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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3 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.

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3hTVEyNjNvMUCwNEBvVQ>? NILKeI01QCCq NYHZV5QxcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnrtNlQ6Pzl{OUS=
MCF-7/LTED MmHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXQ[FQyNjNvMUCwNEBvVQ>? NIq0S2o1QCCq MVHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MnW5NlQ6Pzl{OUS=
HCC1428 M1H5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo[xNU4{NTFyMECgcm0> NXvkVYdPPDhiaB?= NHX1VGZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mnu0NlQ6Pzl{OUS=
HCC1428/LTED MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXJNU4{NTFyMECgcm0> MXS0PEBp NIPDTYtqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MXyyOFk4QTJ7NB?=
LCC1 MlLlSpVv[3Srb36gRZN{[Xl? MoXJNVAxKG6P MUO0PE0yPDRiaB?= NGHFeJli[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= M{CwelI1QDV6Mke3
LCC9 NY\2[4RSTnWwY4Tpc44hSXO|YYm= NWmyWox6OTByIH7N M4HJclQ5NTF2NDDo MljKZYN1cX[jdHXzJHVRWiC|aXfuZYxqdmd? M3rjUlI1QDV6Mke3
MCF-7  MoO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGqxVGMyODBibl2= NF\NPYU2KGR? NX\aeXZPcW6qaXLpeJMh[2WubDDndo94fGhidH:gNVDwxIV? MlfaNlQ5OTl3NUC=
mesangial  NH\4bItHfW6ldHnvckBCe3OjeR?= MXKwMlEuOTByIH7N M{nLZlQ5KGh? MV\zeZBxemW|c3XzJHRITi4QskGtbY5lfWOnZDD0fZBmKEmYIHPvcIxi\2Ww NITOd2QzPDd7M{[zPS=>
Mesangial Mk\VSpVv[3Srb36gRZN{[Xl? Mnv4NE4yNTFyMDDuUS=> M3W4T|AvPSCq MoDKbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIGPtZYQzKHCqb4PwbI9zgWyjdHnvckB3cWFiR2DFVi=> MUWyOFc6OzZ|OR?=
ER+ MCF-7/2a NW\uW4VsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwMEC0JO69VQ>? MV:xOVMzPDh6NB?=
ER+ MCF-7 M4fi[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mln3NlAxKGh? MVHJR|UxRTBwMkGgcm0> MnzDNVU{OjR6OES=
MCF-7  M3PTcmZ2dmO2aX;uJGF{e2G7 NHPXTY4yOMLibl5CpC=> M{Xpc|czKGh? MkXvdoV3\XK|ZYOgeIhmKGW|dILv[4VvKGWoZnXjeEhKSzVyIEGuPUDEnyBzMPMIllkhVSl? NGTnenIzPDlyOE[1Ni=>
MCF-7  MnL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxyqCxZjDhdJBzd3irbXH0[Yx6KDJibl2= NVPOR49YOjN2NEizOFY>
H1975  M4\1PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{H2SVPDqM7:TR?= NH\rb|kyKG1? NVnoRotRcW6lcnXhd4V{KHSqZTDn[YZqfGmwaXKgd4Vve2m2aY\peJkhd2ZiSEG5O|Uh[2WubIRCpC=> NESwXIQzPDJ4OEixNC=>
H1975 MnjxSpVv[3Srb36gRZN{[Xl? MYKzxsDPxE1? M2TPd|EhdQ>? NV3ucmJ7fXC{ZXf1cIF1\XNidHjlJIxmfmWuIH;mJGxmfC15Yx?= M1fVTVI1OjZ6OEGw
MCF-7  M1:zdWZ2dmO2aX;uJGF{e2G7 MUWxNFDjiImwTdMg MkXmO|IhcA>? M3TpVZJmfmW{c3XzJJRp\SCycn;0[YN1cX[nIHXm[oVkfCCxZjDFNuKhcW5iY3XscEBqdn[jc3nvci=> M13iSVI{QTN4N{ez
MCF-7  M3LUcGZ2dmO2aX;uJGF{e2G7 NUP4eGZqOTBy4pEJcm3DqA>? MnW3NlQwPDhiaB?= MnL0[oFkcWyrdHH0[ZMhcW64YYPpc44hfGi{b4XnbEBOVVC|JzDtc4R2dGG2aX;u MYmyN|k{Pjd5Mx?=
BT474-tet-shMED1 MoThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrROlM2OC5zLUWg{txO MlTXO{Bl MnXZbY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MXKyN|k{PjJ|NB?=
ZR75-1-tet-shMED1  MoHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rzblAvOS13IN88US=> MkLtO{Bl MWDpcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MUeyN|k{PjJ|NB?=
MCF-7-tet-shMED1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\WPVAvOS13IN88US=> NVLodnM4PyCm MnL0bY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NXzFWWxKOjN7M{[yN|Q>
HepG2  NX;YXJE4TnWwY4Tpc44hSXO|YYm= NVWxPZhiOC5yMT2xNEDPxE1? M2PhdVE5KGkEoB?= NWHNRmg3[WO2aY\heIV{KHSqZTDFVmUudWWmaXH0[YQhfHKjboPjdolxfGmxbjDv[kBCTjKHUh?= MU[yN|c{OzF6OB?=
MCF-7L  MoiySpVv[3Srb36gRZN{[Xl? NUDyNYkxOTByIH7NxsA> MXuxNEBucW5xMkSgbE81QCCq MlHkdoV{fWy2czDpckBGT0[ULDDISXIzKGGwZDDISXI{KHCqb4PwbI9zgWyjdHnvckBifCCycn;sc45o\WRiZYjwc5N2emV? MonaNlM3QDZ2MU[=
MCF-7L  NYHuRXI{TnWwY4Tpc44hSXO|YYm= MmDsNVAxKG6PwrC= MoDROFghcA>? NYr2ZoRQcW6mdXPld{B2eHKnZ4XsZZRqd25ib3[gcXJPSSCxZjDFS2ZTKGyrZ3Hu[EBJSi2HR1[= NH\ZeFUzOzZ6NkSxOi=>
MCF-7L MUjGeY5kfGmxbjDBd5NigQ>? MVWxNFAhdk4EoB?= MlPsOFghcA>? NIL3NFVqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU NUfxZXVTOjN4OE[0NVY>
C4-12  MYrGeY5kfGmxbjDBd5NigQ>? NFLKOVEyODBibl5CpC=> NIfzcG01QCCq NXrwXoxmcW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= NF\odIYzOzZ6NkSxOi=>
MCF-7L MkjMSpVv[3Srb36gRZN{[Xl? MnHLNVAxKG6PwrC= MlXrNlQhcA>? MWjpcoR2[2W|IFXHSnIheGixc4Doc5J6dGG2aX;uJJJmeXWrcnXkJGhDNUWJRjDmeY5kfGmxbh?= MXGyN|Y5PjRzNh?=
MMQ  NYf6bnNvTnWwY4Tpc44hSXO|YYm= MlPLNE03OjVibl2= MV63NkBp MXHkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCnc4Tyc4dmdiC{ZXPldJRwei4QsTCoSXLPuSl? MYqyN|UzOzN3Nx?=
H1975  M3K4SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXqwMlMyOjVvMUCg{txO NUXhZ2cyPiCm NULwR3pbcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MmnLNlM{QTl7NUe=
H1975  MnTJRZBweHSxc3nzJGF{e2G7 M{[4RlIxOCCwTR?= NI\xSWc4OiCq NV3xZ4V5\W6qYX7j[ZMh\XKub4TpcoljKGmwZIXj[YQh[XCxcITvd4l{ MoHoNlM{QTl7NUe=
MCF-7  M1jTR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPnR5gzOTBxMUCwM|ExODBibl2= NIOyR4MzNzRxNjDk MXjEUXNQ M{XDNolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= MlvaNlM{OTN3ME[=
MCF-7  M1TKVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWO1WZpbOTByIH7N MWW0JIQ> M3nnPGROW09? NVfPVWFZcW6mdXPld{BiKGirZ3jldkBxem:yb4L0bY9vKG:oIHPlcIx{KGmwIITo[UBIOSCyaHHz[eKh NW\BfXpvOjN|MUO1NFY>
MLO-Y4  MmL6SpVv[3Srb36gRZN{[Xl? NGHEdXEyyqEQvF2= NYnmeWxsOSCq NUDG[WszcW6qaXLpeJMhTTJvaX7keYNm\CCFeESzJIV5eHKnc4Ppc44> MnXUNlMzPDdyNUe=
MCF-7 NH\lOnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrGNVAxKG6P NIX3cJA1QCCq NVzCSlBJ[WK{b3fheIV{KHSqZTDwdo9tcW[ncnH0bZZmKGWoZnXjeEBw\iCvb3TldoF1\SCwaYTyc5NifGm4ZTDzeJJme3N? NVLFXXFIOjN{MU[3OFQ>
TG1-1  NVP4PYU{TnWwY4Tpc44hSXO|YYm= M2rNSVHDqM7:TR?= NH3RdpczPCCq NIix[Gdi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKEiLRj2x{tE> NEPLS20zOzB6OE[wOy=>
TG1-1  MWnGeY5kfGmxbjDBd5NigQ>? MW[xxsDPxE1? MWWyOEBp MVzhZpJw\2G2ZYOgSVLDqGmwZIXj[YQh[WOldX31cIF1cW:wIH;mJHBKO0t? NH73UI0zOzB6OE[wOy=>
MCF7 NEj1bWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHFVVRWOTByIH7N NIKydXk1QCCq NGXIeott\WGmczD0c{BiKHOrbXnsZZIhdG:|czDpckB{fXK4aY\hcEBieyC5aYToJIRwgG:{dXLpZ4lvKGGub37l NEfucWkzOzB5N{K0PS=>
MCF7 MlzuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPRWWdpOTByIH7N NWLFb49xPDhiaB?= M4jkOIVvcGGwY3XzJI52fGyrbj3t[YRq[XSnZDDj[YxtKGSnYYTo Mnv1NlMxPzd{NEm=
MCF-7  M4Hy[2Z2dmO2aX;uJGF{e2G7 NHnubWw3KGh? MVLEUXNQ NGLzZYNifHSnboXheIV{KHSqZTDmcJVlcW:6b37pcE0hd3JiZnXubIV5[W2rZD3pcoR2[2WmIHnuZ5Jm[XOnIHnuJI1qWi1{MTDlfJBz\XO|aX;u M1X5OVI{ODV{MEO2
MCF-7 MojUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPBNVAxKG6PL{Gg{txO NI\1OFM2KGR? Ml7tbY5pcWKrdIOgeIhmKHO2aX31cIF1cW:wIH;mJFE4|rJvZYP0doFlcW:u MXmyNlk5Ojd4NR?=
MCF-7 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2xNFAhdk1? MmLOOUBl M2LObIlvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kBnfXOjcnnlcIlvKEh? NInjOXQzOjl6Mke2OS=>
1471.1 M{O3T2Z2dmO2aX;uJGF{e2G7 MnzkNVAxKG6P NV;XXINJOSCq MkX0SZRQUMLi MkTLeIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu NX\XN3l[OjJ6NkmxNFY>
MCF-7 NX;Rd|lpTnWwY4Tpc44hSXO|YYm= MXGxNFAhdk1? NV7ZSGpiOSCq NF7wSWJGfE:KwrC= NXe2eFRMfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv MmnpNlI5PjlzME[=
HeLa M{jWWGZ2dmO2aX;uJGF{e2G7 MYexNFAhdk1? MlvyNUBp MYPFeG9JyqB? MYT0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= NEHmO2ozOjh4OUGwOi=>
COS-7  M2H5S2Z2dmO2aX;uJGF{e2G7 MnnVNVAxKG6P MnLVNUBp MlXoSZRQUMLi MnrYeIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu M{XseFIzQDZ7MUC2
BG1L-OHTLT  MXvGeY5kfGmxbjDBd5NigQ>? M1nBVFExyqCwTR?= MUGyOOKhcMLi NHXMSG1qdmirYnn0d{BGWs7zIHX4dJJme3Orb36= NVHrRlRkOjJ4NUK1OVg>
BG1L-ICILT MWrGeY5kfGmxbjDBd5NigQ>? NWHaW3ZMOTEEoH7N M13aT|I1yqCqwrC= MYDpcohq[mm2czDFVu6yKGW6cILld5Nqd25? MlzxNlI3PTJ3NUi=
PC-9 M4r1ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LTXlAvODB|LUOwJO69VQ>? M2PXflQ5KGh? M13i[olvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIfNZm8zOjV4ME[zOC=>
H1650 MnTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v3PFAvODB|LUOwJO69VQ>? MVm0PEBp M{\tUYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2PtXFIzPTZyNkO0
H1975 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvmTnkxNjByMz2zNEDPxE1? NVf4NVZMPDhiaB?= NHf3O|ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4fRdlIzPTZyNkO0
H1975 MVvGeY5kfGmxbjDBd5NigQ>? Mn75N:Kh|ryP NH7Kb48{KGh? M3vkOoFjem:pYYTld{B1cGVicHjvd5Bpdy2HR1\SJIlv\HWldHnvckBjgSCnc4Tyc4dmdg>? MmDRNlI2PjB4M{S=
H1975 Mk\zSpVv[3Srb36gRZN{[Xl? MXSzxsDPxE1? NEfhboE4KGR? NGLXUnVqdmS3Y3XzJGVITlJiZYjwdoV{e2mxbh?= NWP2No5UOjJ3NkC2N|Q>
HTR-8 MXTGeY5kfGmxbjDBd5NigQ>? M33ybVHDqM7:TR?= M3HjcFEuPDhiaB?= M3HDNoRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B MWGyNlM5OzFzMR?=
JEG-3 MmXrSpVv[3Srb36gRZN{[Xl? MWKxxsDPxE1? NF3WRlEyNTR6IHi= M2nnZYRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B NUXBRolxOjJ|OEOxNVE>
Huh7 NHewO2xHfW6ldHnvckBCe3OjeR?= NIfUc3E2OMLizszN MlTKOFghcA>? M{HQR4lvcGmkaYTzJIdmdmm|dHXpck1u\WSrYYTl[EBRV05zIITyZY5{[WO2aY\heIlwdg>? NIfwc3kzOjNyNEK5Oi=>
201T NYrC[m1RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUOyZ3pyPSEQvF2= NEHqUoU4OiCq Ml3ibY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? MUWyNlI2QDR5Nh?=
A549  MnfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmH1OUDPxE1? MXq3NkBp MmH0bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? Mk\2NlIzPTh2N{[=
MCF-7 NVPiN5RjTnWwY4Tpc44hSXO|YYm= NWrtZVExOcLizszN NGTxdGwzPCCqwrC= NHrXSXVld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? NVrkTGdoOjJyNEmzNVY>
HCC-1428 NITNVXlHfW6ldHnvckBCe3OjeR?= MYexxsDPxE1? NF3jcmEzPCCqwrC= MXjkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb36gbY5lfWOnZDDifUA1NU:KLWSgxsA> MV:yNlA1QTNzNh?=
MDA-361 Mmj4SpVv[3Srb36gRZN{[Xl? NG[yR5YyyqEQvF2= NHzzN5YzPCCqwrC= MWTkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb36gbY5lfWOnZDDifUA1NU:KLWSgxsA> MnnBNlIxPDl|MU[=
ZR75-1 NH\ZNIRHfW6ldHnvckBCe3OjeR?= NXqxbFI1OcLizszN NHfkXYMzPCCqwrC= NFH6OnZld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? M3nlN|IzODR7M{G2
MCF-7 MkP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3iN5UyyqEQvF2= NWDSVnFMPS1zMDDk MWrzeZBxemW|c3XzJGUzNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> M2m3d|IzODR7M{G2
HCC-1428 M3q2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXqxxsDPxE1? MXS1MVExKGR? NIi1eYl{fXCycnXzd4V{KEV{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? NYjvb3g4OjJyNEmzNVY>
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MCF7 NXH6[IdkTnWwY4Tpc44hSXO|YYm= MYKxNFAhdk1? NWjwTHp1PyCm M1vlWZJm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> NXrPemRFOjF|OU[wPVQ>
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MCF7 NEGwVIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF2yeo0xNjBzLUGg{txO NUnBRmo2PyCm MXzy[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? NIHsNpkzOTN7NkC5OC=>
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MCF7 NXX2O|ZWTnWwY4Tpc44hSXO|YYm= M2PkSlExOCCwTR?= M3jDPVch\A>? MXnpcoR2[2W|IH;mJGVz[kJ|IHHu[EBGemKENDDy[YNmeHSxcjDlfJBz\XO|aX;uJIFv\CC|aXfuZYxtcW6p M2DVXFIyOzl4MEm0
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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 <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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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