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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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 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzjWlcyNjNvMUCwNEBvVQ>? MYG0PEBp NX;Je4RNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NV7kZpVYOjR7N{myPVQ>
MCF-7/LTED MoXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF2ye|kyNjNvMUCwNEBvVQ>? M1Lid|Q5KGh? M2nZbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWnkdI1kOjR7N{myPVQ>
HCC1428 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYmxMlMuOTByMDDuUS=> MlW4OFghcA>? MWHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3frSVI1QTd7Mkm0
HCC1428/LTED MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;2V|F7OS5|LUGwNFAhdk1? NXHSNGJOPDhiaB?= MoizbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NF3QRnIzPDl5OUK5OC=>
LCC1 M2nrbGZ2dmO2aX;uJGF{e2G7 M{TvNlExOCCwTR?= MkLvOFguOTR2IHi= Ml3iZYN1cX[jdHXzJHVRWiC|aXfuZYxqdmd? M1L0fFI1QDV6Mke3
LCC9 MVXGeY5kfGmxbjDBd5NigQ>? MYmxNFAhdk1? NXXIflF[PDhvMUS0JIg> NHfMNY5i[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= MUiyOFg2QDJ5Nx?=
MCF-7  M2j0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[wUpIyODBibl2= M4\JfFUh\A>? MXrpcohq[mm2czDj[YxtKGe{b4f0bEB1dyBzMP-8iS=> NIP5[3kzPDhzOUW1NC=>
mesangial  MnvJSpVv[3Srb36gRZN{[Xl? MWSwMlEuOTByIH7N MVK0PEBp NV;H[VRKe3WycILld5NmeyCWR1[t{tIyNWmwZIXj[YQhfHmyZTDJWkBkd2yuYXflci=> MoHPNlQ4QTN4M{m=
Mesangial NEHmTWZHfW6ldHnvckBCe3OjeR?= NHzaemkxNjFvMUCwJI5O Mnn3NE42KGh? M33KVYlvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDTcYFlOiCyaH;zdIhwenmuYYTpc44hfmmjIFfQSXI> M3\Wb|I1Pzl|NkO5
ER+ MCF-7/2a MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwMEC0JO69VQ>? NUTRT4NxOTV|MkS4PFQ>
ER+ MCF-7 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3yPJkzODBiaB?= NUXm[FJIUUN3ME2wMlIyKG6P NIHTdWwyPTN{NEi4OC=>
MCF-7  Mnf1SpVv[3Srb36gRZN{[Xl? M2T3[FExyqCwTdMg NFvKNW84OiCq NF[5VmZz\X[ncoPld{B1cGViZYP0do9o\W5iZX\m[YN1MEmFNUCgNU46KMPZIEGw5qiTQSCPKR?= M3fwW|I1QTB6NkWy
MCF-7  M1vZVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2C2bmlEPTEEoH;mJIFxeHKxeHntZZRmdHliMjDuUS=> M3\yZ|I{PDR6M{S2
H1975  NXLJUVRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV[zxsDPxE1? NYP4fm5mOSCv M1vVPIlv[3KnYYPld{B1cGViZ3XmbZRqdmmkIIPlcpNqfGm4aYT5JI9nKEhzOUe1JINmdGy|wrC= M4nKTFI1OjZ6OEGw
H1975 M4LM[2Z2dmO2aX;uJGF{e2G7 MlfmN:Kh|ryP M1PlTVEhdQ>? NIfufI52eHKnZ4XsZZRmeyC2aHWgcIV3\Wxib3[gUIV1NTel NI\YNWwzPDJ4OEixNC=>
MCF-7  MVvGeY5kfGmxbjDBd5NigQ>? NX3TUGFpOTBy4pEJcm3DqA>? MofoO|IhcA>? MXfy[ZZmenOnczD0bIUheHKxdHXjeIl3\SCnZn\lZ5Qhd2ZiRUNCpIlvKGOnbHygbY53[XOrb36= MX2yN|k{Pjd5Mx?=
MCF-7  MXrGeY5kfGmxbjDBd5NigQ>? MUSxNFDjiImwTdMg NHHCfnIzPC92ODDo Mkfi[oFkcWyrdHH0[ZMhcW64YYPpc44hfGi{b4XnbEBOVVC|JzDtc4R2dGG2aX;u NVrZTIpZOjN7M{[3O|M>
BT474-tet-shMED1 NVvVVG1DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3[wUFAvOS13IN88US=> NFzVZXM4KGR? NHT0cmlqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NHvKb2QzOzl|NkKzOC=>
ZR75-1-tet-shMED1  Mo\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGryRnIxNjFvNTFOwG0> NWrtbIJbPyCm MmP6bY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NIXrfVYzOzl|NkKzOC=>
MCF-7-tet-shMED1 NXLYSJp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPBdFQxNjFvNTFOwG0> NFS3Rlg4KGR? NGPUT4xqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MlG0NlM6OzZ{M{S=
HepG2  MmO3SpVv[3Srb36gRZN{[Xl? NVTKeZFnOC5yMT2xNEDPxE1? NGTLc5gyQCCqwrC= NUS0XYVR[WO2aY\heIV{KHSqZTDFVmUudWWmaXH0[YQhfHKjboPjdolxfGmxbjDv[kBCTjKHUh?= MXuyN|c{OzF6OB?=
MCF-7L  NILy[4RHfW6ldHnvckBCe3OjeR?= NWexUGFvOTByIH7NxsA> NXfsRppLOTBibXnuM|I1KGhxNEigbC=> M1v4SpJme3WudIOgbY4hTUeIUjygTGVTOiCjbnSgTGVTOyCyaH;zdIhwenmuYYTpc44h[XRicILvcI9v\2WmIHX4dI9{fXKn MkLUNlM3QDZ2MU[=
MCF-7L  MXLGeY5kfGmxbjDBd5NigQ>? NIHIRlMyODBibl5CpC=> NFLHTG81QCCq MX3pcoR2[2W|IIXwdoVofWyjdHnvckBw\iCvUl7BJI9nKEWJRmKgcIlo[W6mIFjCMWVITg>? NXHUeVNTOjN4OE[0NVY>
MCF-7L NG\QeGZHfW6ldHnvckBCe3OjeR?= NXLJOVFiOTByIH7NxsA> MXu0PEBp MlztbY5lfWOnczDFS2ZTKG[jbXnsfUBu\W2kZYKgZYN1cX[jdHnvckBz\XG3aYLl[EBGWg>? MkLUNlM3QDZ2MU[=
C4-12  NFnmO5FHfW6ldHnvckBCe3OjeR?= MkDqNVAxKG6PwrC= NG\4bIU1QCCq M3HBO4lv\HWlZYOgSWdHWiCoYX3pcJkhdWWvYnXyJIFkfGm4YYTpc44hemWzdXny[YQhTVJ? M2DqPVI{Pjh4NEG2
MCF-7L M3WyZmZ2dmO2aX;uJGF{e2G7 NGnMPW4yODBibl5CpC=> M3ziWlI1KGh? NVjxNlZ2cW6mdXPld{BGT0[UIIDoc5NxcG:{eXzheIlwdiC{ZYH1bZJm\CCKQj3FS2Yh\nWwY4Tpc44> MXWyN|Y5PjRzNh?=
MMQ  NHjrNpNHfW6ldHnvckBCe3OjeR?= MofhNE03OjVibl2= MYi3NkBp NXXxZVFl\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[g[ZN1em:pZX6gdoVk\XC2b4Kt{tEhMEWUzsGp Ml70NlM2OjN|NUe=
H1975  M1;JTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYO2R|hKOC5|MUK1MVExKM7:TR?= NF;iT4Q3KGR? MUDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M{HO[lI{Ozl7OUW3
H1975  M1izPWFxd3C2b4Ppd{BCe3OjeR?= M3:xUFIxOCCwTR?= M3T2NVczKGh? NYjWR4dL\W6qYX7j[ZMh\XKub4TpcoljKGmwZIXj[YQh[XCxcITvd4l{ NUH4bmdlOjN|OUm5OVc>
MCF-7  NHjYOFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:zcW4yOC9zMECvNVAxOCCwTR?= M37hfFIwPC94IHS= MmP0SG1UVw>? MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ NXnldWFmOjN|MUO1NFY>
MCF-7  M1\pWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorYNVAxKG6P Ml7SOEBl MlnWSG1UVw>? NXjZcIlvcW6mdXPld{BiKGirZ3jldkBxem:yb4L0bY9vKG:oIHPlcIx{KGmwIITo[UBIOSCyaHHz[eKh M{mwRVI{OzF|NUC2
MLO-Y4  M3fFPWZ2dmO2aX;uJGF{e2G7 NH6z[pUyyqEQvF2= NFLue|EyKGh? NYWybVJscW6qaXLpeJMhTTJvaX7keYNm\CCFeESzJIV5eHKnc4Ppc44> NGHUVnczOzJ2N{C1Oy=>
MCF-7 NXvNSXI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqxNFAhdk1? MoLSOFghcA>? NEHxWVRi[nKxZ3H0[ZMhfGinIIDyc4xq\mW{YYTpeoUh\W[oZXP0JI9nKG2xZHXyZZRmKG6rdILvd4F1cX[nIIP0doV{ew>? MUeyN|IyPjd2NB?=
TG1-1  NFLhS4VHfW6ldHnvckBCe3OjeR?= NWrjT2JbOcLizszN MXyyOEBp MmLqZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x MViyN|A5QDZyNx?=
TG1-1  Mnm5SpVv[3Srb36gRZN{[Xl? MX[xxsDPxE1? MW[yOEBp NETwZmZi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKFCLM1u= NG\6W2UzOzB6OE[wOy=>
MCF7 NUG2ToEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPSXVcyODBibl2= Ml7oOFghcA>? NYPiclk2dGWjZIOgeI8h[SC|aX3pcIFzKGyxc4OgbY4he3W{dnn2ZYwh[XNid3n0bEBld3ixcoXibYNqdiCjbH;u[S=> MXeyN|A4PzJ2OR?=
MCF7 NFnaPXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33Jb|ExOCCwTR?= MVS0PEBp M1zSVYVvcGGwY3XzJI52fGyrbj3t[YRq[XSnZDDj[YxtKGSnYYTo M1q5N|I{ODd5MkS5
MCF-7  M1;p[GZ2dmO2aX;uJGF{e2G7 NXnB[JpVPiCq Mof3SG1UVw>? M2OxdYF1fGWwdXH0[ZMhfGinIH\seYRqd3ixbnnsMUBweiCoZX7o[ZhidWmmLXnu[JVk\WRiaX7jdoVie2ViaX6gcYlTNTJzIHX4dJJme3Orb36= NXjM[lJ3OjNyNUKwN|Y>
MCF-7 M1THVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLYOmIyODBibl2vNUDPxE1? M3zUXlUh\A>? NWTMRYdCcW6qaXLpeJMhfGinIIP0bY12dGG2aX;uJI9nKDF5zsKt[ZN1emGmaX;s MoGwNlI6QDJ5NkW=
MCF-7 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjtNVAxKG6P NUOz[3d7PSCm NI\ubXNqdmirYnn0d{B1cGVic4TpcZVt[XSrb36gc4Yh\nW|YYLp[YxqdiCK MU[yNlk5Ojd4NR?=
1471.1 NIPNR|lHfW6ldHnvckBCe3OjeR?= M13FSVExOCCwTR?= MWCxJIg> NXjDfZhRTXSRSNMg NV7k[XpqfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv NX\UXYFWOjJ6NkmxNFY>
MCF-7 M3Hr[mZ2dmO2aX;uJGF{e2G7 NYi1N2Q4OTByIH7N MXWxJIg> NEmwSmtGfE:KwrC= NXfq[o9TfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv Mof1NlI5PjlzME[=
HeLa M{\rVWZ2dmO2aX;uJGF{e2G7 MlO2NVAxKG6P NWLENYJxOSCq NUi5cVFMTXSRSNMg MWL0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= NUDkdoJDOjJ6NkmxNFY>
COS-7  NEiyRlJHfW6ldHnvckBCe3OjeR?= MY[xNFAhdk1? MnX3NUBp MWjFeG9JyqB? NVLyRnhFfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv MkHxNlI5PjlzME[=
BG1L-OHTLT  M1TpSGZ2dmO2aX;uJGF{e2G7 NV;WU3NqOTEEoH7N MVeyOOKhcMLi MljwbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w MVGyNlY2OjV3OB?=
BG1L-ICILT MnfZSpVv[3Srb36gRZN{[Xl? MWOxNOKhdk1? MViyOOKhcMLi MYjpcohq[mm2czDFVu6yKGW6cILld5Nqd25? NEfh[|QzOjZ3MkW1PC=>
PC-9 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[3NE4xODNvM{Cg{txO MYK0PEBp MVjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1ThTFIzPTZyNkO0
H1650 NYfXZWFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILIbVMxNjByMz2zNEDPxE1? MW[0PEBp NEfSWZlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NF3mfoczOjV4ME[zOC=>
H1975 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDBWmIxNjByMz2zNEDPxE1? NXjBeHF1PDhiaB?= MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NVuyOGF[OjJ3NkC2N|Q>
H1975 M2PKSWZ2dmO2aX;uJGF{e2G7 NYXCcXZ[O8LizszN NFzYUpk{KGh? MkLlZYJzd2ejdHXzJJRp\SCyaH;zdIhwNUWJRmKgbY5lfWO2aX;uJIJ6KGW|dILv[4Vv MU[yNlU3ODZ|NB?=
H1975 NXm5PHI{TnWwY4Tpc44hSXO|YYm= NWDlW5d7O8LizszN NYLlcVcyPyCm MnfnbY5lfWOnczDFS2ZTKGW6cILld5Nqd25? Mon0NlI2PjB4M{S=
HTR-8 NYDlNG9RTnWwY4Tpc44hSXO|YYm= NHjLeFAyyqEQvF2= NXi1TY5bOS12ODDo NXHaPG9u\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gTWdHSlB5IH3SUmE> NUnSe|V1OjJ|OEOxNVE>
JEG-3 NXrHRoljTnWwY4Tpc44hSXO|YYm= MmC5NeKh|ryP M3fYZ|EuPDhiaB?= M2rnOoRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B NFfNOYczOjN6M{GxNS=>
Huh7 NV\3Z|JLTnWwY4Tpc44hSXO|YYm= M4rKTFUxyqEQvF2= MV60PEBp NGr3SVhqdmirYnn0d{Bo\W6rc4TlbY4udWWmaXH0[YQhWE:QMTD0doFve2GldHn2ZZRqd25? MYiyNlMxPDJ7Nh?=
201T MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TvflUh|ryP NVraUop3PzJiaB?= M4HtTIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4YX7k[ZRidmmk MYCyNlI2QDR5Nh?=
A549  MnTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvQOUDPxE1? NYG5UmM3PzJiaB?= NG\WPGpqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnHu[IV1[W6rYh?= NWfpfYl2OjJ{NUi0O|Y>
MCF-7 MWrGeY5kfGmxbjDBd5NigQ>? NVzB[4x5OcLizszN MXWyOEBpyqB? M1LvbIRwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvckBqdmS3Y3XkJIJ6KDRvT1itWEDDqA>? NI\jSWgzOjB2OUOxOi=>
HCC-1428 MoDFSpVv[3Srb36gRZN{[Xl? MomxNeKh|ryP NF7STJMzPCCqwrC= NXvhbHhS\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi M2foXlIzODR7M{G2
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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

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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

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

Estrogen/progestogen Receptor Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID