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 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVixMlMuOTByMDDuUS=> NG\zRYw1QCCq MlTVbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWSyOFk4QTJ7NB?=
MCF-7/LTED MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XySlEvOy1zMECwJI5O NHn3WII1QCCq MXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M2ryOlI1QTd7Mkm0
HCC1428 Mm\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jYSVEvOy1zMECwJI5O NF:5[nU1QCCq M1n0b4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NE\FbW8zPDl5OUK5OC=>
HCC1428/LTED MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGxMlMuOTByMDDuUS=> MVS0PEBp NUO3Z3lQcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGHHW3UzPDl5OUK5OC=>
LCC1 Mnf5SpVv[3Srb36gRZN{[Xl? NFvYWYcyODBibl2= NIS2UJk1QC1zNESgbC=> NUD6cGM2[WO2aY\heIV{KFWSUjDzbYdv[Wyrbne= MYKyOFg2QDJ5Nx?=
LCC9 MUDGeY5kfGmxbjDBd5NigQ>? MmfWNVAxKG6P NI[3WoM1QC1zNESgbC=> M4jWcYFkfGm4YYTld{BWWFJic3nncoFtcW6p MU[yOFg2QDJ5Nx?=
MCF-7  NFvzXWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfqXGcyODBibl2= NVPtVG5RPSCm MVPpcohq[mm2czDj[YxtKGe{b4f0bEB1dyBzMP-8iS=> NHTnTGozPDhzOUW1NC=>
mesangial  M2\vUmZ2dmO2aX;uJGF{e2G7 MW[wMlEuOTByIH7N NYjvSFVMPDhiaB?= M{T5W5N2eHC{ZYPz[ZMhXEeILd8yNU1qdmS3Y3XkJJR6eGViSW[gZ49tdGGpZX6= NYjTR3FkOjR5OUO2N|k>
Mesangial NVLiV5Z1TnWwY4Tpc44hSXO|YYm= M3HoXVAvOS1zMECgcm0> NIPUeHQxNjViaB?= MVfpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRiU33h[FIheGixc4Doc5J6dGG2aX;uJJZq[SCJUFXS NUTYeXF[OjR5OUO2N|k>
ER+ MCF-7/2a M2fwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXX1NYllUUN3ME2wMlAxPCEQvF2= NETNclgyPTN{NEi4OC=>
ER+ MCF-7 NHqxbXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\NR|IxOCCq MUjJR|UxRTBwMkGgcm0> NV7nb5E{OTV|MkS4PFQ>
MCF-7  MkX6SpVv[3Srb36gRZN{[Xl? M4nz[|ExyqCwTdMg NED3fJM4OiCq MkXndoV3\XK|ZYOgeIhmKGW|dILv[4VvKGWoZnXjeEhKSzVyIEGuPUDEnyBzMPMIllkhVSl? MlnQNlQ6ODh4NUK=
MCF-7  NVfJN|cyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mni5TWM2OMLib3[gZZBxem:6aX3heIVtgSB{IH7N MYOyN|Q1QDN2Nh?=
H1975  NIj6b3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVyzxsDPxE1? M2TJb|EhdQ>? NIWzfWJqdmO{ZXHz[ZMhfGinIHfl[ol1cW6rYjDz[Y5{cXSrdnn0fUBw\iCKMUm3OUBk\Wyuc9Mg MVqyOFI3QDhzMB?=
H1975 MWTGeY5kfGmxbjDBd5NigQ>? MVWzxsDPxE1? NV;NS4RZOSCv MoLVeZBz\We3bHH0[ZMhfGinIHzleoVtKG:oIFzleE04[w>? MkGyNlQzPjh6MUC=
MCF-7  NFr5TYJHfW6ldHnvckBCe3OjeR?= NHS2T2EyODEkgJnuUeKh MnjzO|IhcA>? MVfy[ZZmenOnczD0bIUheHKxdHXjeIl3\SCnZn\lZ5Qhd2ZiRUNCpIlvKGOnbHygbY53[XOrb36= M4rCSVI{QTN4N{ez
MCF-7  NXLZPZpCTnWwY4Tpc44hSXO|YYm= NU\VUZljOTBy4pEJcm3DqA>? MXqyOE81QCCq NHLR[Fdn[WOrbHn0ZZRmeyCrbo\hd4lwdiC2aILveYdpKE2PUIOnJI1w\HWuYYTpc44> NYXXdHplOjN7M{[3O|M>
BT474-tet-shMED1 NHTY[XBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrWNE4yNTVizszN MkDEO{Bl M2HueYlv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M1nR[VI{QTN4MkO0
ZR75-1-tet-shMED1  MmP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[wMlEuPSEQvF2= M4W1RVch\A>? NVzDNpU5cW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MlrkNlM6OzZ{M{S=
MCF-7-tet-shMED1 NH64ZW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPSVYkxNjFvNTFOwG0> MmnxO{Bl M{PiZYlv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MWCyN|k{PjJ|NB?=
HepG2  M1HXUWZ2dmO2aX;uJGF{e2G7 NHL0Xo4xNjBzLUGwJO69VQ>? MofGNVghcMLi MlXBZYN1cX[jdHXzJJRp\SCHUlWtcYVlcWG2ZXSgeJJidnOlcnnweIlwdiCxZjDBSlJGWg>? M{P1TlI{PzN|MUi4
MCF-7L  NGnYfndHfW6ldHnvckBCe3OjeR?= MlfLNVAxKG6PwrC= MWSxNEBucW5xMkSgbE81QCCq MV\y[ZN2dHS|IHnuJGVITlJuIFjFVlIh[W6mIFjFVlMheGixc4Doc5J6dGG2aX;uJIF1KHC{b3zvcodm\CCneIDvd5Vz\Q>? MXSyN|Y5PjRzNh?=
MCF-7L  NEe3ZWdHfW6ldHnvckBCe3OjeR?= MofuNVAxKG6PwrC= M{TCXlQ5KGh? NI\IdVNqdmS3Y3XzJJVxemWpdXzheIlwdiCxZjDtVm5CKG:oIFXHSnIhdGmpYX7kJGhDNUWJRh?= MkLjNlM3QDZ2MU[=
MCF-7L NWDudI9KTnWwY4Tpc44hSXO|YYm= NVfx[2U{OTByIH7NxsA> NHj3Zlk1QCCq NYLXdllFcW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= NWXlWHExOjN4OE[0NVY>
C4-12  MU\GeY5kfGmxbjDBd5NigQ>? MmjGNVAxKG6PwrC= MXG0PEBp NHzFdohqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU M{jyOlI{Pjh4NEG2
MCF-7L M{S3SWZ2dmO2aX;uJGF{e2G7 MXGxNFAhdk4EoB?= M1vH[FI1KGh? MlvQbY5lfWOnczDFS2ZTKHCqb4PwbI9zgWyjdHnvckBz\XG3aYLl[EBJSi2HR1[g[pVv[3Srb36= M3iwOFI{Pjh4NEG2
MMQ  MnnBSpVv[3Srb36gRZN{[Xl? M333XFAuPjJ3IH7N MmSyO|IhcA>? MmnN[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiZYP0do9o\W5icnXj[ZB1d3JvzsGgLGVT|rFr Mnu1NlM2OjN|NUe=
H1975  M{D6d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEH2PIExNjNzMkWtNVAh|ryP Ml3YOkBl MXTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmLhNlM{QTl7NUe=
H1975  MmrHRZBweHSxc3nzJGF{e2G7 NWjiOWx{OjByIH7N MnjGO|IhcA>? NIHyUVVmdmijbnPld{BmemyxdHnubYIhcW6mdXPl[EBieG:ydH;zbZM> NUnRW4t5OjN|OUm5OVc>
MCF-7  MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHQNVAwOTByL{GwNFAhdk1? Mon4Nk81NzZiZB?= MUHEUXNQ NIDJUYdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy MkjjNlM{OTN3ME[=
MCF-7  NV\CWJJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjINVAxKG6P MojoOEBl NHXy[YNFVVOR MmTybY5lfWOnczDhJIhq\2incjDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKHSqZTDHNUBxcGG|ZdMg NXfp[|dnOjN|MUO1NFY>
MLO-Y4  NHuwOplHfW6ldHnvckBCe3OjeR?= MkTPNeKh|ryP NWrhTFd{OSCq M3rCdolvcGmkaYTzJGUzNWmwZIXj[YQhS3h2MzDlfJBz\XO|aX;u NYO5[3pROjN{NEewOVc>
MCF-7 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXWOXZJOTByIH7N MV:0PEBp NVf3UIht[WK{b3fheIV{KHSqZTDwdo9tcW[ncnH0bZZmKGWoZnXjeEBw\iCvb3TldoF1\SCwaYTyc5NifGm4ZTDzeJJme3N? M3LwfFI{OjF4N{S0
TG1-1  MV;GeY5kfGmxbjDBd5NigQ>? M4H2bVHDqM7:TR?= MmD6NlQhcA>? MU\hZpJw\2G2ZYOgSVLDqGmwZIXj[YQh[WOldX31cIF1cW:wIH;mJGhKTi1zzsG= M1fqW|I{ODh6NkC3
TG1-1  NEXQWZNHfW6ldHnvckBCe3OjeR?= M{HYRlHDqM7:TR?= MnnqNlQhcA>? NWrZR2pX[WK{b3fheIV{KEV{wrDpcoR2[2WmIHHjZ5VufWyjdHnvckBw\iCSSUPL MkLtNlMxQDh4MEe=
MCF7 NHnCNJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HTclExOCCwTR?= MVy0PEBp NXrTcVYxdGWjZIOgeI8h[SC|aX3pcIFzKGyxc4OgbY4he3W{dnn2ZYwh[XNid3n0bEBld3ixcoXibYNqdiCjbH;u[S=> M1njOlI{ODd5MkS5
MCF7 M1HzbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37wbFExOCCwTR?= MWq0PEBp NH;3UGNmdmijbnPld{BvfXSuaX6tcYVlcWG2ZXSgZ4VtdCCmZXH0bC=> MYCyN|A4PzJ2OR?=
MCF-7  MXrGeY5kfGmxbjDBd5NigQ>? NWD1[5lCPiCq MlvDSG1UVw>? NV73Wolk[XS2ZX71ZZRmeyC2aHWg[ox2\GmxeH;ubYwuKG:{IH\lcohmgGGvaXStbY5lfWOnZDDpcoNz\WG|ZTDpckBucVJvMkGg[ZhxemW|c3nvci=> M3XjTFI{ODV{MEO2
MCF-7 MlfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fkdFExOCCwTT:xJO69VQ>? NHvwWpQ2KGR? M1PpXolvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kAyP87{LXXzeJJi\GmxbB?= NHPN[FkzOjl6Mke2OS=>
MCF-7 NUTZVYZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nveVExOCCwTR?= NFv2Xm42KGR? NYDuSpFZcW6qaXLpeJMhfGinIIP0bY12dGG2aX;uJI9nKG[3c3HybYVtcW5iSB?= NUThZ|F{OjJ7OEK3OlU>
1471.1 M3e4U2Z2dmO2aX;uJGF{e2G7 NFz3cmoyODBibl2= NFfYZWgyKGh? M{nLeGV1V0kEoB?= MUD0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= MUmyNlg3QTFyNh?=
MCF-7 NVHubY1XTnWwY4Tpc44hSXO|YYm= MljBNVAxKG6P Moj0NUBp NIryXppGfE:KwrC= MUf0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= NEC4ZnQzOjh4OUGwOi=>
HeLa MmflSpVv[3Srb36gRZN{[Xl? NH35SlgyODBibl2= MnPCNUBp NXGwTlRMTXSRSNMg MUf0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= MVOyNlg3QTFyNh?=
COS-7  MY\GeY5kfGmxbjDBd5NigQ>? NEHqVosyODBibl2= MYGxJIg> NXy0TJg2TXSRSNMg MmDPeIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu MkT6NlI5PjlzME[=
BG1L-OHTLT  MVPGeY5kfGmxbjDBd5NigQ>? MorMNVDDqG6P NUDhZ2M6OjUEoHlCpC=> MVHpcohq[mm2czDFVu6yKGW6cILld5Nqd25? NYPyPIllOjJ4NUK1OVg>
BG1L-ICILT MWPGeY5kfGmxbjDBd5NigQ>? M1;kc|ExyqCwTR?= M13YUFI1yqCqwrC= NYDIRWNscW6qaXLpeJMhTVMQsTDlfJBz\XO|aX;u MV[yNlY2OjV3OB?=
PC-9 MmPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXibVQxNjByMz2zNEDPxE1? MWW0PEBp NH;MV3hqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXHS[VVLOjJ3NkC2N|Q>
H1650 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljvNE4xODNvM{Cg{txO MVe0PEBp MlqwbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NEXiT4UzOjV4ME[zOC=>
H1975 M1:3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;Wb41LOC5yMEOtN|Ah|ryP MXG0PEBp M{nPUIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXPBVYxSOjJ3NkC2N|Q>
H1975 NIK3VGpHfW6ldHnvckBCe3OjeR?= NG\qNII{yqEQvF2= NITBbJM{KGh? MX\hZpJw\2G2ZYOgeIhmKHCqb4PwbI8uTUeIUjDpcoR2[3Srb36gZpkh\XO2cn;n[Y4> MW[yNlU3ODZ|NB?=
H1975 MVPGeY5kfGmxbjDBd5NigQ>? NXzzTnlVO8LizszN NIrsbW44KGR? NX\1WVl4cW6mdXPld{BGT0[UIHX4dJJme3Orb36= NXOzWHJrOjJ3NkC2N|Q>
HTR-8 M2\0TGZ2dmO2aX;uJGF{e2G7 MYexxsDPxE1? MV:xMVQ5KGh? M2L4VYRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIFnHSmJRPyCvUl7B NUTYdVVXOjJ|OEOxNVE>
JEG-3 NGXlbIVHfW6ldHnvckBCe3OjeR?= M2T6TVHDqM7:TR?= NF[0V5cyNTR6IHi= MV3kc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCLR1\CVFchdVKQQR?= NHLwRpUzOjN6M{GxNS=>
Huh7 NYfHfFduTnWwY4Tpc44hSXO|YYm= NGDEeHg2OMLizszN MomxOFghcA>? NVz4V|NmcW6qaXLpeJMh\2WwaYP0[YlvNW2nZHnheIVlKFCRTkGgeJJidnOjY4TpeoF1cW:w NU\a[lE6OjJ|MESyPVY>
201T MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLaOUDPxE1? NFHjdYw4OiCq MWLpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIghfmGwZHX0ZY5q[g>? NVH1NWtCOjJ{NUi0O|Y>
A549  M{PWNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDGW2hKPSEQvF2= MnW2O|IhcA>? NVnZXZBNcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\hcoRmfGGwaXK= MmnVNlIzPTh2N{[=
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MCF-7 MkHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfEeG0yOcLizszN M2HNV|UuOTBiZB?= MoPXd5VxeHKnc4Pld{BGOi2rbnT1Z4VlKGe{b4f0bEBqdmirYnn0bY9v MlzSNlIxPDl|MU[=
HCC-1428 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;ONeKh|ryP MnvBOU0yOCCm NH3QNmN{fXCycnXzd4V{KEV{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? M{n1V|IzODR7M{G2
MDA-361 M1O4WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvM[IIyyqEQvF2= NF\KVlQ2NTFyIHS= MWrzeZBxemW|c3XzJGUzNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> NYP0OplsOjJyNEmzNVY>
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MCF7S MX3GeY5kfGmxbjDBd5NigQ>? MkLkNeKh|ryP MXu0PEBp M2LidYRwf26{ZXf1cIF1\XNib4\ldoFtdCCHUt8xJJBzd3SnaX6gcIV3\Wy| NUXyUFZ5OjF3M{OxPVU>
MCF7 NWCyendwTnWwY4Tpc44hSXO|YYm= Mn7jNeKh|ryP MX60PEBp MV3kc5dvemWpdXzheIV{KG:4ZYLhcIwhTVMQsTDwdo91\WmwIHzleoVtew>? MmjnNlE2OzNzOUW=
MCF7S MmX6SpVv[3Srb36gRZN{[Xl? NVH6fYRTOcLizszN NIj3fFY4KGR? M4ezc4F1fGWwdXH0[ZMhfHWvb4LzdIhmemViZn;ycYF1cW:wIHHu[EBxem:uaX\ldoF1cW:w NVvkbWVLOjF3M{OxPVU>
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T47D  MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXUVpk1KG6P M{C0eVQxKGh? NXrmfFF5e3WycILld5NmeyClZXzsJIdzd3e2aDDtc4RmemG2ZXz5 NWi0bVM2OjF2OECzPVE>
BT474  M1fGUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVq0JI5O NIizTI01OCCq NGfTW25{fXCycnXzd4V{KGOnbHyg[5Jwf3SqIH3v[IVz[XSnbIm= Ml\5NlE1QDB|OUG=
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MCF7 MljBSpVv[3Srb36gRZN{[Xl? MknHNVAxKG6P MlfuO{Bl M3XkUZJm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> MnTiNlE{QTZyOUS=
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BT474  M2ezeGZ2dmO2aX;uJGF{e2G7 MkjMNVAxKG6P M1K1c|ch\A>? MYDy[YR2[2W|IFXS{tEh\XiycnXzd4lwdiC|aXfubYZq[2GwdHz5 NX;JeJRZOjF|OU[wPVQ>
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MCF7 NX\QVmZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H1VVAvODFvMTFOwG0> M1TqO|ch\A>? MWDy[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? NHjFR4YzOTN7NkC5OC=>
T47D  M3jOO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXGPGNxOC5yMT2xJO69VQ>? M2eye|ch\A>? M37QUpJm\HWlZYOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= Ml;BNlE{QTZyOUS=
BT474  NX7rW2l6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLmOnd{OC5yMT2xJO69VQ>? NFfyOHU4KGR? MVzy[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? M1fOXVIyOzl4MEm0
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T47D  M2XhUWZ2dmO2aX;uJGF{e2G7 NWnHVJpIOTByIH7N NFr2bnc4KGR? NWrLcWJEcW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=> M2[w[lIyOzl4MEm0
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MCF7 MnHrSpVv[3Srb36gRZN{[Xl? MUmxNEBvVQ>? M1\sOFk3KGh? MnHV[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uxsA> MV[yNVM4QDN|Mx?=
MDA-MB-231 NI\KSHVHfW6ldHnvckBCe3OjeR?= MWSxNEBvVQ>? NWjRWGQxQTZiaB?= NVzIW5BD\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vyqB? MYCyNVM4QDN|Mx?=
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MCF-7 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnjNVAxKG6P MlmxO|IwQTZiaB?= NVLmdYRv[2G3c3XzJINmdGxiY4njcIUh[XK{ZYP0 MkfZNlEzQTl6NkK=
MMQ NH6yUZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MViwMlAxQC14MkWgcm0> NYPoemxuPzJiaB?= MWHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4TvUVIxPzByN{W1
MMQ MlXDSpVv[3Srb36gRZN{[Xl? MVmwMlAxQC14MkWgcm0> M2G4WlczKGh? MV3pcohq[mm2czDQVmwhe2WlcnX0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVfjfWo4OjB5MEC3OVU>
MMQ MYrGeY5kfGmxbjDBd5NigQ>? MoHMNE4xPC14MkWgcm0> M3z1S|czKGh? MkDkbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w NXrJbWdrOjB5MEC3OVU>
MMQ MVzGeY5kfGmxbjDBd5NigQ>? M3HreVAvODRvNkK1JI5O MoOyO|IhcA>? M1y4N5VxemWpdXzheIV{KFSJRt8yN{BidmRiVFfG{tJTUUliZYjwdoV{e2mxbh?= NVXqdI14OjB5MEC3OVU>

... 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(数据来自Selleck实验检测而非文献):
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