Fulvestrant

目录号:S1191 别名: ICI-182780, ZD 9238

Fulvestrant Chemical Structure

Molecular Weight(MW): 606.77

Fulvestrant是一种Estrogen receptor(ER)拮抗剂, 无细胞试验中IC50为0.094 nM。

规格 价格 库存 购买数量  
RMB 533.25 现货
RMB 567.34 现货
RMB 2233.34 现货
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客户使用该产品的5个实验数据:

  • 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.

产品安全说明书

Estrogen/progestogen Receptor抑制剂选择性比较

生物活性

产品描述 Fulvestrant是一种Estrogen receptor(ER)拮抗剂, 无细胞试验中IC50为0.094 nM。
靶点
ER [1]
(Cell-free assay)
0.94 nM
体外研究

Fulvestrant 有效抑制ER阳性的MCF-7生长(IC50为 0.29 nM),而对ER阴性的的 BT-20人类乳腺癌细胞的生长没有作用效果。Fulvestrant 使细胞在 G0/G1 期累积,也降低了能持续进行DNA合成的细胞比例。[1] Fulvestrant 竞争性地抑制雌二醇与雌激素受体结合。 Fulvestrant通过损害受体二聚化和能量依赖型核质转运,而阻断ER的核定位。由于Fulvestrant-ER复合体的不稳定性,Fulvestrant与ER的结合最终会导致 ER蛋白的加速退化。[2] Fulvestrant (10 nM) 不仅可降低IGF-IR mRNA水平,也降低半衰期。[3] 100 μM Fulvestrant 处理MCF-7细胞,提高TNFR1 和TRADD 稳态的mRNA水平,这种作用具有时间依赖性。[4] Fulvestrant 作用于LNCaP人类前列腺癌细胞,可以下调雄激素受体的表达,也减少雄激素的反应。Fulvestrant也显著降低R1881 刺激的生长,降低 70%。[5]Fulvestrant作用于未成熟的小脑神经元,通过快速激活MAPK,可以调节有丝分裂和细胞死亡。[6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 M33mWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Sxd|EvOy1zMECwJI5O NXPtRXg6PDhiaB?= MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXrHNIJjOjR7N{myPVQ>
MCF-7/LTED NHTtWJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfjNU4{NTFyMECgcm0> MWC0PEBp NH74dXJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnzoNlQ6Pzl{OUS=
HCC1428 MnTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfaV25VOS5|LUGwNFAhdk1? M33Ec|Q5KGh? M1fyeIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIfLe24zPDl5OUK5OC=>
HCC1428/LTED NWjMZXQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVmxMlMuOTByMDDuUS=> MXy0PEBp NUexVZRPcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MXmyOFk4QTJ7NB?=
LCC1 NH;jfpZHfW6ldHnvckBCe3OjeR?= NEPye28yODBibl2= NF[0OHk1QC1zNESgbC=> NWHN[ZI3[WO2aY\heIV{KFWSUjDzbYdv[Wyrbne= NFrOcWozPDh3OEK3Oy=>
LCC9 MYrGeY5kfGmxbjDBd5NigQ>? NU[3T|BlOTByIH7N MWi0PE0yPDRiaB?= MXnhZ5RqfmG2ZYOgWXBTKHOrZ37hcIlv\w>? NVjKOYFkOjR6NUiyO|c>
MCF-7  Mmr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVGxNFAhdk1? NVPISldpPSCm M1fXeYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSxIEGw89yG M4rDUFI1QDF7NUWw
mesangial  NFnNZYRHfW6ldHnvckBCe3OjeR?= M1z2UlAvOS1zMECgcm0> MlvzOFghcA>? NXftNlNqe3WycILld5NmeyCWR1[t{tIyNWmwZIXj[YQhfHmyZTDJWkBkd2yuYXflci=> NEG4b5YzPDd7M{[zPS=>
Mesangial MUfGeY5kfGmxbjDBd5NigQ>? NHSxVGYxNjFvMUCwJI5O MkS1NE42KGh? M1fuOolvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDTcYFlOiCyaH;zdIhwenmuYYTpc44hfmmjIFfQSXI> Mn3uNlQ4QTN4M{m=
ER+ MCF-7/2a NHnPTW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnqTZp3UUN3ME2wMlAxPCEQvF2= MoDvNVU{OjR6OES=
ER+ MCF-7 NHvIWIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LTRlIxOCCq MYPJR|UxRTBwMkGgcm0> NITEXnMyPTN{NEi4OC=>
MCF-7  NHjQXHJHfW6ldHnvckBCe3OjeR?= NFvocIIyOMLibl5CpC=> MYe3NkBp MU\y[ZZmenOnczD0bIUh\XO2cn;n[Y4h\W[oZXP0LGlEPTBiMT65JOOYKDFy4pkSPUBOMQ>? M2POZVI1QTB6NkWy
MCF-7  NF6yR29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmThTWM2OMLib3[gZZBxem:6aX3heIVtgSB{IH7N NGX5OYkzOzR2OEO0Oi=>
H1975  M4mzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVmzxsDPxE1? NYi2blROOSCv NGXD[nlqdmO{ZXHz[ZMhfGinIHfl[ol1cW6rYjDz[Y5{cXSrdnn0fUBw\iCKMUm3OUBk\Wyuc9Mg MnH6NlQzPjh6MUC=
H1975 NYPTXppSTnWwY4Tpc44hSXO|YYm= NXXJR2Z1O8LizszN M4DZfVEhdQ>? Mn7oeZBz\We3bHH0[ZMhfGinIHzleoVtKG:oIFzleE04[w>? MVWyOFI3QDhzMB?=
MCF-7  M4W2ZWZ2dmO2aX;uJGF{e2G7 MlTqNVAx6oDLbl5CpC=> NH3rVnc4OiCq NHe4PI1z\X[ncoPld{B1cGVicILveIVkfGm4ZTDl[oZm[3Rib3[gSVLDqGmwIHPlcIwhcW64YYPpc44> NGLnXoMzOzl|Nke3Ny=>
MCF-7  NV;xO49uTnWwY4Tpc44hSXO|YYm= Mn3pNVAx6oDLbl5CpC=> M3TUfVI1NzR6IHi= MlvB[oFkcWyrdHH0[ZMhcW64YYPpc44hfGi{b4XnbEBOVVC|JzDtc4R2dGG2aX;u M4HmdFI{QTN4N{ez
BT474-tet-shMED1 NHn6[HFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[wMlEuPSEQvF2= M{Xiflch\A>? NYe3NWV7cW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MWOyN|k{PjJ|NB?=
ZR75-1-tet-shMED1  MofWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{m3flAvOS13IN88US=> MUW3JIQ> NXizVYx3cW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NHLTcoYzOzl|NkKzOC=>
MCF-7-tet-shMED1 MlnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTPNE4yNTVizszN NUfhZWdLPyCm NUe2ZXR1cW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M2C3U|I{QTN4MkO0
HepG2  NVjLbFhXTnWwY4Tpc44hSXO|YYm= MmPwNE4xOS1zMDFOwG0> NGLpRmEyQCCqwrC= MXHhZ5RqfmG2ZYOgeIhmKEWURT3t[YRq[XSnZDD0doFve2O{aYD0bY9vKG:oIFHGNmVT M1\VcFI{PzN|MUi4
MCF-7L  M2nSOWZ2dmO2aX;uJGF{e2G7 NFfTWnQyODBibl5CpC=> NInTVogyOCCvaX6vNlQhcC92ODDo MoCzdoV{fWy2czDpckBGT0[ULDDISXIzKGGwZDDISXI{KHCqb4PwbI9zgWyjdHnvckBifCCycn;sc45o\WRiZYjwc5N2emV? MoTvNlM3QDZ2MU[=
MCF-7L  M4TnZWZ2dmO2aX;uJGF{e2G7 Ml64NVAxKG6PwrC= NXf3Sm1JPDhiaB?= MX3pcoR2[2W|IIXwdoVofWyjdHnvckBw\iCvUl7BJI9nKEWJRmKgcIlo[W6mIFjCMWVITg>? NI\lPWMzOzZ6NkSxOi=>
MCF-7L NFriV5RHfW6ldHnvckBCe3OjeR?= NWnMbnNoOTByIH7NxsA> MoPZOFghcA>? MVjpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT Ml;5NlM3QDZ2MU[=
C4-12  M3O2PGZ2dmO2aX;uJGF{e2G7 NEL5d|AyODBibl5CpC=> NIKwOJE1QCCq NWPWbnlwcW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= M{\oW|I{Pjh4NEG2
MCF-7L NV7ZfXJrTnWwY4Tpc44hSXO|YYm= M1jjfVExOCCwTdMg NXv0NIF[OjRiaB?= M{XW[Ylv\HWlZYOgSWdHWiCyaH;zdIhwenmuYYTpc44hemWzdXny[YQhUEJvRVfGJIZ2dmO2aX;u NXq5TYxFOjN4OE[0NVY>
MMQ  MWTGeY5kfGmxbjDBd5NigQ>? MVKwMVYzPSCwTR?= M3TQNFczKGh? NUP6XZFK\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[g[ZN1em:pZX6gdoVk\XC2b4Kt{tEhMEWUzsGp MoT0NlM2OjN|NUe=
H1975  M2\sWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj0fJQxNjNzMkWtNVAh|ryP NXLpd2dJPiCm MYfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3fNbVI{Ozl7OUW3
H1975  NHnNSFFCeG:ydH;zbZMhSXO|YYm= NIXwTYIzODBibl2= MmTlO|IhcA>? MmXm[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz MVKyN|M6QTl3Nx?=
MCF-7  M1vaW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHpOYoyOC9zMECvNVAxOCCwTR?= MV[yM|QwPiCm MXTEUXNQ MoDRbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= MYmyN|MyOzVyNh?=
MCF-7  NHXURYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[xNFAhdk1? NIPpUmE1KGR? MojsSG1UVw>? MnvUbY5lfWOnczDhJIhq\2incjDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKHSqZTDHNUBxcGG|ZdMg M{jaVlI{OzF|NUC2
MLO-Y4  MVjGeY5kfGmxbjDBd5NigQ>? NUL4V4ZbOcLizszN NV:3WJR1OSCq MYDpcohq[mm2czDFNk1qdmS3Y3XkJGN5PDNiZYjwdoV{e2mxbh?= M4XkNVI{OjR5MEW3
MCF-7 M3[5[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHNXXoyODBibl2= Mn60OFghcA>? MYLhZpJw\2G2ZYOgeIhmKHC{b3zp[oVz[XSrdnWg[YZn\WO2IH;mJI1w\GW{YYTlJI5qfHKxc3H0bZZmKHO2cnXzdy=> NIj1fWEzOzJzNke0OC=>
TG1-1  MoLySpVv[3Srb36gRZN{[Xl? M2PsWlHDqM7:TR?= NYTzcFRkOjRiaB?= M4XiN4Fjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhUEmILUJOtS=> MX6yN|A5QDZyNx?=
TG1-1  M2TrcmZ2dmO2aX;uJGF{e2G7 Mo\LNeKh|ryP M2TLU|I1KGh? MWrhZpJw\2G2ZYOgSVLDqGmwZIXj[YQh[WOldX31cIF1cW:wIH;mJHBKO0t? NVP6ZndxOjNyOEi2NFc>
MCF7 NFjieG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPSbHQyODBibl2= NYG3TlQ4PDhiaB?= NIjXN5dt\WGmczD0c{BiKHOrbXnsZZIhdG:|czDpckB{fXK4aY\hcEBieyC5aYToJIRwgG:{dXLpZ4lvKGGub37l Mm\NNlMxPzd{NEm=
MCF7 NWfNOHlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUCxNFAhdk1? NGXjd|k1QCCq NVjyflBu\W6qYX7j[ZMhdnW2bHnuMY1m\GmjdHXkJINmdGxiZHXheIg> NYnTe|I2OjNyN{eyOFk>
MCF-7  NV:1bIpNTnWwY4Tpc44hSXO|YYm= MWW2JIg> NFLySlhFVVOR M{jNd4F1fGWwdXH0[ZMhfGinIH\seYRqd3ixbnnsMUBweiCoZX7o[ZhidWmmLXnu[JVk\WRiaX7jdoVie2ViaX6gcYlTNTJzIHX4dJJme3Orb36= MVWyN|A2OjB|Nh?=
MCF-7 M4TmSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rreFExOCCwTT:xJO69VQ>? MX21JIQ> MWXpcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[gNVfPui2nc4TyZYRqd2x? M1XoTlIzQTh{N{[1
MCF-7 NFL0VoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnySFJNOTByIH7N MkjjOUBl MX7pcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[g[pV{[XKrZXzpckBJ NHrWTpczOjl6Mke2OS=>
1471.1 NFr6V4tHfW6ldHnvckBCe3OjeR?= M3KwdVExOCCwTR?= NV3HfJpmOSCq MW\FeG9JyqB? MXv0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= MmG1NlI5PjlzME[=
MCF-7 M1PYSWZ2dmO2aX;uJGF{e2G7 NFHxcnUyODBibl2= NHrxR2EyKGh? MWLFeG9JyqB? M2TzUpRic2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> MWmyNlg3QTFyNh?=
HeLa MVzGeY5kfGmxbjDBd5NigQ>? MmLrNVAxKG6P MVKxJIg> NX7jNXZbTXSRSNMg NInUUHh1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> NUfaTGZZOjJ6NkmxNFY>
COS-7  M{n1S2Z2dmO2aX;uJGF{e2G7 MnH4NVAxKG6P NXvTblJwOSCq MnGzSZRQUMLi NGq4NW91[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> NVHRV21{OjJ6NkmxNFY>
BG1L-OHTLT  MlrvSpVv[3Srb36gRZN{[Xl? NVPtPYk3OTEEoH7N M17Cb|I1yqCqwrC= MVfpcohq[mm2czDFVu6yKGW6cILld5Nqd25? NWT6d2dSOjJ4NUK1OVg>
BG1L-ICILT M1XyUGZ2dmO2aX;uJGF{e2G7 MUCxNOKhdk1? MYeyOOKhcMLi NIXqbVRqdmirYnn0d{BGWs7zIHX4dJJme3Orb36= NFPLWJAzOjZ3MkW1PC=>
PC-9 M4POeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTYWGdzOC5yMEOtN|Ah|ryP NXj1bIhyPDhiaB?= M4nlN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVmyNlU3ODZ|NB?=
H1650 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\lWIpIOC5yMEOtN|Ah|ryP NF;tR2U1QCCq MXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUiyNlU3ODZ|NB?=
H1975 NWi2VIpQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUiwMlAxOy1|MDFOwG0> NF;EV2Q1QCCq NIDNV4dqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NHPobmozOjV4ME[zOC=>
H1975 MWPGeY5kfGmxbjDBd5NigQ>? MmjXN:Kh|ryP M3zpWFMhcA>? MmLQZYJzd2ejdHXzJJRp\SCyaH;zdIhwNUWJRmKgbY5lfWO2aX;uJIJ6KGW|dILv[4Vv MlPFNlI2PjB4M{S=
H1975 M2e1WGZ2dmO2aX;uJGF{e2G7 NILyZpk{yqEQvF2= MorXO{Bl MWjpcoR2[2W|IFXHSnIh\XiycnXzd4lwdg>? MlW4NlI2PjB4M{S=
HTR-8 NVzleINMTnWwY4Tpc44hSXO|YYm= NUH1PVZ4OcLizszN NYHMW3ZNOS12ODDo NFPs[|Rld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDJS2ZDWDdibWLORS=> MYCyNlM5OzFzMR?=
JEG-3 M{DpOWZ2dmO2aX;uJGF{e2G7 NG\3WosyyqEQvF2= NXy5fFUxOS12ODDo MlHy[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSVfGRnA4KG2UTlG= Mnj4NlI{QDNzMUG=
Huh7 Mnu0SpVv[3Srb36gRZN{[Xl? NWXKVHdOPTEEoN88US=> M1S4ZlQ5KGh? MVTpcohq[mm2czDn[Y5qe3SnaX6tcYVlcWG2ZXSgVG9POSC2cnHud4FkfGm4YYTpc44> MmXGNlI{ODR{OU[=
201T NHXxU2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLqNGdyPSEQvF2= NEPtN|U4OiCq NUXxVplocW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\hcoRmfGGwaXK= MXqyNlI2QDR5Nh?=
A549  M3T1U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHjWYxmPSEQvF2= M{faSFczKGh? MW\pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIghfmGwZHX0ZY5q[g>? M4qzXlIzOjV6NEe2
MCF-7 NHPoZpJHfW6ldHnvckBCe3OjeR?= M1vQWFHDqM7:TR?= NWHQXIc3OjRiaNMg MX3kc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb36gbY5lfWOnZDDifUA1NU:KLWSgxsA> NX[yV2tVOjJyNEmzNVY>
HCC-1428 M1H5U2Z2dmO2aX;uJGF{e2G7 NInse3cyyqEQvF2= M1Hab|I1KGkEoB?= M1jjToRwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvckBqdmS3Y3XkJIJ6KDRvT1itWEDDqA>? MUeyNlA1QTNzNh?=
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ZR75-1 MkezSpVv[3Srb36gRZN{[Xl? NYn6[I9lOcLizszN M3nY[|I1KGkEoB?= M3LDVIRwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvckBqdmS3Y3XkJIJ6KDRvT1itWEDDqA>? NHq4dYQzOjB2OUOxOi=>
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MDA-361 Mmr2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGxxsDPxE1? Ml3zOU0yOCCm NFvIWI9{fXCycnXzd4V{KEV{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? MknKNlIxPDl|MU[=
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MCF7S M3\yW2Z2dmO2aX;uJGF{e2G7 NFTWOpQyyqEQvF2= NFnXVJQ1QCCq M1[2U4Rwf26{ZXf1cIF1\XNib4\ldoFtdCCHUt8xJJBzd3SnaX6gcIV3\Wy| M3TOZVIyPTN|MUm1
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MCF7S NYXJVYtjTnWwY4Tpc44hSXO|YYm= MoP4NeKh|ryP M4\3RVch\A>? NYriO3p7[XS2ZX71ZZRmeyC2dX3vdpNxcGW{ZTDmc5Ju[XSrb36gZY5lKHC{b3zp[oVz[XSrb36= NHHmb2EzOTV|M{G5OS=>
MCF7S MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHEU4I1OC53L{Gg{txO NYn1eGtzPyCm MlP2SG1UVw>? NF;UVoRl\WO{ZXHz[ZMh[2WubDDlfJBidnOrb36= M1Pl[|IyPTN|MUm1
T47D  MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWS0JI5O MWO0NEBp NG\LUZl{fXCycnXzd4V{KGOnbHyg[5Jwf3SqIH3v[IVz[XSnbIm= M2XxWFIyPDhyM{mx
BT474  M3;OcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV60JI5O NUjqZWxuPDBiaB?= NYrRe5BTe3WycILld5NmeyClZXzsJIdzd3e2aDDtc4RmemG2ZXz5 MnvlNlE1QDB|OUG=
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MCF7 MomzSpVv[3Srb36gRZN{[Xl? NGqwNogyODBibl2= MofFO{Bl MXPy[YR2[2W|IFXS{tEh\XiycnXzd4lwdiC|aXfubYZq[2GwdHz5 MkLYNlE{QTZyOUS=
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MCF7 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrXNE4xOS1zIN88US=> MX[3JIQ> NFnIdoNz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MlXINlE{QTZyOUS=
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MCF7 M{i0NGZ2dmO2aX;uJGF{e2G7 NELzcVEyODBibl2= MmTVO{Bl NHLJWZhqdmS3Y3XzJI9nKEW{YlKzJIFv\CCHcnLCOEBz\WOncITvdkBmgHC{ZYPzbY9vKGGwZDDzbYdv[WyuaX7n MYWyNVM6PjB7NB?=
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MCF7 NG\oWYlHfW6ldHnvckBCe3OjeR?= NYG4flY3OTBibl2= MkD5PVYhcA>? Ml\W[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uxsA> MXeyNVM4QDN|Mx?=
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MCF-7 M1PNU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi2dW0yODBibl2= NHr2Z2g4Oi97NjDo M{PoXoNifXOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NGPPbFIzOTJ7OUi2Ni=>
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MMQ M{XrfWZ2dmO2aX;uJGF{e2G7 Mnr0NE4xODhvNkK1JI5O M2XRblczKGh? NVzzNo8xcW6qaXLpeJMhWFKOIIPlZ5JmfGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NV7yTYRROjB5MEC3OVU>
MMQ NVzGSXczTnWwY4Tpc44hSXO|YYm= NUSzc3dtOC5yND22NlUhdk1? MUW3NkBp M1j1UYlvcGmkaYTzJGVT|rFiZYjwdoV{e2mxbh?= M2juNVIxPzByN{W1
MMQ MX\GeY5kfGmxbjDBd5NigQ>? M{X1V|AvODRvNkK1JI5O M37nblczKGh? MXT1dJJm\3WuYYTld{BVT0cQskOgZY5lKFSJRt8yVmlKKGW6cILld5Nqd25? NHHKZZYzODdyMEe1OS=>

... Click to View More Cell Line Experimental Data

体内研究 Fulvestrant缺乏子宫活性,与雌二醇联用皮下注射给药未成熟的雌性大鼠,有效抑制雌二醇的子宫内活性,ED50 为0.06 mg/kg/day。5 mg Fulvestrant悬浮液皮下注射到MCF-7移植瘤中,完全抑制肿瘤生长。10 μM Fulvestrant也有效抑制BrlO人类乳腺癌移植瘤的生长。[1] Fulvestrant (10 mg/rat) 皮下注射到大鼠前列腺腹侧,降低雄激素受体的表达,ERK1/2磷酸化,和细胞增殖。[7]Fulvestrant作用于鸡胚绒毛尿囊膜还具有抗血管生成的作用效果。[8]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
+ 展开
  • Cell lines: MCF-7 乳腺癌细胞
  • Concentrations: 2.9 nM
  • Incubation Time: 5 天
  • Method: MCF-7细胞培养在多孔板中(24孔,按4 × 104密度为接种),孔中含基本必需培养基,培养基中包含酚红,胰岛素(10 μg/mL),和5%活性炭处理的胎牛血清,不含额外的雌二醇。接种2天后,在新鲜的培养基中加入Fulvestrant 和/或雌二醇。培养持续5天,且进一步改变培养基,通过在实验处理开始和结束测量全部细胞蛋白,且与只用乙醇(0.1%)处理的对照组进行比较后,测评生长状况。
    (Only for Reference)
动物实验:[6]
+ 展开
  • Animal Models: 携带人类乳腺癌移植瘤MCF-7的裸鼠
  • Formulation: 50 mg/mL 花生油
  • Dosages: 5 mg
  • Administration: 皮下注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (164.8 mM)
Ethanol 100 mg/mL warmed (164.8 mM)
Water Insoluble
体内 从左到右依次加入纯溶剂:
5% DMSO+95% Corn oil
30mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 606.77
化学式

C32H47F5O3S

CAS号 129453-61-8
稳定性 powder
别名 ICI-182780, ZD 9238

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    Is there any information for the half-life of fulvestrant (Cat No.S1191)?

  • 回答:

    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