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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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 Ml3IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7mcYlwOS5|LUGwNFAhdk1? NWXQeHd6PDhiaB?= MUXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHnGTWUzPDl5OUK5OC=>
MCF-7/LTED M4TsW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuxMlMuOTByMDDuUS=> NHPDZmk1QCCq NEjv[GRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVmyOFk4QTJ7NB?=
HCC1428 M3fYdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKxMlMuOTByMDDuUS=> NHrBWpk1QCCq MYXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFi2XXEzPDl5OUK5OC=>
HCC1428/LTED MmG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDVOYtDOS5|LUGwNFAhdk1? NHnFUGM1QCCq MmnubY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NGf2bpQzPDl5OUK5OC=>
LCC1 M3T5[mZ2dmO2aX;uJGF{e2G7 MoLUNVAxKG6P MXS0PE0yPDRiaB?= MnPVZYN1cX[jdHXzJHVRWiC|aXfuZYxqdmd? MWmyOFg2QDJ5Nx?=
LCC9 NFnOWmlHfW6ldHnvckBCe3OjeR?= MX2xNFAhdk1? MWe0PE0yPDRiaB?= M2\Cd4FkfGm4YYTld{BWWFJic3nncoFtcW6p MljqNlQ5PTh{N{e=
MCF-7  MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVX2UWIyOTByIH7N MXq1JIQ> NHi2bphqdmirYnn0d{Bk\WyuIHfyc5d1cCC2bzCxNQ+9jQ>? MXuyOFgyQTV3MB?=
mesangial  M1SwVmZ2dmO2aX;uJGF{e2G7 M37xWVAvOS1zMECgcm0> MWK0PEBp NV;hRW1se3WycILld5NmeyCWR1[t{tIyNWmwZIXj[YQhfHmyZTDJWkBkd2yuYXflci=> NF\nR2UzPDd7M{[zPS=>
Mesangial M3X4WWZ2dmO2aX;uJGF{e2G7 MWKwMlEuOTByIH7N M2H5TlAvPSCq MVjpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRiU33h[FIheGixc4Doc5J6dGG2aX;uJJZq[SCJUFXS M2j4WFI1Pzl|NkO5
ER+ MCF-7/2a NYnHZ|h7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTBwMEC0JO69VQ>? NYrl[3pEOTV|MkS4PFQ>
ER+ MCF-7 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKyNFAhcA>? MlS1TWM2OD1yLkKxJI5O MXOxOVMzPDh6NB?=
MCF-7  MWjGeY5kfGmxbjDBd5NigQ>? NECzW3AyOMLibl5CpC=> MlnTO|IhcA>? NW[3W4ZbemW4ZYLz[ZMhfGinIHXzeJJw\2WwIHXm[oVkfCiLQ{WwJFEvQSEFlzCxNQKJmjliTTm= NVLEV4JTOjR7MEi2OVI>
MCF-7  MnG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPvZZFKSzVywrDv[kBieHC{b4jpcYF1\Wy7IEKgcm0> MUKyN|Q1QDN2Nh?=
H1975  NFzTPWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYizxsDPxE1? MWmxJI0> MXzpcoNz\WG|ZYOgeIhmKGenZnn0bY5q[iC|ZX7zbZRqfmm2eTDv[kBJOTl5NTDj[Yxte8Li MlXYNlQzPjh6MUC=
H1975 M13rdWZ2dmO2aX;uJGF{e2G7 MX[zxsDPxE1? MYmxJI0> M1HSOZVxemWpdXzheIV{KHSqZTDs[ZZmdCCxZjDM[ZQuP2N? NUniZ|IzOjR{Nki4NVA>
MCF-7  NF\zdllHfW6ldHnvckBCe3OjeR?= M1;4XlExOOLCiX7NxsA> NET3dYg4OiCq MnrpdoV3\XK|ZYOgeIhmKHC{b4TlZ5RqfmViZX\m[YN1KG:oIFWyxsBqdiClZXzsJIlvfmG|aX;u M3fofFI{QTN4N{ez
