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  
In DMSO RMB 533.25 现货
RMB 567.34 现货
RMB 2233.34 现货
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客户使用Selleck该产品发表文献26篇:

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 M1vJNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzESGgyNjNvMUCwNEBvVQ>? NH7IVYQ1QCCq MoKybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3Ty[|I1QTd7Mkm0
MCF-7/LTED MoPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXWxMlMuOTByMDDuUS=> NHXSVJk1QCCq MUTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MmryNlQ6Pzl{OUS=
HCC1428 M2fre2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPUNU4{NTFyMECgcm0> M4HBR|Q5KGh? NG\JXFVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnrXNlQ6Pzl{OUS=
HCC1428/LTED NIHTbJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWD5dlF1OS5|LUGwNFAhdk1? NYHa[odlPDhiaB?= MUjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NInycpAzPDl5OUK5OC=>
LCC1 NEnwRlhHfW6ldHnvckBCe3OjeR?= MlOyNVAxKG6P M3z6WlQ5NTF2NDDo NIi0cnVi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= MkT0NlQ5PTh{N{e=
LCC9 MXfGeY5kfGmxbjDBd5NigQ>? NFjHOXEyODBibl2= NGflbXM1QC1zNESgbC=> NHjwTYZi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= NIPxSYMzPDh3OEK3Oy=>
MCF-7  MkDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfzNoUzOTByIH7N M4TnXFUh\A>? M4H3WolvcGmkaYTzJINmdGxiZ4Lve5RpKHSxIEGw89yG NYDJeo9iOjR6MUm1OVA>
mesangial  MkO3SpVv[3Srb36gRZN{[Xl? MU[wMlEuOTByIH7N M4jSUFQ5KGh? MV3zeZBxemW|c3XzJHRITi4QskGtbY5lfWOnZDD0fZBmKEmYIHPvcIxi\2Ww MWKyOFc6OzZ|OR?=
Mesangial Moe2SpVv[3Srb36gRZN{[Xl? M3[5ZlAvOS1zMECgcm0> NVnKRXRtOC53IHi= M2D6cYlvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDTcYFlOiCyaH;zdIhwenmuYYTpc44hfmmjIFfQSXI> M4fhPFI1Pzl|NkO5
ER+ MCF-7/2a Mm\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnx[ZJKSzVyPUCuNFA1KM7:TR?= NGPPfokyPTN{NEi4OC=>
ER+ MCF-7 NIKx[HBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKyNFAhcA>? MWXJR|UxRTBwMkGgcm0> NULhfohrOTV|MkS4PFQ>
MCF-7  MmH1SpVv[3Srb36gRZN{[Xl? MW[xNOKhdk4EoB?= M2\XN|czKGh? NV;lcJg6emW4ZYLz[ZMhfGinIHXzeJJw\2WwIHXm[oVkfCiLQ{WwJFEvQSEFlzCxNQKJmjliTTm= M4XSUlI1QTB6NkWy
MCF-7  NW\DbIhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1z1Z2lEPTEEoH;mJIFxeHKxeHntZZRmdHliMjDuUS=> NULMNIxEOjN2NEizOFY>
H1975  MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUm4dXBuO8LizszN MXuxJI0> MofsbY5kemWjc3XzJJRp\SCpZX\peIlvcWJic3Xud4l1cX[rdImgc4YhUDF7N{WgZ4VtdHQEoB?= M1vaWlI1OjZ6OEGw
H1975 M2XZWmZ2dmO2aX;uJGF{e2G7 MofEN:Kh|ryP MV[xJI0> M4i2SJVxemWpdXzheIV{KHSqZTDs[ZZmdCCxZjDM[ZQuP2N? NHLjN20zPDJ4OEixNC=>
MCF-7  MVvGeY5kfGmxbjDBd5NigQ>? Mn\uNVAx6oDLbl5CpC=> NGfxW4g4OiCq M1P0NJJmfmW{c3XzJJRp\SCycn;0[YN1cX[nIHXm[oVkfCCxZjDFNuKhcW5iY3XscEBqdn[jc3nvci=> MW[yN|k{Pjd5Mx?=
MCF-7  M1X1XWZ2dmO2aX;uJGF{e2G7 MVWxNFDjiImwTdMg M3r1eVI1NzR6IHi= Mk[z[oFkcWyrdHH0[ZMhcW64YYPpc44hfGi{b4XnbEBOVVC|JzDtc4R2dGG2aX;u MkDPNlM6OzZ5N{O=
BT474-tet-shMED1 NFLHbY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXizeW9xOC5zLUWg{txO NH;Cclk4KGR? NWDUUlVbcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MV6yN|k{PjJ|NB?=
ZR75-1-tet-shMED1  MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;UXFAvOS13IN88US=> Mn6xO{Bl M33DOIlv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M4q4Z|I{QTN4MkO0
MCF-7-tet-shMED1 NGqyOVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7FVZZXOC5zLUWg{txO Mnn5O{Bl NH3TUIpqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NH:2c4gzOzl|NkKzOC=>
HepG2  MYDGeY5kfGmxbjDBd5NigQ>? NXrJ[pFsOC5yMT2xNEDPxE1? Mm\yNVghcMLi MlviZYN1cX[jdHXzJJRp\SCHUlWtcYVlcWG2ZXSgeJJidnOlcnnweIlwdiCxZjDBSlJGWg>? MVeyN|c{OzF6OB?=
MCF-7L  Mn\kSpVv[3Srb36gRZN{[Xl? NEPPWXcyODBibl5CpC=> NF7ZR3gyOCCvaX6vNlQhcC92ODDo NHrVdWVz\XO3bITzJIlvKEWJRmKsJGhGWjJiYX7kJGhGWjNicHjvd5Bpd3K7bHH0bY9vKGG2IIDyc4xwdmenZDDlfJBwe3W{ZR?= Ml3sNlM3QDZ2MU[=
MCF-7L  NYHLNIYyTnWwY4Tpc44hSXO|YYm= NIfGd2QyODBibl5CpC=> MkfkOFghcA>? NGLicmpqdmS3Y3XzJJVxemWpdXzheIlwdiCxZjDtVm5CKG:oIFXHSnIhdGmpYX7kJGhDNUWJRh?= MUeyN|Y5PjRzNh?=
MCF-7L MWDGeY5kfGmxbjDBd5NigQ>? NHXVcJcyODBibl5CpC=> MXm0PEBp MVHpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT NXTxVnZpOjN4OE[0NVY>
C4-12  MVTGeY5kfGmxbjDBd5NigQ>? Ml\GNVAxKG6PwrC= MVq0PEBp NIHHV4JqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU NWS0T3VwOjN4OE[0NVY>
MCF-7L MV;GeY5kfGmxbjDBd5NigQ>? NWKw[XhqOTByIH7NxsA> NWDaVmNXOjRiaB?= MXHpcoR2[2W|IFXHSnIheGixc4Doc5J6dGG2aX;uJJJmeXWrcnXkJGhDNUWJRjDmeY5kfGmxbh?= NX\j[4U5OjN4OE[0NVY>
MMQ  NWLQNlFHTnWwY4Tpc44hSXO|YYm= M2jjeFAuPjJ3IH7N M3fmU|czKGh? MVzkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCnc4Tyc4dmdiC{ZXPldJRwei4QsTCoSXLPuSl? M4XnV|I{PTJ|M{W3
H1975  NI[zc3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLER|YxNjNzMkWtNVAh|ryP MUW2JIQ> Mmi1bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYLBSZJnOjN|OUm5OVc>
H1975  M3;je2Fxd3C2b4Ppd{BCe3OjeR?= MW[yNFAhdk1? NFvN[pk4OiCq MlKw[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz NIH3UIwzOzN7OUm1Oy=>
MCF-7  NVziPWoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\IUo8yOC9zMECvNVAxOCCwTR?= MmrpNk81NzZiZB?= MoPLSG1UVw>? M2C1dolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= MX[yN|MyOzVyNh?=
MCF-7  M{LKWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnSNVAxKG6P MYe0JIQ> NF7mcZNFVVOR M4T5Rolv\HWlZYOgZUBpcWeqZYKgdJJweG:{dHnvckBw\iClZXzsd{BqdiC2aHWgS|EheGijc3ZCpC=> M161blI{OzF|NUC2
MLO-Y4  NXK0UWN1TnWwY4Tpc44hSXO|YYm= M1zjXVHDqM7:TR?= NFOweYgyKGh? NXLhNY9scW6qaXLpeJMhTTJvaX7keYNm\CCFeESzJIV5eHKnc4Ppc44> M1vwXlI{OjR5MEW3
MCF-7 NUDiSIJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHtS5p[OTByIH7N NGHqe4Q1QCCq M1XqVYFjem:pYYTld{B1cGVicILvcIln\XKjdHn2[UBm\m[nY4Sgc4YhdW:mZYLheIUhdmm2cn;zZZRqfmVic4Ty[ZN{ MUKyN|IyPjd2NB?=
TG1-1  MoTCSpVv[3Srb36gRZN{[Xl? NXj2NFNKOcLizszN NWrYT3ZvOjRiaB?= M2jJT4Fjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhUEmILUJOtS=> MnHQNlMxQDh4MEe=
TG1-1  NYXLe5htTnWwY4Tpc44hSXO|YYm= M3nPc|HDqM7:TR?= NGjv[IQzPCCq NIq2SYdi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKFCLM1u= MXyyN|A5QDZyNx?=
MCF7 M13vUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXGxNFAhdk1? MoT0OFghcA>? NVXnXYNtdGWjZIOgeI8h[SC|aX3pcIFzKGyxc4OgbY4he3W{dnn2ZYwh[XNid3n0bEBld3ixcoXibYNqdiCjbH;u[S=> NGLaS2EzOzB5N{K0PS=>
MCF7 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PnT|ExOCCwTR?= NGrXZ|k1QCCq MYTlcohidmOnczDueZRtcW5vbXXkbYF1\WRiY3XscEBl\WG2aB?= NVq1fnVXOjNyN{eyOFk>
MCF-7  NH:xTpRHfW6ldHnvckBCe3OjeR?= NXTuXXQ{PiCq NYrZb|ZCTE2VTx?= M2m5[IF1fGWwdXH0[ZMhfGinIH\seYRqd3ixbnnsMUBweiCoZX7o[ZhidWmmLXnu[JVk\WRiaX7jdoVie2ViaX6gcYlTNTJzIHX4dJJme3Orb36= NV;0TId{OjNyNUKwN|Y>
MCF-7 M4HqZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOxNFAhdk1xMTFOwG0> NUPPdYx{PSCm Mly2bY5pcWKrdIOgeIhmKHO2aX31cIF1cW:wIH;mJFE4|rJvZYP0doFlcW:u MlXCNlI6QDJ5NkW=
MCF-7 M1fZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnqe3FEOTByIH7N NVfHNVJMPSCm MkLsbY5pcWKrdIOgeIhmKHO2aX31cIF1cW:wIH;mJIZ2e2G{aXXsbY4hUA>? NFnoRogzOjl6Mke2OS=>
1471.1 MkDxSpVv[3Srb36gRZN{[Xl? M1;nTVExOCCwTR?= MknUNUBp M4jiU2V1V0kEoB?= MlvKeIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu NYnBW2d{OjJ6NkmxNFY>
MCF-7 NIS0[nJHfW6ldHnvckBCe3OjeR?= NUH4S|NZOTByIH7N MWWxJIg> MkL1SZRQUMLi MknyeIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu M4S2O|IzQDZ7MUC2
HeLa NULFeW1ETnWwY4Tpc44hSXO|YYm= NVzwVYNbOTByIH7N MkXXNUBp MnrBSZRQUMLi Mn7GeIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu MXSyNlg3QTFyNh?=
COS-7  MWrGeY5kfGmxbjDBd5NigQ>? NHzCOHcyODBibl2= NX24bFBTOSCq MnviSZRQUMLi MVf0ZYtmeyCxbjDhJJB2dmO2YYTlJJN1[WmwaX7nJJBifHSncn6= NX;adJVmOjJ6NkmxNFY>
BG1L-OHTLT  MlTPSpVv[3Srb36gRZN{[Xl? NUL1dZFpOTEEoH7N M3z5VlI1yqCqwrC= M3u1TIlvcGmkaYTzJGVT|rFiZYjwdoV{e2mxbh?= MmWxNlI3PTJ3NUi=
BG1L-ICILT NYLG[JdETnWwY4Tpc44hSXO|YYm= NHvoPIkyOMLibl2= MUiyOOKhcMLi MYPpcohq[mm2czDFVu6yKGW6cILld5Nqd25? NXzRfHFEOjJ4NUK1OVg>
PC-9 MlL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLCNE4xODNvM{Cg{txO NHfhUI01QCCq NY\uXWxEcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGHZR4EzOjV4ME[zOC=>
H1650 M1fRW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfuVIZJOC5yMEOtN|Ah|ryP NFXaWmo1QCCq MoS1bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NGG2e4YzOjV4ME[zOC=>
H1975 MoH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fne|AvODB|LUOwJO69VQ>? MUS0PEBp NYDvSpdDcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NEnhW5gzOjV4ME[zOC=>
H1975 MlXlSpVv[3Srb36gRZN{[Xl? MX6zxsDPxE1? MVuzJIg> M2LSOYFjem:pYYTld{B1cGVicHjvd5Bpdy2HR1\SJIlv\HWldHnvckBjgSCnc4Tyc4dmdg>? M{LKO|IzPTZyNkO0
H1975 M1voRmZ2dmO2aX;uJGF{e2G7 Ml3iN:Kh|ryP M3S4c|ch\A>? NWTDNHZqcW6mdXPld{BGT0[UIHX4dJJme3Orb36= M2rWXlIzPTZyNkO0
HTR-8 NXryb2JoTnWwY4Tpc44hSXO|YYm= Mn\uNeKh|ryP MYSxMVQ5KGh? MlzG[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSVfGRnA4KG2UTlG= MVGyNlM5OzFzMR?=
JEG-3 NIHLdYhHfW6ldHnvckBCe3OjeR?= NH;2UY4yyqEQvF2= MWKxMVQ5KGh? MVjkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCLR1\CVFchdVKQQR?= MXyyNlM5OzFzMR?=
Huh7 MlPxSpVv[3Srb36gRZN{[Xl? NIGyUHk2OMLizszN MVO0PEBp M2W2XYlvcGmkaYTzJIdmdmm|dHXpck1u\WSrYYTl[EBRV05zIITyZY5{[WO2aY\heIlwdg>? NFru[ZczOjNyNEK5Oi=>
201T M1PFdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XwXFUh|ryP MlXEO|IhcA>? MoDXbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? M1;VTlIzOjV6NEe2
A549  NVnIZnFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXi1JO69VQ>? NXvUVFJkPzJiaB?= M4fhfIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4YX7k[ZRidmmk MmTmNlIzPTh2N{[=
MCF-7 MlL3SpVv[3Srb36gRZN{[Xl? MVuxxsDPxE1? MYWyOEBpyqB? NGrRfGJld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? MUeyNlA1QTNzNh?=
HCC-1428 Mo\pSpVv[3Srb36gRZN{[Xl? M3Tpc|HDqM7:TR?= NVrBW2w6OjRiaNMg MnjW[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh M3e4[VIzODR7M{G2
MDA-361 MoHISpVv[3Srb36gRZN{[Xl? MnSzNeKh|ryP MmXGNlQhcMLi NIO4THhld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? MlnhNlIxPDl|MU[=
ZR75-1 MnvLSpVv[3Srb36gRZN{[Xl? NFTkSZIyyqEQvF2= NFXVT5EzPCCqwrC= Mmjv[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh M4\wV|IzODR7M{G2
MCF-7 NEPQNG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUCxxsDPxE1? MVu1MVExKGR? MUnzeZBxemW|c3XzJGUzNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> NXPvVHBWOjJyNEmzNVY>
HCC-1428 M{XHWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1z2dVHDqM7:TR?= MYG1MVExKGR? NXHy[Y94e3WycILld5NmeyCHMj3pcoR2[2WmIHfyc5d1cCCrbnjpZol1cW:w MnnUNlIxPDl|MU[=
MDA-361 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfGTIl3OcLizszN NF[0V2Q2NTFyIHS= MVHzeZBxemW|c3XzJGUzNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> MXuyNlA1QTNzNh?=
ZR75-1 NFraZVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTtNeKh|ryP MlXrOU0yOCCm MXTzeZBxemW|c3XzJGUzNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> MWqyNlA1QTNzNh?=
MCF-7/AC-1 MkfCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUKwMVAvOiEQvF2= M1q1cFYh\A>? NFP6[oJqdmirYnn0d{Bk\WyuIHfyc5d1cCCvb3Tld5RtgQ>? NULqdFlxOjJyNEK3PVI>
MCF7 MknqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[xNEDDvU1? NFX4Opk1QCCq M3q4d4lv\HWlZYOgZ4VtdCCrbnjpZol1cW:wIIfobYNpKGOjbjDi[UBmdmijbnPl[EBjgSCoaXLyc4Jt[XO2cx?= MV2yNlA1OTh6Nx?=
MMQ NWK5ZXRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEm3OHAxNTZ{NTDuUS=> NWDpTIF4PzJiaB?= NXrGdlBoeHKxZIXj[ZMhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbtMg MWKyNlAyPTFyMR?=
MMQ MYHGeY5kfGmxbjDBd5NigQ>? MVKwMVYzPSCwTR?= NIn1dGE4OiCq MYDwdo9lfWOnczDhJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSsJIRwe2VvZHXw[Y5l\W62IILl[JVkfGmxbjDpckBRWkxic3XjdoV1cW:w NG\ibpozOjBzNUGwNS=>
MCF7 Ml7DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjBNE0yKM7:TR?= NGjxbWYzPC1zMkCgbC=> M4TlNIlvcGmkaYTzJJRp\SCpcn;3eIghd2ZiTVPGO{1[Si1zwrC= MljNNlE5PjN{NUi=
HepG2 MUnBdI9xfG:|aYOgRZN{[Xl? NFnN[JYxNjIEoN88US=> NFfMdmszPCCq MVvhZo9tcXOqZYOgeIhmKGW|dILv[4VvNWmwZIXj[YQhfXBvcnXneYxifGmxbjDv[kBieG:DSTDhcoQh[XCxTR?= NHXNT|EzOThzNkKzNy=>
MCF7–iFR3 NF[1WppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DxWVIxNTFyMDDuUS=> MWG5OkBp NVLScFVv\W6qYX7j[ZMhSVBvaX7keYNm\CClZXzsJIdzd3e2aDDpcohq[mm2aX;u MlPXNlE4QTJ6OEm=
MCF7S MVzGeY5kfGmxbjDBd5NigQ>? MYWxxsDPxE1? NHzEW|U1QCCq NFjjfWFld3ewcnXneYxifGW|IH;2[ZJidGxiRWNOtUBxem:2ZXnuJIxmfmWucx?= NHT2Wo0zOTV|M{G5OS=>
MCF7 M4noc2Z2dmO2aX;uJGF{e2G7 MXOxxsDPxE1? Ml\VOFghcA>? M1PySYRwf26{ZXf1cIF1\XNib4\ldoFtdCCHUt8xJJBzd3SnaX6gcIV3\Wy| NYjqPYltOjF3M{OxPVU>
MCF7S M1ftcGZ2dmO2aX;uJGF{e2G7 NUjsS2dGOcLizszN MUS3JIQ> NWf1WmtU[XS2ZX71ZZRmeyC2dX3vdpNxcGW{ZTDmc5Ju[XSrb36gZY5lKHC{b3zp[oVz[XSrb36= MkDtNlE2OzNzOUW=
MCF7S NVflfZZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTnNE42NzFizszN MXG3JIQ> MWHEUXNQ MV\k[YNz\WG|ZYOgZ4VtdCCneIDhcpNqd25? MWSyNVU{OzF7NR?=
T47D  MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHmzUmQ1KG6P Mm\6OFAhcA>? MkTjd5VxeHKnc4Pld{Bk\WyuIHfyc5d1cCCvb3TldoF1\Wy7 MUWyNVQ5ODN7MR?=
BT474  M4PX[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXe0JI5O MnXpOFAhcA>? M33SdpN2eHC{ZYPz[ZMh[2WubDDndo94fGhibX;k[ZJifGWueR?= M4\PcFIyPDhyM{mx
T47D  NV\JcnZvTnWwY4Tpc44hSXO|YYm= NVrMO25GOTBibl2= M1rUdFQxKGh? NV;seWNJ\G:5boLl[5Vt[XSnczDFVu6yKHC{b4TlbY4> NF;QWmkzOTR6MEO5NS=>
BT474  M{HjTWZ2dmO2aX;uJGF{e2G7 NW\xUXhYOTBibl2= MWC0NEBp NFf6XXRld3ewcnXneYxifGW|IFXS{tEheHKxdHXpci=> M1XzelIyPDhyM{mx
MCF7 NVq3[WJOTnWwY4Tpc44hSXO|YYm= M1LTTFExOCCwTR?= MoHKO{Bl MknjdoVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> MWKyNVM6PjB7NB?=
T47D  Ml;RSpVv[3Srb36gRZN{[Xl? M2Dm[lExOCCwTR?= MkHwO{Bl NHXLSY9z\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 NYLub4tzOjF|OU[wPVQ>
BT474  NH;mXI1HfW6ldHnvckBCe3OjeR?= NYrTSIVHOTByIH7N NHi0bFE4KGR? NYf4TVByemWmdXPld{BGWs7zIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? MWiyNVM6PjB7NB?=
MDAMB361 NVW4bnR1TnWwY4Tpc44hSXO|YYm= MkH2NVAxKG6P NVrNPZplPyCm MnTIdoVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> MViyNVM6PjB7NB?=
MCF7 M2O5b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXGwMlAyNTFizszN NEXFVmI4KGR? MVHy[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? NHK0fIgzOTN7NkC5OC=>
T47D  MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TmUFAvODFvMTFOwG0> MlLqO{Bl NHj2dGZz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NFfidGIzOTN7NkC5OC=>
BT474  MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nqfVAvODFvMTFOwG0> NGHle4Q4KGR? NHTrZmNz\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M{fiTlIyOzl4MEm0
MDAMB361 NX3LTHNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXKwMlAyNTFizszN Mk\IO{Bl MWPy[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? NHjH[HEzOTN7NkC5OC=>
MCF7 MoD4SpVv[3Srb36gRZN{[Xl? MmjPNVAxKG6P NYTmW3NHPyCm M3n2UYlv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= Ml;PNlE{QTZyOUS=
T47D  MlThSpVv[3Srb36gRZN{[Xl? NVLKd4Q2OTByIH7N Mk\sO{Bl NYPLZolOcW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=> M4WwfVIyOzl4MEm0
BT474  MVLGeY5kfGmxbjDBd5NigQ>? NFzWSWgyODBibl2= M3\W[Fch\A>? NYrmRWQycW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=> NX3mcoVuOjF|OU[wPVQ>
MDAMB361 M{fvUGZ2dmO2aX;uJGF{e2G7 MWGxNFAhdk1? MU[3JIQ> NFnQRnZqdmS3Y3XzJI9nKEW{YlKzJIFv\CCHcnLCOEBz\WOncITvdkBmgHC{ZYPzbY9vKGGwZDDzbYdv[WyuaX7n NWnu[2hLOjF|OU[wPVQ>
MCF7 NX\TRoVETnWwY4Tpc44hSXO|YYm= Ml\lNVAhdk1? MnzYPVYhcA>? M4T4VIRwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvcuKh NEfxVXQzOTN5OEOzNy=>
MDA-MB-231 NYnGXZhjTnWwY4Tpc44hSXO|YYm= M3XHNlExKG6P NVqxWlg4QTZiaB?= NVPPfpRO\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vyqB? NV3Ud4JkOjF|N{izN|M>
SK-BR-3 M{XGNWZ2dmO2aX;uJGF{e2G7 M4mwTFExKG6P M2D4WFk3KGh? MoHa[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uxsA> M1HXR|IyOzd6M{Oz
MCF-7 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HKNFExOCCwTR?= M2DyW|czNzl4IHi= MljhZ4F2e2W|IHPlcIwh[3mlbHWgZZJz\XO2 M3OyVlIyOjl7OE[y
MMQ MlHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrFb5UxNjByOD22NlUhdk1? Ml3aO|IhcA>? NH20WGpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKHSrbXWtJIFv\CCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NF[1PHAzODdyMEe1OS=>
MMQ M33ROmZ2dmO2aX;uJGF{e2G7 M3jJcFAvODB6LU[yOUBvVQ>? NVzsb41JPzJiaB?= M1nMNolvcGmkaYTzJHBTVCC|ZXPy[ZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MonHNlA4ODB5NUW=
MMQ MkXUSpVv[3Srb36gRZN{[Xl? Mn3FNE4xPC14MkWgcm0> MWW3NkBp NUP6UG9wcW6qaXLpeJMhTVMQsTDlfJBz\XO|aX;u MnKyNlA4ODB5NUW=
MMQ M{PpbWZ2dmO2aX;uJGF{e2G7 NFXZcogxNjB2LU[yOUBvVQ>? NF7vW|I4OiCq NHnYT3J2eHKnZ4XsZZRmeyCWR1dOtlMh[W6mIGTHSu6zWkmLIHX4dJJme3Orb36= MVuyNFcxODd3NR?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
MDM2 / ER; 

PubMed: 24747123     


MCF7 (A) and T47D (B) cells were cultured in the presence of different concentrations of fulvestrant (Fulv) for 66 h. ER and MDM2 were detected by Western blot and normalized to β-actin. The decrease in protein expression (shown relative to vehicle control treatment) after fulvestrant treatment was calculated for each drug concentration. *P < 0.05 compared to vehicle control treatment. 

p-ErbB3 Y1289 / ErbB3 / p-ErbB4 Y1056 / ErbB4 / p-AKT / AKT / p-ERK / ERK; 

PubMed: 21396094     


Western blots showing the effect of increasing concentrations of heregulin β1 (HRGβ1) (0.1 to 10 ng/ml for five minutes) on total and phosphorylated ErbB3, ErbB4, AKT and extracellular signal-regulated kinases 1 and 2 (ERK1/2) protein expression in MCF-7 and T47D cells, maintained for 7 days in the presence of either fulvestrant (100 nM) of vehicle control (ethanol). 

ErbB3; 

PubMed: 23999432     


Immunofluorescence of ErbB3 in cells cultured for 24 hours with or without fulvestrant. 

ERα; 

PubMed: 19815064     


Breast cancer cells were treated with different doses of ICI for 3 hours. The expression levels of ERα and actin were assayed by Western blot using anti-ERα and anti-actin antibodies.

24747123 21396094 23999432 19815064
Immunofluorescence
IGF-1R / Erα; 

PubMed: 19815064     


Confocal microscope study of fulvestrant-induced ERα and IGF-1R co-localization on the cell membrane in non-permeabilized condition. Cells were starved in 1% DCC medium for 24 hr and then treated with either vehicle (left) or ICI at 100 nM (right) for 15 min. Treated cells were fixed in 4% formaldehyde and stained with mouse monoclonal anti-IGF-1R antibody (a), rabbit polyclonal anti-ERα antibody (b), or nuclear staining with DAPI (c). The merged images are shown in d. Scale bar = 20 μm.

Snail / E-cadherin ; 

PubMed: 23936773     


E-cadherin and Snail protein localization in MCF-7 cells 48 h after treatment of cells with E2 and the tested agents. C: control (untreated cells); E2: cells treated with 17β-estradiol; Fulv: cells treated with E2 + 100 nM Fulv. The image is representative of three independent experiments using a magnification of 63X.

19815064 23936773
Growth inhibition assay
Cell viability; 

PubMed: 29787591     


MTT assay of MCF-7 cells treated with various concentration of fulvestrant. Statistically significant reduced the % viability in MCF-7 cells (One-way ANOVA; ****p < 0.0001).

29787591
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):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
0.4mg/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
储存条件 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
NCT04024436 Not yet recruiting Metastatic Breast Cancer|FGFR2 Amplification Taiho Oncology Inc. August 30 2019 Phase 2
NCT03854903 Recruiting Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer Georgetown University|Pfizer April 1 2019 Phase 1
NCT03584009 Recruiting Estrogen Receptor-positive (ER+)/Human Epidermal Growth Factor Receptor (HER2)-Negative Locally Advanced or Metastatic Breast Cancer Hoffmann-La Roche September 6 2018 Phase 2
NCT03393845 Recruiting Breast Cancer Nancy Chan MD|Merck Sharp & Dohme Corp.|Big Ten Cancer Research Consortium January 29 2018 Phase 2
NCT03363893 Recruiting Advanced Solid Malignancies Carrick Therapeutics Limited November 14 2017 Phase 1|Phase 2
NCT03294694 Recruiting Metastatic Hormone-Receptor-Positive (HR+) Breast Cancer|HER2-Negative Breast Cancer|Metastatic Epithelial Ovarian Cancer Dana-Farber Cancer Institute|Novartis October 18 2017 Phase 1

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

相关Estrogen/progestogen Receptor产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID