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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Cited by 10 Publications

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.

     

    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.

  • Biochim Biophys Acta, 2018, 1863(6):625-638. 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 NVjmZXRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TNR|EvOy1zMECwJI5O M3XzOFQ5KGh? NFfnW|lqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MXyyOFk4QTJ7NB?=
MCF-7/LTED NUTW[Jh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLKNU4{NTFyMECgcm0> NIjyZ5I1QCCq M3H1OolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVi1VXBSOjR7N{myPVQ>
HCC1428 NVvaNW93T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLvNU4{NTFyMECgcm0> MX:0PEBp MmfQbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NIHjWnIzPDl5OUK5OC=>
HCC1428/LTED MmHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTXNZFNOS5|LUGwNFAhdk1? M4DNZlQ5KGh? M1zJdolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NH:w[YkzPDl5OUK5OC=>
LCC1 NIjLXVVHfW6ldHnvckBCe3OjeR?= NH7Kbo0yODBibl2= NVv5PXhvPDhvMUS0JIg> M4fDSYFkfGm4YYTld{BWWFJic3nncoFtcW6p MX:yOFg2QDJ5Nx?=
LCC9 NWjZVlNCTnWwY4Tpc44hSXO|YYm= NWD3fVRQOTByIH7N NGXHZZI1QC1zNESgbC=> NFThVHNi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= M3voXFI1QDV6Mke3
MCF-7  NFfmW5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEi1TFMyODBibl2= MWq1JIQ> NH\POmZqdmirYnn0d{Bk\WyuIHfyc5d1cCC2bzCxNQ+9jQ>? NXHCSG5EOjR6MUm1OVA>
mesangial  NWL1d25CTnWwY4Tpc44hSXO|YYm= NHrSUVUxNjFvMUCwJI5O MWK0PEBp NE\DUG9{fXCycnXzd4V{KFSJRj5OtlEucW6mdXPl[EB1gXCnIFnWJINwdGyjZ3Xu M333bFI1Pzl|NkO5
Mesangial NH7D[WFHfW6ldHnvckBCe3OjeR?= Mn72NE4yNTFyMDDuUS=> NX3VdI9lOC53IHi= MXvpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRiU33h[FIheGixc4Doc5J6dGG2aX;uJJZq[SCJUFXS M{XLN|I1Pzl|NkO5
ER+ MCF-7/2a NFnY[plIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7TTWM2OD1yLkCwOEDPxE1? NUTTepVzOTV|MkS4PFQ>
ER+ MCF-7 M3f0TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTscnZuOjByIHi= NFnSUmdKSzVyPUCuNlEhdk1? NHntcZoyPTN{NEi4OC=>
MCF-7  MmHySpVv[3Srb36gRZN{[Xl? NILJU2UyOMLibl5CpC=> M3XMXFczKGh? MXry[ZZmenOnczD0bIUh\XO2cn;n[Y4h\W[oZXP0LGlEPTBiMT65JOOYKDFy4pkSPUBOMQ>? NXv6NGF{OjR7MEi2OVI>
MCF-7  NXm4TZgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1L2OGlEPTEEoH;mJIFxeHKxeHntZZRmdHliMjDuUS=> NH;q[okzOzR2OEO0Oi=>
H1975  M2PEN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jRe|PDqM7:TR?= MkPPNUBu NXHHb4V6cW6lcnXhd4V{KHSqZTDn[YZqfGmwaXKgd4Vve2m2aY\peJkhd2ZiSEG5O|Uh[2WubIRCpC=> NYDSW5dROjR{Nki4NVA>
H1975 NEfKNJlHfW6ldHnvckBCe3OjeR?= M2fadlPDqM7:TR?= M3[5fFEhdQ>? NUHReXQzfXC{ZXf1cIF1\XNidHjlJIxmfmWuIH;mJGxmfC15Yx?= MVqyOFI3QDhzMB?=
MCF-7  MojvSpVv[3Srb36gRZN{[Xl? NGDYW2oyODEkgJnuUeKh NIntbZY4OiCq MWjy[ZZmenOnczD0bIUheHKxdHXjeIl3\SCnZn\lZ5Qhd2ZiRUNCpIlvKGOnbHygbY53[XOrb36= MUGyN|k{Pjd5Mx?=
MCF-7  NH\SUJBHfW6ldHnvckBCe3OjeR?= MojKNVAx6oDLbl5CpC=> NHPCfpgzPC92ODDo NILjbGhn[WOrbHn0ZZRmeyCrbo\hd4lwdiC2aILveYdpKE2PUIOnJI1w\HWuYYTpc44> MnL4NlM6OzZ5N{O=
BT474-tet-shMED1 MmPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUSwMlEuPSEQvF2= NV7RN4tnPyCm NWLrfY41cW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MV:yN|k{PjJ|NB?=
ZR75-1-tet-shMED1  M{jM[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPmT2pQOC5zLUWg{txO MYW3JIQ> NX[wSm1IcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NXHqN5V6OjN7M{[yN|Q>
MCF-7-tet-shMED1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[wMlEuPSEQvF2= M3XzNlch\A>? NEXZc3NqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MWSyN|k{PjJ|NB?=
HepG2  MWfGeY5kfGmxbjDBd5NigQ>? NIGzdI8xNjBzLUGwJO69VQ>? MXGxPEBpyqB? MlnDZYN1cX[jdHXzJJRp\SCHUlWtcYVlcWG2ZXSgeJJidnOlcnnweIlwdiCxZjDBSlJGWg>? NGLo[mIzOzd|M{G4PC=>
MCF-7L  M3LSeGZ2dmO2aX;uJGF{e2G7 NV\yTmVzOTByIH7NxsA> MW[xNEBucW5xMkSgbE81QCCq M1\VXJJme3WudIOgbY4hTUeIUjygTGVTOiCjbnSgTGVTOyCyaH;zdIhwenmuYYTpc44h[XRicILvcI9v\2WmIHX4dI9{fXKn NXvqWWZ3OjN4OE[0NVY>
MCF-7L  MVfGeY5kfGmxbjDBd5NigQ>? MnXTNVAxKG6PwrC= NY\rdJl2PDhiaB?= M1;zRolv\HWlZYOgeZBz\We3bHH0bY9vKG:oIH3SUmEhd2ZiRVfGVkBtcWejbnSgTGIuTUeI NI[x[FIzOzZ6NkSxOi=>
MCF-7L NFGyUXRHfW6ldHnvckBCe3OjeR?= MVmxNFAhdk4EoB?= MkO3OFghcA>? M2fVWolv\HWlZYOgSWdHWiCoYX3pcJkhdWWvYnXyJIFkfGm4YYTpc44hemWzdXny[YQhTVJ? NXHHS4g3OjN4OE[0NVY>
C4-12  MojHSpVv[3Srb36gRZN{[Xl? NVzRZll2OTByIH7NxsA> MXy0PEBp NWrne3htcW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= MkiwNlM3QDZ2MU[=
MCF-7L NYP5fYJsTnWwY4Tpc44hSXO|YYm= NIDZU4cyODBibl5CpC=> NHL6bmwzPCCq NGnPV2tqdmS3Y3XzJGVITlJicHjvd5Bpd3K7bHH0bY9vKHKncYXpdoVlKEiELVXHSkBnfW6ldHnvci=> M37q[FI{Pjh4NEG2
MMQ  NYPwUlJwTnWwY4Tpc44hSXO|YYm= NECyZnkxNTZ{NTDuUS=> NVrDdZdbPzJiaB?= NHrG[Fdld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDld5Rzd2enbjDy[YNmeHSxcj5OtUApTVMQsTm= NHjCW5YzOzV{M{O1Oy=>
H1975  NYjlPZlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvHSG4xNjNzMkWtNVAh|ryP M4rE[lYh\A>? NXzoXlRHcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NV7uS5RrOjN|OUm5OVc>
H1975  NYPwR3NJSXCxcITvd4l{KEG|c3H5 MU[yNFAhdk1? NXvnRmNNPzJiaB?= NWf2VIE2\W6qYX7j[ZMh\XKub4TpcoljKGmwZIXj[YQh[XCxcITvd4l{ NYXlNmxnOjN|OUm5OVc>
MCF-7  M3rwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnzXnJMOTBxMUCwM|ExODBibl2= NGLqbYkzNzRxNjDk NULmbYR{TE2VTx?= NEi3[3dqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy NXLKVWpkOjN|MUO1NFY>
MCF-7  M1HFS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4Xr[|ExOCCwTR?= M1:1NFQh\A>? M4GwemROW09? NIjjeINqdmS3Y3XzJIEhcGmpaHXyJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5idHjlJGcyKHCqYYPlxsA> MVuyN|MyOzVyNh?=
MLO-Y4  NF;GXGpHfW6ldHnvckBCe3OjeR?= MmjJNeKh|ryP NEHETpUyKGh? M2TYTYlvcGmkaYTzJGUzNWmwZIXj[YQhS3h2MzDlfJBz\XO|aX;u NX\4W2JGOjN{NEewOVc>
MCF-7 MnHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVGxNFAhdk1? M4DlfFQ5KGh? Mn75ZYJzd2ejdHXzJJRp\SCycn;sbYZmemG2aY\lJIVn\mWldDDv[kBud2SncnH0[UBvcXS{b4PheIl3\SC|dILld5M> NYTNRYFlOjN{MU[3OFQ>
TG1-1  MYDGeY5kfGmxbjDBd5NigQ>? NFriS4cyyqEQvF2= MWCyOEBp Ml71ZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x MmjFNlMxQDh4MEe=
TG1-1  MoPCSpVv[3Srb36gRZN{[Xl? MYmxxsDPxE1? NWK0V206OjRiaB?= NV\vNnBK[WK{b3fheIV{KEV{wrDpcoR2[2WmIHHjZ5VufWyjdHnvckBw\iCSSUPL NG\jOGkzOzB6OE[wOy=>
MCF7 M{PMe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfWTZEyODBibl2= M2L3cFQ5KGh? MlnjcIVi\HNidH:gZUB{cW2rbHHyJIxwe3NiaX6gd5Vzfmm4YXygZZMhf2m2aDDkc5hwenWkaXPpckBidG:wZR?= NEPMPXczOzB5N{K0PS=>
MCF7 MoPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjPd|IyODBibl2= MlzZOFghcA>? M12xcYVvcGGwY3XzJI52fGyrbj3t[YRq[XSnZDDj[YxtKGSnYYTo MluzNlMxPzd{NEm=
MCF-7  M2GxV2Z2dmO2aX;uJGF{e2G7 MWW2JIg> NILKdY5FVVOR NEXjOVlifHSnboXheIV{KHSqZTDmcJVlcW:6b37pcE0hd3JiZnXubIV5[W2rZD3pcoR2[2WmIHnuZ5Jm[XOnIHnuJI1qWi1{MTDlfJBz\XO|aX;u NUfQWHVZOjNyNUKwN|Y>
MCF-7 NIW5Z|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTWUI1NOTByIH7NM|Eh|ryP NXTHO2t3PSCm MUXpcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[gNVfPui2nc4TyZYRqd2x? MXeyNlk5Ojd4NR?=
MCF-7 M3zKSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTRU4R7OTByIH7N NUKzWIxpPSCm M3HIVYlvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kBnfXOjcnnlcIlvKEh? Mm\4NlI6QDJ5NkW=
1471.1 NXnIUmdETnWwY4Tpc44hSXO|YYm= MmLHNVAxKG6P MmfYNUBp MWHFeG9JyqB? MoLBeIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu M3W5OlIzQDZ7MUC2
MCF-7 NX7qS3g1TnWwY4Tpc44hSXO|YYm= MkDsNVAxKG6P NXKzXY4{OSCq NVTLZmp{TXSRSNMg MYX0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= MViyNlg3QTFyNh?=
HeLa NFjQc5dHfW6ldHnvckBCe3OjeR?= NGHlZZMyODBibl2= NHOyT4kyKGh? M37POGV1V0kEoB?= NWK0VWY1fGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv NX3DS3R7OjJ6NkmxNFY>
COS-7  MY\GeY5kfGmxbjDBd5NigQ>? MWixNFAhdk1? MmrhNUBp NVr5UWdCTXSRSNMg MYn0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= Mo[2NlI5PjlzME[=
BG1L-OHTLT  MlrHSpVv[3Srb36gRZN{[Xl? MUWxNOKhdk1? MUGyOOKhcMLi M{nlWIlvcGmkaYTzJGVT|rFiZYjwdoV{e2mxbh?= NHLCc5gzOjZ3MkW1PC=>
BG1L-ICILT Mn\6SpVv[3Srb36gRZN{[Xl? MkXhNVDDqG6P MWOyOOKhcMLi NH:5fWVqdmirYnn0d{BGWs7zIHX4dJJme3Orb36= NH:3dWIzOjZ3MkW1PC=>
PC-9 NH3PUFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmwMlAxOy1|MDFOwG0> NVzPRno{PDhiaB?= MlLibY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mni3NlI2PjB4M{S=
H1650 MmXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP6OXltOC5yMEOtN|Ah|ryP NGPoepA1QCCq M1;Yd4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MXuyNlU3ODZ|NB?=
H1975 M4rUdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVKzUldlOC5yMEOtN|Ah|ryP NVf6[mlXPDhiaB?= MXrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWqyNlU3ODZ|NB?=
H1975 MVTGeY5kfGmxbjDBd5NigQ>? M3[5flPDqM7:TR?= M33yeFMhcA>? MmXUZYJzd2ejdHXzJJRp\SCyaH;zdIhwNUWJRmKgbY5lfWO2aX;uJIJ6KGW|dILv[4Vv MVWyNlU3ODZ|NB?=
H1975 NH3x[5RHfW6ldHnvckBCe3OjeR?= NXXjZm04O8LizszN Mke3O{Bl MnfDbY5lfWOnczDFS2ZTKGW6cILld5Nqd25? MYKyNlU3ODZ|NB?=
HTR-8 M33oWWZ2dmO2aX;uJGF{e2G7 MmrONeKh|ryP MkH5NU01QCCq MYPkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCLR1\CVFchdVKQQR?= NWXhZpJNOjJ|OEOxNVE>
JEG-3 M1nGZWZ2dmO2aX;uJGF{e2G7 NGOxS5UyyqEQvF2= MmLvNU01QCCq NVu5Tlhs\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gTWdHSlB5IH3SUmE> M{fNOVIzOzh|MUGx
Huh7 NFjsTpFHfW6ldHnvckBCe3OjeR?= MoP6OVDDqM7:TR?= NGKze4Y1QCCq MmL5bY5pcWKrdIOg[4VvcXO2ZXnuMY1m\GmjdHXkJHBQVjFidILhcpNi[3SrdnH0bY9v M2HTVFIzOzB2Mkm2
201T NGHFNIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnpb3Q2KM7:TR?= M3qyPVczKGh? MlzEbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? M1HoelIzOjV6NEe2
A549  MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PtPFUh|ryP MmnWO|IhcA>? MmTkbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? NE\KOowzOjJ3OES3Oi=>
MCF-7 M{i0emZ2dmO2aX;uJGF{e2G7 NIrXNXEyyqEQvF2= MXSyOEBpyqB? NULHbHd{\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi MUmyNlA1QTNzNh?=
HCC-1428 MofHSpVv[3Srb36gRZN{[Xl? NVnoS5JvOcLizszN NViwcXl6OjRiaNMg MkHa[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh MX:yNlA1QTNzNh?=
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MCF7 NITzflFHfW6ldHnvckBCe3OjeR?= MV[xxsDPxE1? M4\PO|Q5KGh? NHKyXFdld3ewcnXneYxifGW|IH;2[ZJidGxiRWNOtUBxem:2ZXnuJIxmfmWucx?= NGnz[YMzOTV|M{G5OS=>
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MCF7 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3jSYkxNjBzLUGg{txO MVi3JIQ> M3HBPJJm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MkHaNlE{QTZyOUS=
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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

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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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*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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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
NCT03531645 Not yet recruiting Malignant Neoplasms of Female Genital Organs M.D. Anderson Cancer Center|AstraZeneca|Pfizer April 1 2019 Phase 2
NCT03531645 Not yet recruiting Malignant Neoplasms of Female Genital Organs M.D. Anderson Cancer Center|AstraZeneca|Pfizer April 1 2019 Phase 2
NCT03854903 Not yet recruiting Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer Georgetown University|Pfizer March 2019 Phase 1
NCT03854903 Not yet recruiting Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer Georgetown University|Pfizer March 2019 Phase 1
NCT03691493 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 February 8 2019 Phase 2
NCT03803761 Not yet recruiting Anatomic Stage IV Breast Cancer AJCC v8|Breast Carcinoma Metastatic in the Brain|Estrogen Receptor Positive|HER2/Neu Negative|Metastatic Breast Carcinoma|Postmenopausal|Prognostic Stage IV Breast Cancer AJCC v8 National Cancer Institute (NCI) February 12 2019 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.

  • * Indicates a Required Field

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