MCF-7  NV[yWIdWTnWwY4Tpc44hSXO|YYm= MlLrNVAx6oDLbl5CpC=> M{HaeVI1NzR6IHi= MXHmZYNqdGm2YYTld{Bqdn[jc3nvckB1cHKxdXfoJG1OWHNpIH3v[JVt[XSrb36= Ml\MNlM6OzZ5N{O=
BT474-tet-shMED1 M3ezOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYiwMlEuPSEQvF2= NELpWYI4KGR? NWr5UG9RcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MoXVNlM6OzZ{M{S=
ZR75-1-tet-shMED1  NYrR[3c2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGWzZnUxNjFvNTFOwG0> MlWwO{Bl NGnISVVqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NYCxR3dCOjN7M{[yN|Q>
MCF-7-tet-shMED1 MmmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHwZmkxNjFvNTFOwG0> NVrsXnVMPyCm MoG4bY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MVuyN|k{PjJ|NB?=
HepG2  M3;LV2Z2dmO2aX;uJGF{e2G7 NUfQcZo{OC5yMT2xNEDPxE1? MkPINVghcMLi MYDhZ5RqfmG2ZYOgeIhmKEWURT3t[YRq[XSnZDD0doFve2O{aYD0bY9vKG:oIFHGNmVT MV:yN|c{OzF6OB?=
MCF-7L  MVPGeY5kfGmxbjDBd5NigQ>? M1\RXFExOCCwTdMg NGSyOIIyOCCvaX6vNlQhcC92ODDo M3LV[5Jme3WudIOgbY4hTUeIUjygTGVTOiCjbnSgTGVTOyCyaH;zdIhwenmuYYTpc44h[XRicILvcI9v\2WmIHX4dI9{fXKn M{PsRlI{Pjh4NEG2
MCF-7L  NVr1UoFVTnWwY4Tpc44hSXO|YYm= M{S3OFExOCCwTdMg MYK0PEBp NWrj[lhHcW6mdXPld{B2eHKnZ4XsZZRqd25ib3[gcXJPSSCxZjDFS2ZTKGyrZ3Hu[EBJSi2HR1[= NXT5dWtLOjN4OE[0NVY>
MCF-7L MXrGeY5kfGmxbjDBd5NigQ>? NFm4[lcyODBibl5CpC=> NFzjWpA1QCCq MXnpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT MlT6NlM3QDZ2MU[=
C4-12  NV6yd29QTnWwY4Tpc44hSXO|YYm= M3XVV|ExOCCwTdMg M4PqdlQ5KGh? M1;5Rolv\HWlZYOgSWdHWiCoYX3pcJkhdWWvYnXyJIFkfGm4YYTpc44hemWzdXny[YQhTVJ? NF6zZ4wzOzZ6NkSxOi=>
MCF-7L NF\K[4ZHfW6ldHnvckBCe3OjeR?= NV7SdJVPOTByIH7NxsA> MUWyOEBp NF7aWHFqdmS3Y3XzJGVITlJicHjvd5Bpd3K7bHH0bY9vKHKncYXpdoVlKEiELVXHSkBnfW6ldHnvci=> MWOyN|Y5PjRzNh?=
MMQ  Mkf5SpVv[3Srb36gRZN{[Xl? M4fWUVAuPjJ3IH7N MlH1O|IhcA>? MUHkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCnc4Tyc4dmdiC{ZXPldJRwei4QsTCoSXLPuSl? NWLhXGdoOjN3MkOzOVc>
H1975  MoTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mli1NE4{OTJ3LUGwJO69VQ>? M4PHXFYh\A>? Mk\abY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFvrcVYzOzN7OUm1Oy=>
H1975  MVrBdI9xfG:|aYOgRZN{[Xl? MVuyNFAhdk1? M1vtNlczKGh? Mmfk[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz NEXVeoUzOzN7OUm1Oy=>
MCF-7  MlTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fRVlExNzFyMD:xNFAxKG6P M1;2fFIwPC94IHS= MVjEUXNQ NFrRTpFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy Ml\0NlM{OTN3ME[=
MCF-7  NWnqPG5jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XQRVExOCCwTR?= NHzLT481KGR? NWfi[GU1TE2VTx?= NUHqNVNJcW6mdXPld{BiKGirZ3jldkBxem:yb4L0bY9vKG:oIHPlcIx{KGmwIITo[UBIOSCyaHHz[eKh NGO5c4YzOzNzM{WwOi=>
MLO-Y4  M3LDfmZ2dmO2aX;uJGF{e2G7 M3vUelHDqM7:TR?= NGHvTI8yKGh? MUjpcohq[mm2czDFNk1qdmS3Y3XkJGN5PDNiZYjwdoV{e2mxbh?= Mmr1NlMzPDdyNUe=
MCF-7 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;NbYoyODBibl2= MYm0PEBp NHmzfoli[nKxZ3H0[ZMhfGinIIDyc4xq\mW{YYTpeoUh\W[oZXP0JI9nKG2xZHXyZZRmKG6rdILvd4F1cX[nIIP0doV{ew>? MWKyN|IyPjd2NB?=
TG1-1  NU\VOmVKTnWwY4Tpc44hSXO|YYm= MkjDNeKh|ryP NGXKfWEzPCCq NH;zfGpi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKEiLRj2x{tE> NWL3NXJ6OjNyOEi2NFc>
TG1-1  NEK2bWRHfW6ldHnvckBCe3OjeR?= MW[xxsDPxE1? MYGyOEBp MknIZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBRUTON MmO4NlMxQDh4MEe=
MCF7 NXXlUI9sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV[xNFAhdk1? M3e3ZlQ5KGh? NFTKWFht\WGmczD0c{BiKHOrbXnsZZIhdG:|czDpckB{fXK4aY\hcEBieyC5aYToJIRwgG:{dXLpZ4lvKGGub37l M1zNdVI{ODd5MkS5
MCF7 NIn2dYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVexNFAhdk1? MW[0PEBp NHXrV21mdmijbnPld{BvfXSuaX6tcYVlcWG2ZXSgZ4VtdCCmZXH0bC=> NFjER|gzOzB5N{K0PS=>
MCF-7  NWC5Z|RuTnWwY4Tpc44hSXO|YYm= MojHOkBp NEDPZ4NFVVOR MYTheJRmdnWjdHXzJJRp\SCobIXkbY95d26rbD2gc5Ih\mWwaHX4ZY1q\C2rbnT1Z4VlKGmwY4LlZZNmKGmwIH3pVk0zOSCneIDy[ZN{cW:w NXrvN4dwOjNyNUKwN|Y>
MCF-7 MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2xNFAhdk1xMTFOwG0> MWO1JIQ> NFrUNlRqdmirYnn0d{B1cGVic4TpcZVt[XSrb36gc4YhOTgQsj3ld5Rz[WSrb3y= M{nzNFIzQTh{N{[1
MCF-7 MnPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX:xNFAhdk1? NEjLcXI2KGR? M2rlR4lvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kBnfXOjcnnlcIlvKEh? M2TVUlIzQTh{N{[1
1471.1 NE\1TIdHfW6ldHnvckBCe3OjeR?= MVexNFAhdk1? MnzHNUBp MXXFeG9JyqB? MV70ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= M1jGUlIzQDZ7MUC2
MCF-7 NVHze3ViTnWwY4Tpc44hSXO|YYm= MYqxNFAhdk1? MUOxJIg> NXvBNZJQTXSRSNMg NX3DRlgyfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv MUeyNlg3QTFyNh?=
HeLa MVLGeY5kfGmxbjDBd5NigQ>? NWP1fXF3OTByIH7N MoXTNUBp NXXW[nRiTXSRSNMg NWS0O4V3fGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv M{noXVIzQDZ7MUC2
COS-7  MVTGeY5kfGmxbjDBd5NigQ>? Mmj0NVAxKG6P NHe4XIwyKGh? MkDTSZRQUMLi NFXlTlB1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> Ml24NlI5PjlzME[=
BG1L-OHTLT  NGWyOodHfW6ldHnvckBCe3OjeR?= MXmxNOKhdk1? NYWzV2VHOjUEoHlCpC=> MXHpcohq[mm2czDFVu6yKGW6cILld5Nqd25? MnW4NlI3PTJ3NUi=
BG1L-ICILT NVLIflk1TnWwY4Tpc44hSXO|YYm= NEP1RnYyOMLibl2= NIrLZWIzPMLiaNMg MVvpcohq[mm2czDFVu6yKGW6cILld5Nqd25? NVjyRlV4OjJ4NUK1OVg>
PC-9 NGLNfpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fxUFAvODB|LUOwJO69VQ>? M3nmNVQ5KGh? MWXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWrNT5JyOjJ3NkC2N|Q>
H1650 NVfJ[2lFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHId5AxNjByMz2zNEDPxE1? NWPtUGVZPDhiaB?= M3nSV4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXGyNlU3ODZ|NB?=
H1975 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\xe2NjOC5yMEOtN|Ah|ryP NX3NWYtGPDhiaB?= NUn2XpB3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NF7uNXUzOjV4ME[zOC=>
H1975 MXPGeY5kfGmxbjDBd5NigQ>? MmXaN:Kh|ryP Ml[0N{Bp M2\LW4Fjem:pYYTld{B1cGVicHjvd5Bpdy2HR1\SJIlv\HWldHnvckBjgSCnc4Tyc4dmdg>? M{HGUFIzPTZyNkO0
H1975 MVLGeY5kfGmxbjDBd5NigQ>? NEnES2Y{yqEQvF2= MUO3JIQ> NEjjUnRqdmS3Y3XzJGVITlJiZYjwdoV{e2mxbh?= NI[x[XozOjV4ME[zOC=>
HTR-8 MoTZSpVv[3Srb36gRZN{[Xl? MYOxxsDPxE1? Mm\yNU01QCCq M2XuToRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B NXPPc3Y2OjJ|OEOxNVE>
JEG-3 MWfGeY5kfGmxbjDBd5NigQ>? NXuzRm43OcLizszN Mo[2NU01QCCq M{TTZoRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B M4TGdFIzOzh|MUGx
Huh7 MUHGeY5kfGmxbjDBd5NigQ>? NV;vXopZPTEEoN88US=> NX\oXlFTPDhiaB?= MXfpcohq[mm2czDn[Y5qe3SnaX6tcYVlcWG2ZXSgVG9POSC2cnHud4FkfGm4YYTpc44> MYiyNlMxPDJ7Nh?=
201T MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLYOUDPxE1? NGPsXWs4OiCq M1qyZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4YX7k[ZRidmmk M{jPblIzOjV6NEe2
A549  MlHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\CbIFkPSEQvF2= NX65NZplPzJiaB?= NWLWTml4cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\hcoRmfGGwaXK= NHjIbYIzOjJ3OES3Oi=>
MCF-7 MV\GeY5kfGmxbjDBd5NigQ>? MY[xxsDPxE1? NXHSSmR{OjRiaNMg Mmj4[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh NIrWVFQzOjB2OUOxOi=>
HCC-1428 NULj[G5LTnWwY4Tpc44hSXO|YYm= MYKxxsDPxE1? MXKyOEBpyqB? Mljr[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh MoPhNlIxPDl|MU[=
MDA-361 MUDGeY5kfGmxbjDBd5NigQ>? NXjaPGtWOcLizszN NYDifHNVOjRiaNMg M1fkcYRwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvckBqdmS3Y3XkJIJ6KDRvT1itWEDDqA>? M1e4SlIzODR7M{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 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
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).

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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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Molecular Weight Calculator

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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