHDqM7:TR?= M1zOT|Q5KGh? MXvkc5dvemWpdXzheIV{KG:4ZYLhcIwhTVMQsTDwdo91\WmwIHzleoVtew>? M2Pm[|IyPTN|MUm1
MCF7S MYjGeY5kfGmxbjDBd5NigQ>? NFzMcWEyyqEQvF2= NWi5UZduPyCm MVrheJRmdnWjdHXzJJR2dW:{c4Do[ZJmKG[xcn3heIlwdiCjbnSgdJJwdGmoZYLheIlwdg>? MUCyNVU{OzF7NR?=
MCF7S NYHYNoxET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnmUWttOC53L{Gg{txO MnKwO{Bl NV7Ne5ZSTE2VTx?= NWDucWM1\GWlcnXhd4V{KGOnbHyg[Zhx[W6|aX;u NXXKTlBFOjF3M{OxPVU>
T47D  M1fzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkCyOEBvVQ>? MoXrOFAhcA>? MYTzeZBxemW|c3XzJINmdGxiZ4Lve5RpKG2xZHXyZZRmdHl? MUGyNVQ5ODN7MR?=
BT474  NFLzRo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{THdlQhdk1? NXHqe3cxPDBiaB?= NEHOV2h{fXCycnXzd4V{KGOnbHyg[5Jwf3SqIH3v[IVz[XSnbIm= M4\ZeVIyPDhyM{mx
T47D  MmDzSpVv[3Srb36gRZN{[Xl? NYfw[JY{OTBibl2= MnfIOFAhcA>? NEeyVWVld3ewcnXneYxifGW|IFXS{tEheHKxdHXpci=> NIL2fm0zOTR6MEO5NS=>
BT474  M{CyTWZ2dmO2aX;uJGF{e2G7 NGXmSoEyOCCwTR?= NXjOUnF6PDBiaB?= NY\WbolL\G:5boLl[5Vt[XSnczDFVu6yKHC{b4TlbY4> NY\BNldQOjF2OECzPVE>
MCF7 NXr3SI5mTnWwY4Tpc44hSXO|YYm= NEWxWm8yODBibl2= NVnIWFhVPyCm NFzGS4tz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 MV2yNVM6PjB7NB?=
T47D  NUL6NIJzTnWwY4Tpc44hSXO|YYm= MU[xNFAhdk1? MVW3JIQ> MlfzdoVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> MX2yNVM6PjB7NB?=
BT474  M{jmbmZ2dmO2aX;uJGF{e2G7 NHTaN5MyODBibl2= NV;V[FJ{PyCm Mlf3doVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> MUOyNVM6PjB7NB?=
MDAMB361 MoTDSpVv[3Srb36gRZN{[Xl? MYqxNFAhdk1? NIfFVI44KGR? MmK0doVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> NXnSN3RxOjF|OU[wPVQ>
MCF7 M1LoPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT6NokxNjBzLUGg{txO MnPBO{Bl NXHoN3RmemWmdXPld{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NWS2XVhsOjF|OU[wPVQ>
T47D  NI\NV3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX60fm8yOC5yMT2xJO69VQ>? NH7OTW44KGR? M{GzV5Jm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MVyyNVM6PjB7NB?=
BT474  NFvITG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXubFcxNjBzLUGg{txO NHrBOXc4KGR? M1\VUJJm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MoizNlE{QTZyOUS=
MDAMB361 NILqV|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TORlAvODFvMTFOwG0> MXS3JIQ> M2PrZ5Jm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NULoO|JkOjF|OU[wPVQ>
MCF7 NEnFRnBHfW6ldHnvckBCe3OjeR?= NFnNRogyODBibl2= NI\ITXk4KGR? M{ji[olv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= M2HS[lIyOzl4MEm0
T47D  M3i2[WZ2dmO2aX;uJGF{e2G7 NUjH[mUxOTByIH7N NFvnRXI4KGR? NEj4NIZqdmS3Y3XzJI9nKEW{YlKzJIFv\CCHcnLCOEBz\WOncITvdkBmgHC{ZYPzbY9vKGGwZDDzbYdv[WyuaX7n MVuyNVM6PjB7NB?=
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MMQ NFewcJZHfW6ldHnvckBCe3OjeR?= NWS4RpJIOC5yND22NlUhdk1? NXPpTVN7PzJiaB?= MWj1dJJm\3WuYYTld{BVT0cQskOgZY5lKFSJRt8yVmlKKGW6cILld5Nqd25? NWfjT|V7OjB5MEC3OVU>

... 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 <1 mg/mL
In vivo 5% DMSO+95% Corn oil 30mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
NCT01797120 Active, not recruiting Metastatic Breast Cancer PrECOG, LLC.|Novartis May 31, 2013 Phase 2
NCT01633060 Active, not recruiting Metastatic Breast Cancer Novartis Pharmaceuticals|Novartis October 3, 2012 Phase 3
NCT03007979 Not yet recruiting Breast Cancer|Breast Carcinoma|Cancer of Breast|Malignant Tumor of Breast Washington University School of Medicine February 28, 2017 Phase 2
NCT03024580 Not yet recruiting Breast Neoplasm Instituto Nacional de Cancer, Brazil|Cancer Research UK Cambridge Institute March 2017 Phase 2
NCT02947685 Not yet recruiting HER-2 Positive Breast Cancer|Estrogen Receptor Positive Breast Cancer Alliance Foundation Trials, LLC.|Pfizer|German Breast Group (GBG)|Fondazione Michelangelo|PrECOG, LLC.|The Australia and New Zealand Breast Cancer Trials Group (ANZBCTG)|Alliance Foundation Trials Biorepository - Washington State University|Alliance Foundation Trials Central Imaging Core Lab - Ohio State University|Mastering Breast Cancer Initiative, LLC|Mayo Clinic Statistics and Data Center|INC Research|SOLTI Breast Cancer Research Group February 2017 Phase 3
NCT02983604 Recruiting Advanced Estrogen Receptor Positive HER2- Breast Cancer Gilead Sciences January 2017 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID