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, 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 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVOxMlMuOTByMDDuUS=> M1fsRlQ5KGh? Ml\JbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M{TLfFI1QTd7Mkm0
MCF-7/LTED MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:xMlMuOTByMDDuUS=> NIXuSWo1QCCq M3K0Z4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MkjBNlQ6Pzl{OUS=
HCC1428 NWKwR4N7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXTOngyNjNvMUCwNEBvVQ>? M3HSOVQ5KGh? M3HobolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4TpVVI1QTd7Mkm0
HCC1428/LTED NEjObWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jITVEvOy1zMECwJI5O NYfQcFcxPDhiaB?= MoS3bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUnYdIJCOjR7N{myPVQ>
LCC1 MX\GeY5kfGmxbjDBd5NigQ>? NHm4WlUyODBibl2= NYnRNWZ3PDhvMUS0JIg> MnLpZYN1cX[jdHXzJHVRWiC|aXfuZYxqdmd? M1\EeVI1QDV6Mke3
LCC9 NXjhd41UTnWwY4Tpc44hSXO|YYm= NUnlb5luOTByIH7N MYi0PE0yPDRiaB?= M{PSWYFkfGm4YYTld{BWWFJic3nncoFtcW6p M322dVI1QDV6Mke3
MCF-7  M1fzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXMNVAxKG6P NFWzWoM2KGR? NX7mbId[cW6qaXLpeJMh[2WubDDndo94fGhidH:gNVDwxIV? NUPmO5I1OjR6MUm1OVA>
mesangial  MXnGeY5kfGmxbjDBd5NigQ>? MmToNE4yNTFyMDDuUS=> MXy0PEBp M2LpNpN2eHC{ZYPz[ZMhXEeILd8yNU1qdmS3Y3XkJJR6eGViSW[gZ49tdGGpZX6= MYiyOFc6OzZ|OR?=
Mesangial Ml;tSpVv[3Srb36gRZN{[Xl? NF\KZncxNjFvMUCwJI5O NY\USphUOC53IHi= Mk\CbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIGPtZYQzKHCqb4PwbI9zgWyjdHnvckB3cWFiR2DFVi=> MXWyOFc6OzZ|OR?=
ER+ MCF-7/2a NVL2XoRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVe2c45PUUN3ME2wMlAxPCEQvF2= M4KxdVE2OzJ2OEi0
ER+ MCF-7 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoS4NlAxKGh? NU\tb|hOUUN3ME2wMlIyKG6P MWixOVMzPDh6NB?=
MCF-7  NVTicot3TnWwY4Tpc44hSXO|YYm= NF;hVFEyOMLibl5CpC=> M{fhW|czKGh? NGnQe|lz\X[ncoPld{B1cGViZYP0do9o\W5iZX\m[YN1MEmFNUCgNU46KMPZIEGw5qiTQSCPKR?= M2HieFI1QTB6NkWy
MCF-7  NFzUTolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHHW4dKSzVywrDv[kBieHC{b4jpcYF1\Wy7IEKgcm0> NVXmZVZTOjN2NEizOFY>
H1975  NUmwdG5nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCzxsDPxE1? MYWxJI0> MmLybY5kemWjc3XzJJRp\SCpZX\peIlvcWJic3Xud4l1cX[rdImgc4YhUDF7N{WgZ4VtdHQEoB?= MVmyOFI3QDhzMB?=
H1975 M1vxU2Z2dmO2aX;uJGF{e2G7 MnPQN:Kh|ryP MnXyNUBu MXL1dJJm\3WuYYTld{B1cGVibHX2[Ywhd2ZiTHX0MVdk Mk\wNlQzPjh6MUC=
MCF-7  NVnCU5Z{TnWwY4Tpc44hSXO|YYm= M{D2VVExOOLCiX7NxsA> NWXsTJdiPzJiaB?= MX\y[ZZmenOnczD0bIUheHKxdHXjeIl3\SCnZn\lZ5Qhd2ZiRUNCpIlvKGOnbHygbY53[XOrb36= NYf0Rm5UOjN7M{[3O|M>
MCF-7  MX3GeY5kfGmxbjDBd5NigQ>? NIXYU|gyODEkgJnuUeKh NWfkfFZKOjRxNEigbC=> MYTmZYNqdGm2YYTld{Bqdn[jc3nvckB1cHKxdXfoJG1OWHNpIH3v[JVt[XSrb36= M2HvZlI{QTN4N{ez
BT474-tet-shMED1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvsNE4yNTVizszN M1vlZlch\A>? M4HDNIlv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MnWzNlM6OzZ{M{S=
ZR75-1-tet-shMED1  M3nKNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;ZZWkxNjFvNTFOwG0> Mn7MO{Bl M3rR[olv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M1fxVFI{QTN4MkO0
MCF-7-tet-shMED1 NUPCVG1ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DxUFAvOS13IN88US=> M1L5d|ch\A>? MmPobY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MofkNlM6OzZ{M{S=
HepG2  MonxSpVv[3Srb36gRZN{[Xl? MnPrNE4xOS1zMDFOwG0> NVnoe2tQOThiaNMg NH2wfoZi[3SrdnH0[ZMhfGinIFXSSU1u\WSrYYTl[EB1emGwc3PybZB1cW:wIH;mJGFHOkWU MoP6NlM4OzNzOEi=
MCF-7L  MofKSpVv[3Srb36gRZN{[Xl? NGOwZlMyODBibl5CpC=> NXTBWoRXOTBibXnuM|I1KGhxNEigbC=> NYfISo94emW|dXz0d{BqdiCHR1\SMEBJTVJ{IHHu[EBJTVJ|IIDoc5NxcG:{eXzheIlwdiCjdDDwdo9td26pZXSg[Zhxd3O3cnW= M1fWV|I{Pjh4NEG2
MCF-7L  M3jMVWZ2dmO2aX;uJGF{e2G7 MkHNNVAxKG6PwrC= MkKzOFghcA>? MX\pcoR2[2W|IIXwdoVofWyjdHnvckBw\iCvUl7BJI9nKEWJRmKgcIlo[W6mIFjCMWVITg>? NXXySXp[OjN4OE[0NVY>
MCF-7L M3LYPGZ2dmO2aX;uJGF{e2G7 NWnyWG1ROTByIH7NxsA> NFWwdY01QCCq NWW0b|hZcW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= NVjQRY1QOjN4OE[0NVY>
C4-12  MV3GeY5kfGmxbjDBd5NigQ>? MXqxNFAhdk4EoB?= MUC0PEBp MXvpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT NHrYSm4zOzZ6NkSxOi=>
MCF-7L MY\GeY5kfGmxbjDBd5NigQ>? M1\TclExOCCwTdMg NWXtWFNbOjRiaB?= NXP1c2l5cW6mdXPld{BGT0[UIIDoc5NxcG:{eXzheIlwdiC{ZYH1bZJm\CCKQj3FS2Yh\nWwY4Tpc44> MljoNlM3QDZ2MU[=
MMQ  NIHmbZJHfW6ldHnvckBCe3OjeR?= MnrUNE03OjVibl2= MmHmO|IhcA>? MX;kc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCnc4Tyc4dmdiC{ZXPldJRwei4QsTCoSXLPuSl? MX6yN|UzOzN3Nx?=
H1975  MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXewMlMyOjVvMUCg{txO NGLCN|Q3KGR? M3XpTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MoPwNlM{QTl7NUe=
H1975  NIHDb|FCeG:ydH;zbZMhSXO|YYm= MlPyNlAxKG6P MorOO|IhcA>? MkLB[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz MYCyN|M6QTl3Nx?=
MCF-7  MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfWNVAwOTByL{GwNFAhdk1? M2\6flIwPC94IHS= NXfBfWZpTE2VTx?= M{jD[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= NV6yZppOOjN|MUO1NFY>
MCF-7  NIHVRYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUCxNFAhdk1? NF:2eHY1KGR? M4qzXmROW09? M2nrcYlv\HWlZYOgZUBpcWeqZYKgdJJweG:{dHnvckBw\iClZXzsd{BqdiC2aHWgS|EheGijc3ZCpC=> M2XCWVI{OzF|NUC2
MLO-Y4  MX7GeY5kfGmxbjDBd5NigQ>? M4\wN|HDqM7:TR?= M{DvRVEhcA>? MlKzbY5pcWKrdIOgSVIucW6mdXPl[EBEgDR|IHX4dJJme3Orb36= NV34WlFtOjN{NEewOVc>
MCF-7 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXixNFAhdk1? NHTrcFI1QCCq M{TOc4Fjem:pYYTld{B1cGVicILvcIln\XKjdHn2[UBm\m[nY4Sgc4YhdW:mZYLheIUhdmm2cn;zZZRqfmVic4Ty[ZN{ MWKyN|IyPjd2NB?=
TG1-1  NIfTemNHfW6ldHnvckBCe3OjeR?= M{DlT|HDqM7:TR?= MkjjNlQhcA>? MkTsZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x MlTVNlMxQDh4MEe=
TG1-1  Mn;ESpVv[3Srb36gRZN{[Xl? M2Cw[lHDqM7:TR?= MVuyOEBp MmfZZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBRUTON MnnnNlMxQDh4MEe=
MCF7 M3\ZN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\zUWwyODBibl2= MXW0PEBp NXP1UZpudGWjZIOgeI8h[SC|aX3pcIFzKGyxc4OgbY4he3W{dnn2ZYwh[XNid3n0bEBld3ixcoXibYNqdiCjbH;u[S=> NGPTdJkzOzB5N{K0PS=>
MCF7 MoPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7hZYUyODBibl2= NUj1R21JPDhiaB?= NGSyXW1mdmijbnPld{BvfXSuaX6tcYVlcWG2ZXSgZ4VtdCCmZXH0bC=> NGPTb4gzOzB5N{K0PS=>
MCF-7  NHruO2lHfW6ldHnvckBCe3OjeR?= M{XFPVYhcA>? NV61b|F4TE2VTx?= M3ewbYF1fGWwdXH0[ZMhfGinIH\seYRqd3ixbnnsMUBweiCoZX7o[ZhidWmmLXnu[JVk\WRiaX7jdoVie2ViaX6gcYlTNTJzIHX4dJJme3Orb36= M2D3WVI{ODV{MEO2
MCF-7 MnvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7xVIJNOTByIH7NM|Eh|ryP M2S0WVUh\A>? MUHpcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[gNVfPui2nc4TyZYRqd2x? M4KwVFIzQTh{N{[1
MCF-7 Mn7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjMc|NOOTByIH7N M3vsWlUh\A>? MXPpcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[g[pV{[XKrZXzpckBJ M4PvbFIzQTh{N{[1
1471.1 M2XCWWZ2dmO2aX;uJGF{e2G7 MXOxNFAhdk1? NEPO[3oyKGh? M1LFOGV1V0kEoB?= MYf0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= MX:yNlg3QTFyNh?=
MCF-7 MVrGeY5kfGmxbjDBd5NigQ>? NInVcIMyODBibl2= MX:xJIg> M{DtSGV1V0kEoB?= MmHGeIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu MX6yNlg3QTFyNh?=
HeLa MljiSpVv[3Srb36gRZN{[Xl? NHTlSJQyODBibl2= MVexJIg> NFrTTlFGfE:KwrC= NWjhSnBZfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv NF31NJIzOjh4OUGwOi=>
COS-7  M2HrXWZ2dmO2aX;uJGF{e2G7 MWixNFAhdk1? M{TwT|EhcA>? M4W1b2V1V0kEoB?= MVv0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= M1TqPFIzQDZ7MUC2
BG1L-OHTLT  MlK5SpVv[3Srb36gRZN{[Xl? M1HEV|ExyqCwTR?= NGq5R4czPMLiaNMg MX3pcohq[mm2czDFVu6yKGW6cILld5Nqd25? M36y[|IzPjV{NUW4
BG1L-ICILT NGS0cJlHfW6ldHnvckBCe3OjeR?= MkHrNVDDqG6P NU\TW2xrOjUEoHlCpC=> MoDwbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w MlPMNlI3PTJ3NUi=
PC-9 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\YNE4xODNvM{Cg{txO M1:3NlQ5KGh? MkHrbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NF;nS|kzOjV4ME[zOC=>
H1650 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37TVlAvODB|LUOwJO69VQ>? NYftXGc{PDhiaB?= M2nkTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1;nRVIzPTZyNkO0
H1975 M4OyTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DvelAvODB|LUOwJO69VQ>? M1\lUVQ5KGh? M2nkOolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Moe4NlI2PjB4M{S=
H1975 MmjsSpVv[3Srb36gRZN{[Xl? NYS1[FlVO8LizszN NH7CdZo{KGh? NEW4S3Ri[nKxZ3H0[ZMhfGinIIDoc5NxcG9vRVfGVkBqdmS3Y4Tpc44h[nliZYP0do9o\W5? NGL1fnEzOjV4ME[zOC=>
H1975 NIjpem5HfW6ldHnvckBCe3OjeR?= MXuzxsDPxE1? NFHHeW44KGR? MnHhbY5lfWOnczDFS2ZTKGW6cILld5Nqd25? NH3KfGEzOjV4ME[zOC=>
HTR-8 MkTYSpVv[3Srb36gRZN{[Xl? NXvyZVY5OcLizszN MoDxNU01QCCq NHTOXWRld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDJS2ZDWDdibWLORS=> NEXiSI8zOjN6M{GxNS=>
JEG-3 MVvGeY5kfGmxbjDBd5NigQ>? MVqxxsDPxE1? MVuxMVQ5KGh? NFfvVVVld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDJS2ZDWDdibWLORS=> MnLMNlI{QDNzMUG=
Huh7 MlXxSpVv[3Srb36gRZN{[Xl? NVrxelVLPTEEoN88US=> MmXGOFghcA>? NITKOXVqdmirYnn0d{Bo\W6rc4TlbY4udWWmaXH0[YQhWE:QMTD0doFve2GldHn2ZZRqd25? M3PxR|IzOzB2Mkm2
201T NWfQ[|hFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfsTFk2KM7:TR?= NWnyV4xlPzJiaB?= M{PLe4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4YX7k[ZRidmmk NIHJfFQzOjJ3OES3Oi=>
A549  M1nXS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1K0OVUh|ryP MV[3NkBp Mn\abY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? M3;yNlIzOjV6NEe2
MCF-7 NGfjVlZHfW6ldHnvckBCe3OjeR?= Mn;KNeKh|ryP NYPJWWZGOjRiaNMg NGnsWWRld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? M4PLUFIzODR7M{G2
HCC-1428 MoLRSpVv[3Srb36gRZN{[Xl? MWSxxsDPxE1? NVjZcY1[OjRiaNMg NVuwVVJp\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi Mn7aNlIxPDl|MU[=
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MCF7S NYjpZmFMTnWwY4Tpc44hSXO|YYm= NXXsXJAzOcLizszN M4fwO|ch\A>? NIPB[HRifHSnboXheIV{KHS3bX;yd5Bp\XKnIH\vdo1ifGmxbjDhcoQheHKxbHnm[ZJifGmxbh?= NYTEdlVuOjF3M{OxPVU>
MCF7S NFWyVJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjUTolEOC53L{Gg{txO M4XmdFch\A>? MXfEUXNQ NVLRVVJ[\GWlcnXhd4V{KGOnbHyg[Zhx[W6|aX;u NETBdJczOTV|M{G5OS=>
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T47D  NXuwdINDTnWwY4Tpc44hSXO|YYm= MWGxNFAhdk1? MWC3JIQ> NIDNNXRz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 NYr4dYxCOjF|OU[wPVQ>
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T47D  NFHIeFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fjNlAvODFvMTFOwG0> MUC3JIQ> NIfqTYVz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3L1dlIyOzl4MEm0
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MCF7 NFztWIFHfW6ldHnvckBCe3OjeR?= NIT3c4EyODBibl2= NU[4bo1zPyCm MYjpcoR2[2W|IH;mJGVz[kJ|IHHu[EBGemKENDDy[YNmeHSxcjDlfJBz\XO|aX;uJIFv\CC|aXfuZYxtcW6p NYrQfnlCOjF|OU[wPVQ>
T47D  NG\FOI9HfW6ldHnvckBCe3OjeR?= M1nrR|ExOCCwTR?= MX23JIQ> MkXnbY5lfWOnczDv[kBGemKEMzDhcoQhTXKkQkSgdoVk\XC2b4Kg[ZhxemW|c3nvckBidmRic3nncoFtdGmwZx?= MVuyNVM6PjB7NB?=
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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 slightly soluble or insoluble
In vivo Add solvents individually and in order:
5% DMSO+95% Corn oil
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

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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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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID