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, 2017, 36(16):2255-2264. 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 MkPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVOxMlMuOTByMDDuUS=> NI[3bmQ1QCCq MWPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXOwNmFOOjR7N{myPVQ>
MCF-7/LTED M{jpeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfDS|FuOS5|LUGwNFAhdk1? NFLKXlI1QCCq M2LYV4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NInLUJkzPDl5OUK5OC=>
HCC1428 MkGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rDcVEvOy1zMECwJI5O M{PoU|Q5KGh? MU\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MX2yOFk4QTJ7NB?=
HCC1428/LTED NW[zSo1CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HoZVEvOy1zMECwJI5O M4TUe|Q5KGh? NFXiUI1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXjQfmlPOjR7N{myPVQ>
LCC1 NFS1XYpHfW6ldHnvckBCe3OjeR?= NVPJRY1rOTByIH7N MkniOFguOTR2IHi= MUThZ5RqfmG2ZYOgWXBTKHOrZ37hcIlv\w>? NFy0foQzPDh3OEK3Oy=>
LCC9 M1;0UWZ2dmO2aX;uJGF{e2G7 M1rhSFExOCCwTR?= Ml\HOFguOTR2IHi= M13Ie4FkfGm4YYTld{BWWFJic3nncoFtcW6p NWHqZXZSOjR6NUiyO|c>
MCF-7  M4rzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37wbFExOCCwTR?= MVK1JIQ> NED6Z|JqdmirYnn0d{Bk\WyuIHfyc5d1cCC2bzCxNQ+9jQ>? MmWzNlQ5OTl3NUC=
mesangial  NF\IZ4hHfW6ldHnvckBCe3OjeR?= NETibWUxNjFvMUCwJI5O NYXKfWRZPDhiaB?= MoHqd5VxeHKnc4Pld{BVT0ZvzsKxMYlv\HWlZXSgeJlx\SCLVjDjc4xt[Wenbh?= MoXsNlQ4QTN4M{m=
Mesangial NYm5TGdmTnWwY4Tpc44hSXO|YYm= M3\yW|AvOS1zMECgcm0> NIn5UmUxNjViaB?= Mkf4bY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIGPtZYQzKHCqb4PwbI9zgWyjdHnvckB3cWFiR2DFVi=> M3L6ZlI1Pzl|NkO5
ER+ MCF-7/2a M33xN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLNTWM2OD1yLkCwOEDPxE1? MYmxOVMzPDh6NB?=
ER+ MCF-7 NVv5[3BwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTKTodOOjByIHi= MmW0TWM2OD1yLkKxJI5O NX30ZZFYOTV|MkS4PFQ>
MCF-7  MUXGeY5kfGmxbjDBd5NigQ>? Ml7tNVDDqG6PwrC= MWS3NkBp NE[weJBz\X[ncoPld{B1cGViZYP0do9o\W5iZX\m[YN1MEmFNUCgNU46KMPZIEGw5qiTQSCPKR?= NXfCc3hKOjR7MEi2OVI>
MCF-7  NEHXfIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxyqCxZjDhdJBzd3irbXH0[Yx6KDJibl2= NHrjNIozOzR2OEO0Oi=>
H1975  NYnIbop3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7YTpc{yqEQvF2= NFHKPJYyKG1? NUDsUHdTcW6lcnXhd4V{KHSqZTDn[YZqfGmwaXKgd4Vve2m2aY\peJkhd2ZiSEG5O|Uh[2WubIRCpC=> NGPVPWIzPDJ4OEixNC=>
H1975 MUHGeY5kfGmxbjDBd5NigQ>? NEDafpU{yqEQvF2= MmHsNUBu MW\1dJJm\3WuYYTld{B1cGVibHX2[Ywhd2ZiTHX0MVdk NWnGcIdjOjR{Nki4NVA>
MCF-7  MUfGeY5kfGmxbjDBd5NigQ>? NGnqSWoyODEkgJnuUeKh MV:3NkBp MYPy[ZZmenOnczD0bIUheHKxdHXjeIl3\SCnZn\lZ5Qhd2ZiRUNCpIlvKGOnbHygbY53[XOrb36= MlX5NlM6OzZ5N{O=
MCF-7  Ml3YSpVv[3Srb36gRZN{[Xl? M37uPFExOOLCiX7NxsA> M3XKV|I1NzR6IHi= NIfNSo1n[WOrbHn0ZZRmeyCrbo\hd4lwdiC2aILveYdpKE2PUIOnJI1w\HWuYYTpc44> M1fLc|I{QTN4N{ez
BT474-tet-shMED1 MmriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXewMlEuPSEQvF2= MYG3JIQ> MWXpcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NH\wUoQzOzl|NkKzOC=>
ZR75-1-tet-shMED1  MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV[wMlEuPSEQvF2= NF;uNZg4KGR? NWjFU2JTcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NYHnPYxnOjN7M{[yN|Q>
MCF-7-tet-shMED1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjQeYtxOC5zLUWg{txO NF6xUpI4KGR? NFvTcYlqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NFu0SZYzOzl|NkKzOC=>
HepG2  MVfGeY5kfGmxbjDBd5NigQ>? M2H6clAvODFvMUCg{txO M2TzNlE5KGkEoB?= NF;yOXli[3SrdnH0[ZMhfGinIFXSSU1u\WSrYYTl[EB1emGwc3PybZB1cW:wIH;mJGFHOkWU M2fUflI{PzN|MUi4
MCF-7L  MV3GeY5kfGmxbjDBd5NigQ>? MXuxNFAhdk4EoB?= M3HVNVExKG2rbj:yOEBpNzR6IHi= NWrsW2k5emW|dXz0d{BqdiCHR1\SMEBJTVJ{IHHu[EBJTVJ|IIDoc5NxcG:{eXzheIlwdiCjdDDwdo9td26pZXSg[Zhxd3O3cnW= MnjvNlM3QDZ2MU[=
MCF-7L  MVrGeY5kfGmxbjDBd5NigQ>? NHPXXoIyODBibl5CpC=> NIPidVI1QCCq MnXXbY5lfWOnczD1dJJm\3WuYYTpc44hd2ZibWLORUBw\iCHR1\SJIxq\2GwZDDIRk1GT0Z? NV7i[IlxOjN4OE[0NVY>
MCF-7L M1XjfGZ2dmO2aX;uJGF{e2G7 MnjZNVAxKG6PwrC= MXy0PEBp NVTBOI9QcW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= NYPON49GOjN4OE[0NVY>
C4-12  NEDhNoRHfW6ldHnvckBCe3OjeR?= M3GxXFExOCCwTdMg MXS0PEBp MULpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT NUTPSIdtOjN4OE[0NVY>
MCF-7L NHfQN2pHfW6ldHnvckBCe3OjeR?= M{nLcVExOCCwTdMg MW[yOEBp Mn7DbY5lfWOnczDFS2ZTKHCqb4PwbI9zgWyjdHnvckBz\XG3aYLl[EBJSi2HR1[g[pVv[3Srb36= MmrKNlM3QDZ2MU[=
MMQ  NWnEeJN[TnWwY4Tpc44hSXO|YYm= NYLMN3VuOC14MkWgcm0> NGK4eos4OiCq MVLkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCnc4Tyc4dmdiC{ZXPldJRwei4QsTCoSXLPuSl? NVHWWWZ4OjN3MkOzOVc>
H1975  NYnmTYxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjlNE4{OTJ3LUGwJO69VQ>? NUX2UY1EPiCm NHXTOG1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MYeyN|M6QTl3Nx?=
H1975  NHWwUmxCeG:ydH;zbZMhSXO|YYm= MYiyNFAhdk1? MVi3NkBp Mmi0[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz MW[yN|M6QTl3Nx?=
MCF-7  MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfvNVAwOTByL{GwNFAhdk1? MnTRNk81NzZiZB?= MYjEUXNQ NFn4eVNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy NX[z[JVvOjN|MUO1NFY>
MCF-7  NVHkS4FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOxNFAhdk1? M1zXUVQh\A>? MkDOSG1UVw>? M4rBVYlv\HWlZYOgZUBpcWeqZYKgdJJweG:{dHnvckBw\iClZXzsd{BqdiC2aHWgS|EheGijc3ZCpC=> MmXQNlM{OTN3ME[=
MLO-Y4  M4HqUWZ2dmO2aX;uJGF{e2G7 NEDUPWUyyqEQvF2= M{mxVFEhcA>? MUHpcohq[mm2czDFNk1qdmS3Y3XkJGN5PDNiZYjwdoV{e2mxbh?= NH\C[FEzOzJ2N{C1Oy=>
MCF-7 Ml\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTNNVAxKG6P NVfoZVluPDhiaB?= NY\NeGZm[WK{b3fheIV{KHSqZTDwdo9tcW[ncnH0bZZmKGWoZnXjeEBw\iCvb3TldoF1\SCwaYTyc5NifGm4ZTDzeJJme3N? MmDaNlMzOTZ5NES=
TG1-1  M4TiN2Z2dmO2aX;uJGF{e2G7 MXixxsDPxE1? MoP5NlQhcA>? MkLMZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x M4f5RlI{ODh6NkC3
TG1-1  MULGeY5kfGmxbjDBd5NigQ>? MlTMNeKh|ryP MYeyOEBp NHPYNIVi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKFCLM1u= M3P1UlI{ODh6NkC3
MCF7 NIHIcVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWOxNFAhdk1? NILH[GM1QCCq M2XLNIxm[WS|IITvJIEhe2mvaXzhdkBtd3O|IHnuJJN2en[rdnHsJIF{KHerdHig[I95d3K3YnnjbY4h[WyxbnW= NVLncpFCOjNyN{eyOFk>
MCF7 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmq0NVAxKG6P MWq0PEBp Mnnv[Y5p[W6lZYOgcpV1dGmwLX3l[IlifGWmIHPlcIwh\GWjdHi= MXeyN|A4PzJ2OR?=
MCF-7  M1XYRmZ2dmO2aX;uJGF{e2G7 NUGzUZlzPiCq M2DESWROW09? NYnvTFJb[XS2ZX71ZZRmeyC2aHWg[ox2\GmxeH;ubYwuKG:{IH\lcohmgGGvaXStbY5lfWOnZDDpcoNz\WG|ZTDpckBucVJvMkGg[ZhxemW|c3nvci=> NEfIXI8zOzB3MkCzOi=>
MCF-7 NED3bFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\jS|ExOCCwTT:xJO69VQ>? M{XiSVUh\A>? M3jLV4lvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kAyP87{LXXzeJJi\GmxbB?= NWfZRpBlOjJ7OEK3OlU>
MCF-7 NYLGZ3hnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\VbJkyODBibl2= M{f1WlUh\A>? M4jofIlvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kBnfXOjcnnlcIlvKEh? M4G4PFIzQTh{N{[1
1471.1 MmGxSpVv[3Srb36gRZN{[Xl? Mn3vNVAxKG6P NUe3RWFPOSCq M1rlc2V1V0kEoB?= MojueIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu MWOyNlg3QTFyNh?=
MCF-7 MXvGeY5kfGmxbjDBd5NigQ>? MkfwNVAxKG6P NXXRPJpjOSCq MYTFeG9JyqB? M4DpRZRic2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> NIryXnYzOjh4OUGwOi=>
HeLa NF\hPXhHfW6ldHnvckBCe3OjeR?= NUD4[pJPOTByIH7N NEHYT|YyKGh? M1XGc2V1V0kEoB?= Mn7veIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu MljmNlI5PjlzME[=
COS-7  M4Hh[mZ2dmO2aX;uJGF{e2G7 MYmxNFAhdk1? NX2zc3N4OSCq MXjFeG9JyqB? NHz0WGh1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> MXuyNlg3QTFyNh?=
BG1L-OHTLT  MoLVSpVv[3Srb36gRZN{[Xl? NIjwVYYyOMLibl2= MnqyNlTDqGkEoB?= NUT2[HJicW6qaXLpeJMhTVMQsTDlfJBz\XO|aX;u M3ztd|IzPjV{NUW4
BG1L-ICILT MV;GeY5kfGmxbjDBd5NigQ>? NH[yRWIyOMLibl2= NEPheVEzPMLiaNMg Mki2bY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w NH;xSWgzOjZ3MkW1PC=>
PC-9 MlTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjvSVlROC5yMEOtN|Ah|ryP NITPNIo1QCCq MlP4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NV2zcWJNOjJ3NkC2N|Q>
H1650 M{LyT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HaTFAvODB|LUOwJO69VQ>? NXLwSVV[PDhiaB?= M{\BVIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MmjRNlI2PjB4M{S=
H1975 NHzGd3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHWRpRrOC5yMEOtN|Ah|ryP MXO0PEBp NV;PW2hjcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGrYO2kzOjV4ME[zOC=>
H1975 MXfGeY5kfGmxbjDBd5NigQ>? MoLPN:Kh|ryP NHe2WFM{KGh? Mm\rZYJzd2ejdHXzJJRp\SCyaH;zdIhwNUWJRmKgbY5lfWO2aX;uJIJ6KGW|dILv[4Vv MlzsNlI2PjB4M{S=
H1975 NVG4e5MxTnWwY4Tpc44hSXO|YYm= MoDuN:Kh|ryP NUPpdVhTPyCm MXTpcoR2[2W|IFXHSnIh\XiycnXzd4lwdg>? NX\ZfWlZOjJ3NkC2N|Q>
HTR-8 NEezOnFHfW6ldHnvckBCe3OjeR?= NIH6[I8yyqEQvF2= M4Lad|EuPDhiaB?= MVnkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCLR1\CVFchdVKQQR?= MVuyNlM5OzFzMR?=
JEG-3 NFLvOYJHfW6ldHnvckBCe3OjeR?= M4rYPVHDqM7:TR?= M1fme|EuPDhiaB?= NYPFOm9U\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gTWdHSlB5IH3SUmE> MXmyNlM5OzFzMR?=
Huh7 NUXjdHRvTnWwY4Tpc44hSXO|YYm= NFixN5U2OMLizszN NEG0fIg1QCCq NFP3fpdqdmirYnn0d{Bo\W6rc4TlbY4udWWmaXH0[YQhWE:QMTD0doFve2GldHn2ZZRqd25? Mkn4NlI{ODR{OU[=
201T M2DwUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn2wOUDPxE1? NEjwOXQ4OiCq MW\pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIghfmGwZHX0ZY5q[g>? MVOyNlI2QDR5Nh?=
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MCF-7 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4KxPVHDqM7:TR?= Mm\EOU0yOCCm Mkewd5VxeHKnc4Pld{BGOi2rbnT1Z4VlKGe{b4f0bEBqdmirYnn0bY9v MWqyNlA1QTNzNh?=
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HepG2 M4XvZWFxd3C2b4Ppd{BCe3OjeR?= MY[wMlHDqM7:TR?= MXOyOEBp NEXk[41i[m:uaYPo[ZMhfGinIHXzeJJw\2WwLXnu[JVk\WRidYCtdoVofWyjdHnvckBw\iCjcH;BTUBidmRiYYDvUS=> NVvxTWQyOjF6MU[yN|M>
MCF7–iFR3 NVnoS25jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mly0NlAuOTByIH7N MlnsPVYhcA>? M2DrOIVvcGGwY3XzJGFRNWmwZIXj[YQh[2WubDDndo94fGhiaX7obYJqfGmxbh?= NVjvXlhPOjF5OUK4PFk>
MCF7S NU\UO5JTTnWwY4Tpc44hSXO|YYm= NWe1NZdPOcLizszN Mn;5OFghcA>? NFvMUoZld3ewcnXneYxifGW|IH;2[ZJidGxiRWNOtUBxem:2ZXnuJIxmfmWucx?= NWrjT|VQOjF3M{OxPVU>
MCF7 MVLGeY5kfGmxbjDBd5NigQ>? NYr2cmFROcLizszN NFvJOIw1QCCq NXO0R|ZV\G:5boLl[5Vt[XSnczDveoVz[WyuIFXS{tEheHKxdHXpckBt\X[nbIO= NF30V48zOTV|M{G5OS=>
MCF7S NXHRXWMxTnWwY4Tpc44hSXO|YYm= MXuxxsDPxE1? MnrUO{Bl M4q0foF1fGWwdXH0[ZMhfHWvb4LzdIhmemViZn;ycYF1cW:wIHHu[EBxem:uaX\ldoF1cW:w M1vOOlIyPTN|MUm1
MCF7S MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYOxT3VrOC53L{Gg{txO M2jQSVch\A>? MYjEUXNQ MkXE[IVkemWjc3XzJINmdGxiZYjwZY5{cW:w MoHyNlE2OzNzOUW=
T47D  MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnLUnN6PCCwTR?= NGnoNJo1OCCq MYDzeZBxemW|c3XzJINmdGxiZ4Lve5RpKG2xZHXyZZRmdHl? MWiyNVQ5ODN7MR?=
BT474  MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrMOEBvVQ>? NITS[441OCCq MkPTd5VxeHKnc4Pld{Bk\WyuIHfyc5d1cCCvb3TldoF1\Wy7 M{LOe|IyPDhyM{mx
T47D  NVjVRZF2TnWwY4Tpc44hSXO|YYm= MlTTNVAhdk1? NHP6[pY1OCCq NWGwNVMy\G:5boLl[5Vt[XSnczDFVu6yKHC{b4TlbY4> Mk\mNlE1QDB|OUG=
BT474  M3O4[mZ2dmO2aX;uJGF{e2G7 NUjNdGtnOTBibl2= NWH4OXpLPDBiaB?= NES0[Wpld3ewcnXneYxifGW|IFXS{tEheHKxdHXpci=> NGW5WGwzOTR6MEO5NS=>
MCF7 MYfGeY5kfGmxbjDBd5NigQ>? NYjnXIpiOTByIH7N MWO3JIQ> MWfy[YR2[2W|IFXS{tEh\XiycnXzd4lwdiC|aXfubYZq[2GwdHz5 NGHWfYozOTN7NkC5OC=>
T47D  MmrhSpVv[3Srb36gRZN{[Xl? MUSxNFAhdk1? MnXoO{Bl NXH6[nF{emWmdXPld{BGWs7zIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? NYqwOVlnOjF|OU[wPVQ>
BT474  MVfGeY5kfGmxbjDBd5NigQ>? NVPBT2RSOTByIH7N MVS3JIQ> M{nP[ZJm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> MW[yNVM6PjB7NB?=
MDAMB361 M{\MSWZ2dmO2aX;uJGF{e2G7 M4[wdFExOCCwTR?= MmnmO{Bl MVLy[YR2[2W|IFXS{tEh\XiycnXzd4lwdiC|aXfubYZq[2GwdHz5 M2SxRlIyOzl4MEm0
MCF7 NHrVc3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2n6OlAvODFvMTFOwG0> M1ezO|ch\A>? MXry[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? MoPqNlE{QTZyOUS=
T47D  MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYX1[4NpOC5yMT2xJO69VQ>? MVi3JIQ> Mn7QdoVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NUDnO4xsOjF|OU[wPVQ>
BT474  MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonqNE4xOS1zIN88US=> NVLUVI1kPyCm MUjy[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? MYiyNVM6PjB7NB?=
MDAMB361 NF:zOGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzLbGFROC5yMT2xJO69VQ>? MUK3JIQ> NHrqV4tz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NGnDdJIzOTN7NkC5OC=>
MCF7 MoW3SpVv[3Srb36gRZN{[Xl? Mn\ONVAxKG6P NUHISY9HPyCm NXTqbnBMcW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=> MV[yNVM6PjB7NB?=
T47D  NHfjVIRHfW6ldHnvckBCe3OjeR?= NWe1V2ZXOTByIH7N Mnr0O{Bl NXPD[41scW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=> NEflUnEzOTN7NkC5OC=>
BT474  MmXESpVv[3Srb36gRZN{[Xl? M1rkfVExOCCwTR?= MVS3JIQ> M173T4lv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= MVOyNVM6PjB7NB?=
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MCF7 M2XxS2Z2dmO2aX;uJGF{e2G7 MmHqNVAhdk1? Mn3hPVYhcA>? NVu0bHlH\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vyqB? NXLrZm9KOjF|N{izN|M>
MDA-MB-231 NIjsZ4lHfW6ldHnvckBCe3OjeR?= Mlv2NVAhdk1? NGDBcHc6PiCq M{Dt[4Rwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvcuKh MWmyNVM4QDN|Mx?=
SK-BR-3 MkTPSpVv[3Srb36gRZN{[Xl? M4qxNVExKG6P MnHCPVYhcA>? NFe2c21ld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc47DqA>? M1nEc|IyOzd6M{Oz
MCF-7 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYexNFAhdk1? M3zTOlczNzl4IHi= MWjjZZV{\XNiY3XscEBkgWOuZTDhdpJme3R? MUOyNVI6QTh4Mh?=
MMQ MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\LV4R[OC5yMEitOlI2KG6P NES4elM4OiCq NXnFeYt{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lMUBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MljvNlA4ODB5NUW=
MMQ NUnQVopbTnWwY4Tpc44hSXO|YYm= NGTs[mQxNjByOD22NlUhdk1? MkjpO|IhcA>? M{\WN4lvcGmkaYTzJHBTVCC|ZXPy[ZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NIPmVVYzODdyMEe1OS=>
MMQ M1nkRmZ2dmO2aX;uJGF{e2G7 M{fKOVAvODRvNkK1JI5O NID3PIo4OiCq MV\pcohq[mm2czDFVu6yKGW6cILld5Nqd25? NGjjeGozODdyMEe1OS=>
MMQ NVPGUGFmTnWwY4Tpc44hSXO|YYm= NX\5[lBTOC5yND22NlUhdk1? MofUO|IhcA>? NUPjPYFRfXC{ZXf1cIF1\XNiVFfG{tI{KGGwZDDUS2bPulKLSTDlfJBz\XO|aX;u NGHydWszODdyMEe1OS=>

... 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 从左到右依次将纯溶剂加入产品,现配现用:
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
in solvent
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