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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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, 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 NUfHfVY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\SNU4{NTFyMECgcm0> NVHyenZGPDhiaB?= M3XLS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MlfkNlQ6Pzl{OUS=
MCF-7/LTED NVfOe5E1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\XeJdnOS5|LUGwNFAhdk1? NWX5VXJrPDhiaB?= MYfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mo\1NlQ6Pzl{OUS=
HCC1428 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33heFEvOy1zMECwJI5O MkfrOFghcA>? MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUKyOFk4QTJ7NB?=
HCC1428/LTED MlPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2xMlMuOTByMDDuUS=> M1PWblQ5KGh? MVTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NU\iOVRQOjR7N{myPVQ>
LCC1 NUjUUIJMTnWwY4Tpc44hSXO|YYm= NXHQRnl{OTByIH7N MWS0PE0yPDRiaB?= MUjhZ5RqfmG2ZYOgWXBTKHOrZ37hcIlv\w>? M1v0PFI1QDV6Mke3
LCC9 NXvr[VFwTnWwY4Tpc44hSXO|YYm= MYexNFAhdk1? NEXUT3U1QC1zNESgbC=> M3X1VYFkfGm4YYTld{BWWFJic3nncoFtcW6p NUjqW4E5OjR6NUiyO|c>
MCF-7  MmraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrQSVQyODBibl2= NELXUoU2KGR? M1vLcolvcGmkaYTzJINmdGxiZ4Lve5RpKHSxIEGw89yG MmDRNlQ5OTl3NUC=
mesangial  MnW3SpVv[3Srb36gRZN{[Xl? NFzyOoExNjFvMUCwJI5O NXXFTY5EPDhiaB?= MkW0d5VxeHKnc4Pld{BVT0ZvzsKxMYlv\HWlZXSgeJlx\SCLVjDjc4xt[Wenbh?= M3TzS|I1Pzl|NkO5
Mesangial Mo\PSpVv[3Srb36gRZN{[Xl? M2nqUFAvOS1zMECgcm0> M3;OblAvPSCq NUXpVmRScW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJHNu[WR{IIDoc5NxcG:{eXzheIlwdiC4aXGgS3BGWg>? NX[yXnNiOjR5OUO2N|k>
ER+ MCF-7/2a Ml\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHWTGtKSzVyPUCuNFA1KM7:TR?= MmrINVU{OjR6OES=
ER+ MCF-7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jIVVIxOCCq NV:4XHVnUUN3ME2wMlIyKG6P M1Lre|E2OzJ2OEi0
MCF-7  MULGeY5kfGmxbjDBd5NigQ>? NHnN[oQyOMLibl5CpC=> NW\qbWJLPzJiaB?= Ml:2doV3\XK|ZYOgeIhmKGW|dILv[4VvKGWoZnXjeEhKSzVyIEGuPUDEnyBzMPMIllkhVSl? MV:yOFkxQDZ3Mh?=
MCF-7  NYHnXXBKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M161bmlEPTEEoH;mJIFxeHKxeHntZZRmdHliMjDuUS=> MnjiNlM1PDh|NE[=
H1975  MlHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\O[m9YO8LizszN NY\NVYpYOSCv MlO4bY5kemWjc3XzJJRp\SCpZX\peIlvcWJic3Xud4l1cX[rdImgc4YhUDF7N{WgZ4VtdHQEoB?= M3:5WlI1OjZ6OEGw
H1975 MUPGeY5kfGmxbjDBd5NigQ>? MXGzxsDPxE1? NF71XFgyKG1? M3K2O5VxemWpdXzheIV{KHSqZTDs[ZZmdCCxZjDM[ZQuP2N? MmHCNlQzPjh6MUC=
MCF-7  MV\GeY5kfGmxbjDBd5NigQ>? MX2xNFDjiImwTdMg MmHsO|IhcA>? MnjudoV3\XK|ZYOgeIhmKHC{b4TlZ5RqfmViZX\m[YN1KG:oIFWyxsBqdiClZXzsJIlvfmG|aX;u MUiyN|k{Pjd5Mx?=
MCF-7  MkDSSpVv[3Srb36gRZN{[Xl? MorlNVAx6oDLbl5CpC=> NIPzTnkzPC92ODDo NYqwV406\mGlaXzpeIF1\XNiaX72ZZNqd25idHjyc5VocCCPTWDzK{Bud2S3bHH0bY9v Ml\RNlM6OzZ5N{O=
BT474-tet-shMED1 MkXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfpWm8xNjFvNTFOwG0> M{\2Wlch\A>? NHy1TZNqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NGLMU5AzOzl|NkKzOC=>
ZR75-1-tet-shMED1  M3;yd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHoNE4yNTVizszN M1e5WFch\A>? MW\pcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MWqyN|k{PjJ|NB?=
MCF-7-tet-shMED1 M1jne2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4SzUlAvOS13IN88US=> NHSzSVY4KGR? MYLpcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWDyN2xLOjN7M{[yN|Q>
HepG2  MUjGeY5kfGmxbjDBd5NigQ>? MoLWNE4xOS1zMDFOwG0> NHfHOpgyQCCqwrC= MYnhZ5RqfmG2ZYOgeIhmKEWURT3t[YRq[XSnZDD0doFve2O{aYD0bY9vKG:oIFHGNmVT NHfFd|MzOzd|M{G4PC=>
MCF-7L  NE\kU3BHfW6ldHnvckBCe3OjeR?= NY\keYlKOTByIH7NxsA> M3XDPVExKG2rbj:yOEBpNzR6IHi= NIfnPHBz\XO3bITzJIlvKEWJRmKsJGhGWjJiYX7kJGhGWjNicHjvd5Bpd3K7bHH0bY9vKGG2IIDyc4xwdmenZDDlfJBwe3W{ZR?= NELx[XgzOzZ6NkSxOi=>
MCF-7L  Ml74SpVv[3Srb36gRZN{[Xl? M2e1bVExOCCwTdMg NVG4UoprPDhiaB?= MXzpcoR2[2W|IIXwdoVofWyjdHnvckBw\iCvUl7BJI9nKEWJRmKgcIlo[W6mIFjCMWVITg>? M2m3ZVI{Pjh4NEG2
MCF-7L MW\GeY5kfGmxbjDBd5NigQ>? MnnXNVAxKG6PwrC= NGP5Tm41QCCq NW\s[GgycW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= M1S4S|I{Pjh4NEG2
C4-12  NIDGTZRHfW6ldHnvckBCe3OjeR?= MkfFNVAxKG6PwrC= M1HxRlQ5KGh? Mkj5bY5lfWOnczDFS2ZTKG[jbXnsfUBu\W2kZYKgZYN1cX[jdHnvckBz\XG3aYLl[EBGWg>? NFnUdWozOzZ6NkSxOi=>
MCF-7L NWDSN2dpTnWwY4Tpc44hSXO|YYm= M2TuVlExOCCwTdMg M2fGXlI1KGh? MoHUbY5lfWOnczDFS2ZTKHCqb4PwbI9zgWyjdHnvckBz\XG3aYLl[EBJSi2HR1[g[pVv[3Srb36= NHHRO3czOzZ6NkSxOi=>
MMQ  MoHiSpVv[3Srb36gRZN{[Xl? NWf3[YhOOC14MkWgcm0> MWG3NkBp Mly5[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiZYP0do9o\W5icnXj[ZB1d3JvzsGgLGVT|rFr NEDXVG0zOzV{M{O1Oy=>
H1975  MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnr4NE4{OTJ3LUGwJO69VQ>? MnPTOkBl M{LkbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1jVPVI{Ozl7OUW3
H1975  NILG[GdCeG:ydH;zbZMhSXO|YYm= MUKyNFAhdk1? M1XOWFczKGh? M1\FS4VvcGGwY3XzJIVzdG:2aX7pZkBqdmS3Y3XkJIFxd3C2b4Ppdy=> MVOyN|M6QTl3Nx?=
MCF-7  Mmq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnznNVAwOTByL{GwNFAhdk1? M4fMOVIwPC94IHS= NILWR5VFVVOR M2TOV4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= MWmyN|MyOzVyNh?=
MCF-7  MmDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYixNFAhdk1? M{Tp[VQh\A>? NEW0bVRFVVOR NVHZbJl[cW6mdXPld{BiKGirZ3jldkBxem:yb4L0bY9vKG:oIHPlcIx{KGmwIITo[UBIOSCyaHHz[eKh NH\iW|gzOzNzM{WwOi=>
MLO-Y4  NGrk[nhHfW6ldHnvckBCe3OjeR?= NF21PGwyyqEQvF2= MoLaNUBp MV3pcohq[mm2czDFNk1qdmS3Y3XkJGN5PDNiZYjwdoV{e2mxbh?= NU\HXoxnOjN{NEewOVc>
MCF-7 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXezOYtlOTByIH7N M330UFQ5KGh? M2HNb4Fjem:pYYTld{B1cGVicILvcIln\XKjdHn2[UBm\m[nY4Sgc4YhdW:mZYLheIUhdmm2cn;zZZRqfmVic4Ty[ZN{ NGHiUYEzOzJzNke0OC=>
TG1-1  NXrUbZlvTnWwY4Tpc44hSXO|YYm= MnuxNeKh|ryP MVqyOEBp MULhZpJw\2G2ZYOgSVLDqGmwZIXj[YQh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= NHqwPJUzOzB6OE[wOy=>
TG1-1  M4nxe2Z2dmO2aX;uJGF{e2G7 MoK4NeKh|ryP NI\BcJEzPCCq MXjhZpJw\2G2ZYOgSVLDqGmwZIXj[YQh[WOldX31cIF1cW:wIH;mJHBKO0t? NGXQWWIzOzB6OE[wOy=>
MCF7 NGDHU5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWCxNFAhdk1? M{nLPVQ5KGh? NWP3PGs{dGWjZIOgeI8h[SC|aX3pcIFzKGyxc4OgbY4he3W{dnn2ZYwh[XNid3n0bEBld3ixcoXibYNqdiCjbH;u[S=> M4TpSlI{ODd5MkS5
MCF7 MnLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DuWlExOCCwTR?= NYK3N2tbPDhiaB?= NIH5cY5mdmijbnPld{BvfXSuaX6tcYVlcWG2ZXSgZ4VtdCCmZXH0bC=> M1yzdlI{ODd5MkS5
MCF-7  NGr5XI1HfW6ldHnvckBCe3OjeR?= NX3hNIRoPiCq M17LbGROW09? MYfheJRmdnWjdHXzJJRp\SCobIXkbY95d26rbD2gc5Ih\mWwaHX4ZY1q\C2rbnT1Z4VlKGmwY4LlZZNmKGmwIH3pVk0zOSCneIDy[ZN{cW:w MWeyN|A2OjB|Nh?=
MCF-7 NVnM[Zl[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTGNVAxKG6PL{Gg{txO NYjzO5U6PSCm MlLpbY5pcWKrdIOgeIhmKHO2aX31cIF1cW:wIH;mJFE4|rJvZYP0doFlcW:u M3jsWFIzQTh{N{[1
MCF-7 M37wOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXlNVAxKG6P MljoOUBl M{KwdolvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kBnfXOjcnnlcIlvKEh? NXTQSYZCOjJ7OEK3OlU>
1471.1 MUXGeY5kfGmxbjDBd5NigQ>? MorVNVAxKG6P MWWxJIg> NUD0UIRzTXSRSNMg NX[2WnJCfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv M13nPFIzQDZ7MUC2
MCF-7 MVHGeY5kfGmxbjDBd5NigQ>? NWf1dFN[OTByIH7N NH;j[WcyKGh? NH3SVWVGfE:KwrC= NH\xPGN1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> NYLwWWZSOjJ6NkmxNFY>
HeLa NV7hWIRNTnWwY4Tpc44hSXO|YYm= NVvVUIl5OTByIH7N M1\J[|EhcA>? M2LDfGV1V0kEoB?= NIjiSoN1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> MV6yNlg3QTFyNh?=
COS-7  MU\GeY5kfGmxbjDBd5NigQ>? NYnqSYpOOTByIH7N NYjFU4g5OSCq MWXFeG9JyqB? M3PxNJRic2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> MUOyNlg3QTFyNh?=
BG1L-OHTLT  NHWyXpdHfW6ldHnvckBCe3OjeR?= MWCxNOKhdk1? M{XhU|I1yqCqwrC= MoPRbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w M134d|IzPjV{NUW4
BG1L-ICILT M1TFeWZ2dmO2aX;uJGF{e2G7 NEPvbVMyOMLibl2= M1LYNVI1yqCqwrC= NYPiOlZLcW6qaXLpeJMhTVMQsTDlfJBz\XO|aX;u MXWyNlY2OjV3OB?=
PC-9 NY\4XldLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITqWXExNjByMz2zNEDPxE1? MoDpOFghcA>? MXPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUWyNlU3ODZ|NB?=
H1650 MoHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTBdJQxNjByMz2zNEDPxE1? MVq0PEBp MW\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1vzPVIzPTZyNkO0
H1975 M1q0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfjelVoOC5yMEOtN|Ah|ryP MWq0PEBp MoH6bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVeyNlU3ODZ|NB?=
H1975 NYPTT4QzTnWwY4Tpc44hSXO|YYm= NXHQT4g3O8LizszN MVuzJIg> MkHsZYJzd2ejdHXzJJRp\SCyaH;zdIhwNUWJRmKgbY5lfWO2aX;uJIJ6KGW|dILv[4Vv MXSyNlU3ODZ|NB?=
H1975 Ml61SpVv[3Srb36gRZN{[Xl? NInkNGk{yqEQvF2= NEToPIg4KGR? NYrHb4lUcW6mdXPld{BGT0[UIHX4dJJme3Orb36= MnXMNlI2PjB4M{S=
HTR-8 M4\5dGZ2dmO2aX;uJGF{e2G7 MXexxsDPxE1? MVWxMVQ5KGh? M2H4cYRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B MUiyNlM5OzFzMR?=
JEG-3 MXHGeY5kfGmxbjDBd5NigQ>? NH7xfZgyyqEQvF2= M4r3W|EuPDhiaB?= NFPo[mVld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDJS2ZDWDdibWLORS=> M3HtSFIzOzh|MUGx
Huh7 M3PlNmZ2dmO2aX;uJGF{e2G7 M{TWO|UxyqEQvF2= MX20PEBp M373TYlvcGmkaYTzJIdmdmm|dHXpck1u\WSrYYTl[EBRV05zIITyZY5{[WO2aY\heIlwdg>? NGHudHUzOjNyNEK5Oi=>
201T M{XBVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPOOUDPxE1? NInHToM4OiCq MVTpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIghfmGwZHX0ZY5q[g>? MYqyNlI2QDR5Nh?=
A549  M2jKUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXS1JO69VQ>? MojJO|IhcA>? MoX0bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? MVSyNlI2QDR5Nh?=
MCF-7 NWrRRY5PTnWwY4Tpc44hSXO|YYm= MWKxxsDPxE1? MorzNlQhcMLi NEPQS3Fld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? NUP0WnpEOjJyNEmzNVY>
HCC-1428 M4XhPWZ2dmO2aX;uJGF{e2G7 M3XrUlHDqM7:TR?= MlzaNlQhcMLi NGHp[3dld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? NUX3PJdWOjJyNEmzNVY>
MDA-361 M2i5dmZ2dmO2aX;uJGF{e2G7 NGLnb5MyyqEQvF2= NXPTSmJyOjRiaNMg MYrkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb36gbY5lfWOnZDDifUA1NU:KLWSgxsA> MoLGNlIxPDl|MU[=
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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:
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

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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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.

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID