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 NEPtW4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYWxMlMuOTByMDDuUS=> M2j3UVQ5KGh? MmjZbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmL3NlQ6Pzl{OUS=
MCF-7/LTED MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XMdlEvOy1zMECwJI5O NH;TWFY1QCCq M{XpdolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NEnvNZczPDl5OUK5OC=>
HCC1428 NUfHbnBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXINU4{NTFyMECgcm0> NGrncG81QCCq NFTKeZhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{jlRVI1QTd7Mkm0
HCC1428/LTED M4DEW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3nT3AyNjNvMUCwNEBvVQ>? MYe0PEBp NHLSVmZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{HndFI1QTd7Mkm0
LCC1 M{DrcWZ2dmO2aX;uJGF{e2G7 MlnNNVAxKG6P NUTEcFVPPDhvMUS0JIg> Ml:3ZYN1cX[jdHXzJHVRWiC|aXfuZYxqdmd? M4nE[|I1QDV6Mke3
LCC9 M{fm[GZ2dmO2aX;uJGF{e2G7 NVPad5VXOTByIH7N Mn;yOFguOTR2IHi= M1PV[IFkfGm4YYTld{BWWFJic3nncoFtcW6p MmDBNlQ5PTh{N{e=
MCF-7  MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[xNFAhdk1? NF3aSJI2KGR? M{e1ZYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSxIEGw89yG MnyxNlQ5OTl3NUC=
mesangial  MWLGeY5kfGmxbjDBd5NigQ>? NU\VVWp{OC5zLUGwNEBvVQ>? NUXBSmlQPDhiaB?= NXW5Wnpte3WycILld5NmeyCWR1[t{tIyNWmwZIXj[YQhfHmyZTDJWkBkd2yuYXflci=> NG\vflMzPDd7M{[zPS=>
Mesangial M4m2d2Z2dmO2aX;uJGF{e2G7 M4XYdFAvOS1zMECgcm0> NFzZWnExNjViaB?= NWXrNIdUcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJHNu[WR{IIDoc5NxcG:{eXzheIlwdiC4aXGgS3BGWg>? MWCyOFc6OzZ|OR?=
ER+ MCF-7/2a NXHvTollT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTBwMEC0JO69VQ>? NXfEN4dOOTV|MkS4PFQ>
ER+ MCF-7 M4fzNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\nfGYzODBiaB?= NYroUZF2UUN3ME2wMlIyKG6P NI\JNVIyPTN{NEi4OC=>
MCF-7  MnTlSpVv[3Srb36gRZN{[Xl? MV[xNOKhdk4EoB?= NG\QTHY4OiCq MoLzdoV3\XK|ZYOgeIhmKGW|dILv[4VvKGWoZnXjeEhKSzVyIEGuPUDEnyBzMPMIllkhVSl? M1jlbFI1QTB6NkWy
MCF-7  NY[2bI1KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\aXFVKSzVywrDv[kBieHC{b4jpcYF1\Wy7IEKgcm0> NIn6V24zOzR2OEO0Oi=>
H1975  MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:zxsDPxE1? MWCxJI0> MXvpcoNz\WG|ZYOgeIhmKGenZnn0bY5q[iC|ZX7zbZRqfmm2eTDv[kBJOTl5NTDj[Yxte8Li NF[yOJIzPDJ4OEixNC=>
H1975 MmHQSpVv[3Srb36gRZN{[Xl? MWCzxsDPxE1? MYWxJI0> MV71dJJm\3WuYYTld{B1cGVibHX2[Ywhd2ZiTHX0MVdk MUWyOFI3QDhzMB?=
MCF-7  NH\xVY5HfW6ldHnvckBCe3OjeR?= M1LiblExOOLCiX7NxsA> MoXxO|IhcA>? NXfKO4pYemW4ZYLz[ZMhfGinIIDyc5Rm[3SrdnWg[YZn\WO2IH;mJGUzyqCrbjDj[YxtKGmwdnHzbY9v MkP5NlM6OzZ5N{O=
MCF-7  MUXGeY5kfGmxbjDBd5NigQ>? MYexNFDjiImwTdMg MX6yOE81QCCq MUXmZYNqdGm2YYTld{Bqdn[jc3nvckB1cHKxdXfoJG1OWHNpIH3v[JVt[XSrb36= MnX0NlM6OzZ5N{O=
BT474-tet-shMED1 NH\CZWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLSNE4yNTVizszN NFT1bJU4KGR? MVHpcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFvlTnMzOzl|NkKzOC=>
ZR75-1-tet-shMED1  NVjHSVdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\OdpIxNjFvNTFOwG0> M{XiNVch\A>? NED2doRqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M1rJb|I{QTN4MkO0
MCF-7-tet-shMED1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXDNE4yNTVizszN M4C0OFch\A>? NIGwfGdqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M1mwUFI{QTN4MkO0
HepG2  NXHWPWxRTnWwY4Tpc44hSXO|YYm= NYjDPZRvOC5yMT2xNEDPxE1? M2HLU|E5KGkEoB?= NEC2fJJi[3SrdnH0[ZMhfGinIFXSSU1u\WSrYYTl[EB1emGwc3PybZB1cW:wIH;mJGFHOkWU MVyyN|c{OzF6OB?=
MCF-7L  NHPrU|VHfW6ldHnvckBCe3OjeR?= NHPu[oIyODBibl5CpC=> MWSxNEBucW5xMkSgbE81QCCq M1fFOZJme3WudIOgbY4hTUeIUjygTGVTOiCjbnSgTGVTOyCyaH;zdIhwenmuYYTpc44h[XRicILvcI9v\2WmIHX4dI9{fXKn MVOyN|Y5PjRzNh?=
MCF-7L  MWPGeY5kfGmxbjDBd5NigQ>? NF62dVMyODBibl5CpC=> MlXIOFghcA>? M3;wdYlv\HWlZYOgeZBz\We3bHH0bY9vKG:oIH3SUmEhd2ZiRVfGVkBtcWejbnSgTGIuTUeI M{HJWFI{Pjh4NEG2
MCF-7L MVfGeY5kfGmxbjDBd5NigQ>? MVSxNFAhdk4EoB?= NFvp[2U1QCCq M1q5VYlv\HWlZYOgSWdHWiCoYX3pcJkhdWWvYnXyJIFkfGm4YYTpc44hemWzdXny[YQhTVJ? MUGyN|Y5PjRzNh?=
C4-12  M4WwNWZ2dmO2aX;uJGF{e2G7 MWmxNFAhdk4EoB?= NWTJemNUPDhiaB?= M17BR4lv\HWlZYOgSWdHWiCoYX3pcJkhdWWvYnXyJIFkfGm4YYTpc44hemWzdXny[YQhTVJ? MXuyN|Y5PjRzNh?=
MCF-7L M1jZU2Z2dmO2aX;uJGF{e2G7 MX[xNFAhdk4EoB?= MnrlNlQhcA>? M2i1NYlv\HWlZYOgSWdHWiCyaH;zdIhwenmuYYTpc44hemWzdXny[YQhUEJvRVfGJIZ2dmO2aX;u M1e5WlI{Pjh4NEG2
MMQ  MULGeY5kfGmxbjDBd5NigQ>? NX\BV|dqOC14MkWgcm0> MonHO|IhcA>? NFPFR4Zld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDld5Rzd2enbjDy[YNmeHSxcj5OtUApTVMQsTm= Mlv5NlM2OjN|NUe=
H1975  NWLGe21mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjGfmI3OC5|MUK1MVExKM7:TR?= MmLNOkBl M3fvR4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkHzNlM{QTl7NUe=
H1975  NX7Sb41tSXCxcITvd4l{KEG|c3H5 M{LOe|IxOCCwTR?= MUi3NkBp M2jzSIVvcGGwY3XzJIVzdG:2aX7pZkBqdmS3Y3XkJIFxd3C2b4Ppdy=> M3jUSFI{Ozl7OUW3
MCF-7  MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7K[W0yOC9zMECvNVAxOCCwTR?= MmfvNk81NzZiZB?= NU\4SoJTTE2VTx?= NVvDZopScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> NYTWe5VvOjN|MUO1NFY>
MCF-7  Ml3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TMWVExOCCwTR?= NHnhcng1KGR? MmLySG1UVw>? MliwbY5lfWOnczDhJIhq\2incjDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKHSqZTDHNUBxcGG|ZdMg NGLWW|MzOzNzM{WwOi=>
MLO-Y4  M1qwUGZ2dmO2aX;uJGF{e2G7 MYqxxsDPxE1? NHzlNVYyKGh? Ml62bY5pcWKrdIOgSVIucW6mdXPl[EBEgDR|IHX4dJJme3Orb36= M{PqSVI{OjR5MEW3
MCF-7 NH3EfZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;yfI0xOTByIH7N NH\neGI1QCCq M3[5Z4Fjem:pYYTld{B1cGVicILvcIln\XKjdHn2[UBm\m[nY4Sgc4YhdW:mZYLheIUhdmm2cn;zZZRqfmVic4Ty[ZN{ NYmyfHltOjN{MU[3OFQ>
TG1-1  NWSxSY4yTnWwY4Tpc44hSXO|YYm= NXrMO3QyOcLizszN NEHsRmczPCCq M3r4TYFjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhUEmILUJOtS=> M2TJXlI{ODh6NkC3
TG1-1  NID0NWRHfW6ldHnvckBCe3OjeR?= NFfkPVQyyqEQvF2= MnnMNlQhcA>? MYnhZpJw\2G2ZYOgSVLDqGmwZIXj[YQh[WOldX31cIF1cW:wIH;mJHBKO0t? M3nKSlI{ODh6NkC3
MCF7 NGOxVJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fiO|ExOCCwTR?= MkjOOFghcA>? NXzWO2ozdGWjZIOgeI8h[SC|aX3pcIFzKGyxc4OgbY4he3W{dnn2ZYwh[XNid3n0bEBld3ixcoXibYNqdiCjbH;u[S=> MWWyN|A4PzJ2OR?=
MCF7 MlrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jSUlExOCCwTR?= NXLzT3k5PDhiaB?= MYPlcohidmOnczDueZRtcW5vbXXkbYF1\WRiY3XscEBl\WG2aB?= MkfPNlMxPzd{NEm=
MCF-7  NWfOUJhLTnWwY4Tpc44hSXO|YYm= MkLyOkBp NEK2bYpFVVOR M3LRS4F1fGWwdXH0[ZMhfGinIH\seYRqd3ixbnnsMUBweiCoZX7o[ZhidWmmLXnu[JVk\WRiaX7jdoVie2ViaX6gcYlTNTJzIHX4dJJme3Orb36= MmH5NlMxPTJyM{[=
MCF-7 NYPPOJdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmL4NVAxKG6PL{Gg{txO Mk\rOUBl MYDpcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[gNVfPui2nc4TyZYRqd2x? M1foXFIzQTh{N{[1
MCF-7 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHXfZcyODBibl2= MUC1JIQ> MU\pcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[g[pV{[XKrZXzpckBJ M3TYZlIzQTh{N{[1
1471.1 MXTGeY5kfGmxbjDBd5NigQ>? NIXLSm8yODBibl2= MWWxJIg> NHvNZpJGfE:KwrC= MVn0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= NF;zVVYzOjh4OUGwOi=>
MCF-7 NEPJTYJHfW6ldHnvckBCe3OjeR?= MlfuNVAxKG6P MWOxJIg> NGfvcGdGfE:KwrC= MXn0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= NIDJRWgzOjh4OUGwOi=>
HeLa MX\GeY5kfGmxbjDBd5NigQ>? M1Lac|ExOCCwTR?= MnjiNUBp NUOzeZROTXSRSNMg NFSzWYh1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> Mkm4NlI5PjlzME[=
COS-7  NWnCUllWTnWwY4Tpc44hSXO|YYm= M3TZWFExOCCwTR?= NEi4T4YyKGh? NGDSXmJGfE:KwrC= M3rPXZRic2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> MVuyNlg3QTFyNh?=
BG1L-OHTLT  NHnpVHhHfW6ldHnvckBCe3OjeR?= MmflNVDDqG6P NXvGOnl7OjUEoHlCpC=> NVT4epFKcW6qaXLpeJMhTVMQsTDlfJBz\XO|aX;u MnHQNlI3PTJ3NUi=
BG1L-ICILT NIfXOGRHfW6ldHnvckBCe3OjeR?= M{j5UVExyqCwTR?= MkfSNlTDqGkEoB?= NHPZcW9qdmirYnn0d{BGWs7zIHX4dJJme3Orb36= MVmyNlY2OjV3OB?=
PC-9 NUDHW2NtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEC1dFIxNjByMz2zNEDPxE1? MWe0PEBp NF6wcYhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NEH5O5ozOjV4ME[zOC=>
H1650 NUe1OIo4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX:5ZmtOOC5yMEOtN|Ah|ryP NHLLUWI1QCCq NHvDUVNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mli2NlI2PjB4M{S=
H1975 M3\RdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjHWY5IOC5yMEOtN|Ah|ryP MoDyOFghcA>? M1roXYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MlzHNlI2PjB4M{S=
H1975 MUHGeY5kfGmxbjDBd5NigQ>? MWSzxsDPxE1? NWDkcmtuOyCq M{fH[oFjem:pYYTld{B1cGVicHjvd5Bpdy2HR1\SJIlv\HWldHnvckBjgSCnc4Tyc4dmdg>? MWiyNlU3ODZ|NB?=
H1975 NX3XT|N5TnWwY4Tpc44hSXO|YYm= MXKzxsDPxE1? MlqyO{Bl M37pcYlv\HWlZYOgSWdHWiCneIDy[ZN{cW:w NITDfnAzOjV4ME[zOC=>
HTR-8 MWjGeY5kfGmxbjDBd5NigQ>? NX33c4E5OcLizszN NFfrUW4yNTR6IHi= M2O2W4Rwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B MX:yNlM5OzFzMR?=
JEG-3 MV\GeY5kfGmxbjDBd5NigQ>? NF;X[XoyyqEQvF2= MkeyNU01QCCq NI\qPZNld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDJS2ZDWDdibWLORS=> M1m5PVIzOzh|MUGx
Huh7 NXS2bmx3TnWwY4Tpc44hSXO|YYm= MnH2OVDDqM7:TR?= MX20PEBp MlTPbY5pcWKrdIOg[4VvcXO2ZXnuMY1m\GmjdHXkJHBQVjFidILhcpNi[3SrdnH0bY9v NYXSdnZXOjJ|MESyPVY>
201T MnrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknOOUDPxE1? NGnvNJk4OiCq NVGxVHJJcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\hcoRmfGGwaXK= NGXRVWIzOjJ3OES3Oi=>
A549  M1jCOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTjVYNtPSEQvF2= M{K4[VczKGh? NX7ibo9pcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\hcoRmfGGwaXK= Mlf2NlIzPTh2N{[=
MCF-7 M2DMS2Z2dmO2aX;uJGF{e2G7 NUnZV2x4OcLizszN MnS4NlQhcMLi MX\kc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb36gbY5lfWOnZDDifUA1NU:KLWSgxsA> M1LSWVIzODR7M{G2
HCC-1428 NV\5OZd{TnWwY4Tpc44hSXO|YYm= NV\Fd3VnOcLizszN NEP1WJIzPCCqwrC= NUj2bHRi\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi Mn;yNlIxPDl|MU[=
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MCF7 M13PPWZ2dmO2aX;uJGF{e2G7 NGLFbm0yyqEQvF2= NVLmdoU5PDhiaB?= NFnKNGdld3ewcnXneYxifGW|IH;2[ZJidGxiRWNOtUBxem:2ZXnuJIxmfmWucx?= MU[yNVU{OzF7NR?=
MCF7S M3;KfWZ2dmO2aX;uJGF{e2G7 M3vkS|HDqM7:TR?= NGn1XWY4KGR? MWfheJRmdnWjdHXzJJR2dW:{c4Do[ZJmKG[xcn3heIlwdiCjbnSgdJJwdGmoZYLheIlwdg>? M1vQSVIyPTN|MUm1
MCF7S Mn65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3w[VMxNjVxMTFOwG0> MoC3O{Bl MV\EUXNQ M4\GOYRm[3KnYYPld{Bk\WyuIHX4dIFve2mxbh?= MmXQNlE2OzNzOUW=
T47D  MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HDW|Qhdk1? M2Pr[VQxKGh? NUnIWFl[e3WycILld5NmeyClZXzsJIdzd3e2aDDtc4RmemG2ZXz5 M13leVIyPDhyM{mx
BT474  M3\4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkO3OEBvVQ>? NFTNNm81OCCq M3vKNpN2eHC{ZYPz[ZMh[2WubDDndo94fGhibX;k[ZJifGWueR?= NFrpZ3ozOTR6MEO5NS=>
T47D  MWXGeY5kfGmxbjDBd5NigQ>? M2f3SFExKG6P MUW0NEBp MVvkc5dvemWpdXzheIV{KEWUzsGgdJJwfGWrbh?= MUCyNVQ5ODN7MR?=
BT474  Mk\5SpVv[3Srb36gRZN{[Xl? NH7OS24yOCCwTR?= MkTIOFAhcA>? NEPPVIJld3ewcnXneYxifGW|IFXS{tEheHKxdHXpci=> MUiyNVQ5ODN7MR?=
MCF7 NHvwSlNHfW6ldHnvckBCe3OjeR?= M1\mVVExOCCwTR?= NHH2dWg4KGR? NEXBeodz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 MlyzNlE{QTZyOUS=
T47D  MkHHSpVv[3Srb36gRZN{[Xl? M4rldVExOCCwTR?= M3GzXFch\A>? MUTy[YR2[2W|IFXS{tEh\XiycnXzd4lwdiC|aXfubYZq[2GwdHz5 M3:4XVIyOzl4MEm0
BT474  MmfCSpVv[3Srb36gRZN{[Xl? MonMNVAxKG6P NYHidVhYPyCm NIG4[nRz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 MmTTNlE{QTZyOUS=
MDAMB361 NGLJbWxHfW6ldHnvckBCe3OjeR?= M2TLTVExOCCwTR?= M3XCclch\A>? Mn;UdoVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> MlizNlE{QTZyOUS=
MCF7 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzRZmZjOC5yMT2xJO69VQ>? MWe3JIQ> M4H4VZJm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NUjVbIN{OjF|OU[wPVQ>
T47D  M1m2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOwMlAyNTFizszN NHvydW44KGR? NGjaO3pz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3rTU|IyOzl4MEm0
BT474  Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHe0O3kxNjBzLUGg{txO NHTJeow4KGR? NGnEXY1z\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NFvHc2IzOTN7NkC5OC=>
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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

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).

Dilution Calculator

Dilution Calculator

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

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

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Molecular Weight Calculator

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03691493 Not yet 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 December 1 2018 Phase 2
NCT03554044 Not yet recruiting Anatomic Stage III Breast Cancer AJCC v8|Anatomic Stage IIIA Breast Cancer AJCC v8|Anatomic Stage IIIB Breast Cancer AJCC v8|Anatomic Stage IIIC Breast Cancer AJCC v8|Anatomic Stage IV Breast Cancer AJCC v8|Estrogen Receptor Positive|HER2/Neu Negative|Invasive Breast Carcinoma|Prognostic Stage III Breast Cancer AJCC v8|Prognostic Stage IIIA Breast Cancer AJCC v8|Prognostic Stage IIIB Breast Cancer AJCC v8|Prognostic Stage IIIC Breast Cancer AJCC v8|Prognostic Stage IV Breast Cancer AJCC v8|Recurrent Breast Carcinoma University of California San Francisco|Amgen December 11 2018 Phase 1
NCT03531645 Not yet recruiting Malignant Neoplasms of Female Genital Organs M.D. Anderson Cancer Center|AstraZeneca|Pfizer November 2018 Phase 2
NCT03685331 Not yet recruiting Metastatic Breast Cancer|Locally Advanced Breast Cancer|Advanced Breast Cancer|BRCA2 Mutation|BRCA1 Mutation Abramson Cancer Center of the University of Pennsylvania September 2018 Phase 1
NCT03584009 Recruiting Estrogen Receptor-positive (ER+)/Human Epidermal Growth Factor Receptor (HER2)-Negative Locally Advanced or Metastatic Breast Cancer Hoffmann-La Roche September 13 2018 Phase 2
NCT03643510 Recruiting Adenocarcinoma of Endometrium Memorial Sloan Kettering Cancer Center|Eli Lilly and Company August 21 2018 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