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71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 NX3F[VlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LwSVEvOy1zMECwJI5O M3HWeVQ5KGh? NVXUUY95cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MUKyOFk4QTJ7NB?=
MCF-7/LTED NVPJXoc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[xMlMuOTByMDDuUS=> NVLNdYhOPDhiaB?= NW\KVo9jcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHOxZZczPDl5OUK5OC=>
HCC1428 M1Hqfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzoWmcyNjNvMUCwNEBvVQ>? MVS0PEBp MXHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mke5NlQ6Pzl{OUS=
HCC1428/LTED MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fjXVEvOy1zMECwJI5O NWrDfpR[PDhiaB?= MV\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHrifnAzPDl5OUK5OC=>
LCC1 M1XvN2Z2dmO2aX;uJGF{e2G7 MYSxNFAhdk1? M370OVQ5NTF2NDDo M373eIFkfGm4YYTld{BWWFJic3nncoFtcW6p NUnQR|Q4OjR6NUiyO|c>
LCC9 MX7GeY5kfGmxbjDBd5NigQ>? NIXZS3AyODBibl2= NGH3cYk1QC1zNESgbC=> NI\teWZi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= MY[yOFg2QDJ5Nx?=
MCF-7  MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\ZNVAxKG6P NIToeI82KGR? NWH2UYZucW6qaXLpeJMh[2WubDDndo94fGhidH:gNVDwxIV? MmW5NlQ5OTl3NUC=
mesangial  MlfBSpVv[3Srb36gRZN{[Xl? M3fFTVAvOS1zMECgcm0> NVn6THlGPDhiaB?= MUnzeZBxemW|c3XzJHRITi4QskGtbY5lfWOnZDD0fZBmKEmYIHPvcIxi\2Ww NHTOUFMzPDd7M{[zPS=>
Mesangial NVLXdVdiTnWwY4Tpc44hSXO|YYm= MlH6NE4yNTFyMDDuUS=> MVmwMlUhcA>? MoTLbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIGPtZYQzKHCqb4PwbI9zgWyjdHnvckB3cWFiR2DFVi=> M{m3b|I1Pzl|NkO5
ER+ MCF-7/2a M3jOZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX5b4Q{UUN3ME2wMlAxPCEQvF2= M1uyVVE2OzJ2OEi0
ER+ MCF-7 MlnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Xv[VIxOCCq NYr4RphvUUN3ME2wMlIyKG6P Mn\nNVU{OjR6OES=
MCF-7  MV7GeY5kfGmxbjDBd5NigQ>? MYOxNOKhdk4EoB?= MkmzO|IhcA>? M4H6NZJmfmW{c3XzJJRp\SCnc4Tyc4dmdiCnZn\lZ5QpUUN3MDCxMlkhy5diMUFijLI6KE1r Mn71NlQ6ODh4NUK=
MCF-7  NFT3OmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGq3N5dKSzVywrDv[kBieHC{b4jpcYF1\Wy7IEKgcm0> MmPGNlM1PDh|NE[=
H1975  MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYmzxsDPxE1? MU[xJI0> NYDiS3RLcW6lcnXhd4V{KHSqZTDn[YZqfGmwaXKgd4Vve2m2aY\peJkhd2ZiSEG5O|Uh[2WubIRCpC=> NUTTS|JkOjR{Nki4NVA>
H1975 M3z2cGZ2dmO2aX;uJGF{e2G7 NYrXUJN2O8LizszN M{PKcVEhdQ>? M{LFRpVxemWpdXzheIV{KHSqZTDs[ZZmdCCxZjDM[ZQuP2N? MXGyOFI3QDhzMB?=
MCF-7  NWTaNFF1TnWwY4Tpc44hSXO|YYm= M{PrUFExOOLCiX7NxsA> MoHvO|IhcA>? NX3TfGZ7emW4ZYLz[ZMhfGinIIDyc5Rm[3SrdnWg[YZn\WO2IH;mJGUzyqCrbjDj[YxtKGmwdnHzbY9v M17QUFI{QTN4N{ez
MCF-7  M4PocmZ2dmO2aX;uJGF{e2G7 MkD1NVAx6oDLbl5CpC=> Mn7sNlQwPDhiaB?= NIOxZ4Zn[WOrbHn0ZZRmeyCrbo\hd4lwdiC2aILveYdpKE2PUIOnJI1w\HWuYYTpc44> MY[yN|k{Pjd5Mx?=
BT474-tet-shMED1 MnjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1OweVAvOS13IN88US=> NXvRSWEyPyCm NVnQcVhlcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Mn2wNlM6OzZ{M{S=
ZR75-1-tet-shMED1  M17oNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLWfpJXOC5zLUWg{txO Mn7hO{Bl MX3pcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NEXNbY0zOzl|NkKzOC=>
MCF-7-tet-shMED1 MkXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPqNE4yNTVizszN MljzO{Bl MmjDbY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ Moj5NlM6OzZ{M{S=
HepG2  NUXIcYR[TnWwY4Tpc44hSXO|YYm= NGm3WHkxNjBzLUGwJO69VQ>? Ml\tNVghcMLi MkTmZYN1cX[jdHXzJJRp\SCHUlWtcYVlcWG2ZXSgeJJidnOlcnnweIlwdiCxZjDBSlJGWg>? MX:yN|c{OzF6OB?=
MCF-7L  NVTaOVJyTnWwY4Tpc44hSXO|YYm= NX;kb|VUOTByIH7NxsA> M1rjc|ExKG2rbj:yOEBpNzR6IHi= NFm2SG1z\XO3bITzJIlvKEWJRmKsJGhGWjJiYX7kJGhGWjNicHjvd5Bpd3K7bHH0bY9vKGG2IIDyc4xwdmenZDDlfJBwe3W{ZR?= MYWyN|Y5PjRzNh?=
MCF-7L  M3PPbWZ2dmO2aX;uJGF{e2G7 NIr0NXoyODBibl5CpC=> NVjKVHd5PDhiaB?= MVHpcoR2[2W|IIXwdoVofWyjdHnvckBw\iCvUl7BJI9nKEWJRmKgcIlo[W6mIFjCMWVITg>? MWSyN|Y5PjRzNh?=
MCF-7L MljYSpVv[3Srb36gRZN{[Xl? M4TWdlExOCCwTdMg M3LuW|Q5KGh? MVvpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT M{jGUlI{Pjh4NEG2
C4-12  MmfZSpVv[3Srb36gRZN{[Xl? NETENmYyODBibl5CpC=> NGDKVGk1QCCq NG[ydmNqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU NFGxdVAzOzZ6NkSxOi=>
MCF-7L Mk\xSpVv[3Srb36gRZN{[Xl? NHOzVXIyODBibl5CpC=> MWeyOEBp M3LOU4lv\HWlZYOgSWdHWiCyaH;zdIhwenmuYYTpc44hemWzdXny[YQhUEJvRVfGJIZ2dmO2aX;u NV\IfZBROjN4OE[0NVY>
MMQ  MXjGeY5kfGmxbjDBd5NigQ>? MnjaNE03OjVibl2= MmDJO|IhcA>? NIDoOYhld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDld5Rzd2enbjDy[YNmeHSxcj5OtUApTVMQsTm= NUfKOm9wOjN3MkOzOVc>
H1975  MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XRWVAvOzF{NT2xNEDPxE1? M3L1ZlYh\A>? MkfxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mm\pNlM{QTl7NUe=
H1975  MWDBdI9xfG:|aYOgRZN{[Xl? M3XH[FIxOCCwTR?= NWTGU|B5PzJiaB?= MojL[Y5p[W6lZYOg[ZJtd3SrbnniJIlv\HWlZXSgZZBweHSxc3nz MXKyN|M6QTl3Nx?=
MCF-7  MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\4fFExNzFyMD:xNFAxKG6P MWCyM|QwPiCm NWXE[ItvTE2VTx?= MkLObY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEBld3OnLTDhcoQhfGmvZT2g[IVx\W6mZX70JI1idm6nch?= NFLRUo0zOzNzM{WwOi=>
MCF-7  MnzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWOxNFAhdk1? M1j4Z|Qh\A>? MYrEUXNQ M1LmZolv\HWlZYOgZUBpcWeqZYKgdJJweG:{dHnvckBw\iClZXzsd{BqdiC2aHWgS|EheGijc3ZCpC=> MYOyN|MyOzVyNh?=
MLO-Y4  MoDpSpVv[3Srb36gRZN{[Xl? MYexxsDPxE1? MmPUNUBp M4Xn[IlvcGmkaYTzJGUzNWmwZIXj[YQhS3h2MzDlfJBz\XO|aX;u M1y5dVI{OjR5MEW3
MCF-7 NYO1b21[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYmxNFAhdk1? MoHROFghcA>? MY\hZpJw\2G2ZYOgeIhmKHC{b3zp[oVz[XSrdnWg[YZn\WO2IH;mJI1w\GW{YYTlJI5qfHKxc3H0bZZmKHO2cnXzdy=> NVXPNnFqOjN{MU[3OFQ>
TG1-1  MXTGeY5kfGmxbjDBd5NigQ>? NIW2TlYyyqEQvF2= M3fXV|I1KGh? M4nmVYFjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhUEmILUJOtS=> Ml;RNlMxQDh4MEe=
TG1-1  NV;rdW1pTnWwY4Tpc44hSXO|YYm= MWWxxsDPxE1? NWGweXNvOjRiaB?= Mmf4ZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBRUTON M{HLTVI{ODh6NkC3
MCF7 NGDNZXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fvS|ExOCCwTR?= NW\RWHVsPDhiaB?= NVjmXoI{dGWjZIOgeI8h[SC|aX3pcIFzKGyxc4OgbY4he3W{dnn2ZYwh[XNid3n0bEBld3ixcoXibYNqdiCjbH;u[S=> M2LL[VI{ODd5MkS5
MCF7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWxNFAhdk1? M3qze|Q5KGh? NIXYN5BmdmijbnPld{BvfXSuaX6tcYVlcWG2ZXSgZ4VtdCCmZXH0bC=> Ml\pNlMxPzd{NEm=
MCF-7  NH31VVhHfW6ldHnvckBCe3OjeR?= NVPOfWR6PiCq NYXCRnRJTE2VTx?= MnfNZZR1\W63YYTld{B1cGViZnz1[IlwgG:waXytJI9zKG[nbnjlfIFucWRvaX7keYNm\CCrbnPy[YF{\SCrbjDtbXIuOjFiZYjwdoV{e2mxbh?= MUSyN|A2OjB|Nh?=
MCF-7 NHezfHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rZZVExOCCwTT:xJO69VQ>? M4fwRlUh\A>? MkHxbY5pcWKrdIOgeIhmKHO2aX31cIF1cW:wIH;mJFE4|rJvZYP0doFlcW:u M1ezNFIzQTh{N{[1
MCF-7 MnPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnZXYEyODBibl2= M1TsTlUh\A>? MVXpcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[g[pV{[XKrZXzpckBJ M13tc|IzQTh{N{[1
1471.1 NHftS2tHfW6ldHnvckBCe3OjeR?= MofyNVAxKG6P MXexJIg> M3LsXGV1V0kEoB?= NUjyfox{fGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv NGTlXVQzOjh4OUGwOi=>
MCF-7 NVi2fVhFTnWwY4Tpc44hSXO|YYm= M1rmV|ExOCCwTR?= MkXJNUBp NYK4[FhZTXSRSNMg NUSwc4ZSfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv NHza[IUzOjh4OUGwOi=>
HeLa MkPnSpVv[3Srb36gRZN{[Xl? M2D0bFExOCCwTR?= NVT6dppjOSCq NX\DOIF1TXSRSNMg NF7ZVWJ1[WunczDvckBiKHC3bnP0ZZRmKHO2YXnubY5oKHCjdITldo4> M33QVlIzQDZ7MUC2
COS-7  NEDSSYdHfW6ldHnvckBCe3OjeR?= MWGxNFAhdk1? MX[xJIg> NXvDTmd1TXSRSNMg M1G5NJRic2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=> MX:yNlg3QTFyNh?=
BG1L-OHTLT  NXrhOolsTnWwY4Tpc44hSXO|YYm= NIrEcG8yOMLibl2= M4HH[VI1yqCqwrC= NFvhPY1qdmirYnn0d{BGWs7zIHX4dJJme3Orb36= MV[yNlY2OjV3OB?=
BG1L-ICILT NVnhVWVUTnWwY4Tpc44hSXO|YYm= MVixNOKhdk1? NEnGWmMzPMLiaNMg MXLpcohq[mm2czDFVu6yKGW6cILld5Nqd25? NGq4XFczOjZ3MkW1PC=>
PC-9 NH7wRVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHnNE4xODNvM{Cg{txO MUC0PEBp NEDtRmFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NI\2Z2MzOjV4ME[zOC=>
H1650 M1nMSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nDXFAvODB|LUOwJO69VQ>? NV;0WJBWPDhiaB?= MkfjbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> Mnj3NlI2PjB4M{S=
H1975 M{f3dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzj[ZIxNjByMz2zNEDPxE1? MXq0PEBp M2XiNIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWKyNlU3ODZ|NB?=
H1975 MlvVSpVv[3Srb36gRZN{[Xl? MoC0N:Kh|ryP MlHUN{Bp MlfxZYJzd2ejdHXzJJRp\SCyaH;zdIhwNUWJRmKgbY5lfWO2aX;uJIJ6KGW|dILv[4Vv NEnrbpMzOjV4ME[zOC=>
H1975 NFTKdoJHfW6ldHnvckBCe3OjeR?= MXuzxsDPxE1? M1ew[|ch\A>? M4W0Uolv\HWlZYOgSWdHWiCneIDy[ZN{cW:w NX7SZ5hDOjJ3NkC2N|Q>
HTR-8 NXm0XlI2TnWwY4Tpc44hSXO|YYm= NYXycpNvOcLizszN M{\0Z|EuPDhiaB?= NUPP[FFb\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gTWdHSlB5IH3SUmE> MXuyNlM5OzFzMR?=
JEG-3 Ml7GSpVv[3Srb36gRZN{[Xl? M3;F[VHDqM7:TR?= M{nGZlEuPDhiaB?= MUnkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCLR1\CVFchdVKQQR?= MVWyNlM5OzFzMR?=
Huh7 M3SzV2Z2dmO2aX;uJGF{e2G7 MYm1NOKh|ryP NVfCV3BJPDhiaB?= MXLpcohq[mm2czDn[Y5qe3SnaX6tcYVlcWG2ZXSgVG9POSC2cnHud4FkfGm4YYTpc44> Mlf4NlI{ODR{OU[=
201T MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnvbIdYPSEQvF2= MX[3NkBp MoG0bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueTDjc41jcW6nZDD3bZRpKH[jbnTleIFvcWJ? M4n1clIzOjV6NEe2
A549  NFj2V29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TjdVUh|ryP NEn5TnY4OiCq NELldZBqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnHu[IV1[W6rYh?= NVroZ3ppOjJ{NUi0O|Y>
MCF-7 MVrGeY5kfGmxbjDBd5NigQ>? NHTLOoQyyqEQvF2= NHXQbmMzPCCqwrC= NVjHRoh4\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi NYX6b4tqOjJyNEmzNVY>
HCC-1428 M1PBZmZ2dmO2aX;uJGF{e2G7 MoDoNeKh|ryP Mn[2NlQhcMLi M2P6fIRwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvckBqdmS3Y3XkJIJ6KDRvT1itWEDDqA>? NV64cpZrOjJyNEmzNVY>
MDA-361 MXHGeY5kfGmxbjDBd5NigQ>? NWnWZYNFOcLizszN M{nKTFI1KGkEoB?= MoHx[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh NXH3XW44OjJyNEmzNVY>
ZR75-1 NWLMTGpKTnWwY4Tpc44hSXO|YYm= Ml23NeKh|ryP NFuyfZYzPCCqwrC= NHHXeFlld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? Ml71NlIxPDl|MU[=
MCF-7 NH3NUI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLnNeKh|ryP MXi1MVExKGR? M13hOpN2eHC{ZYPz[ZMhTTJvaX7keYNm\CCpcn;3eIghcW6qaXLpeIlwdg>? M1;GXVIzODR7M{G2
HCC-1428 NYPnWGlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVexxsDPxE1? MWq1MVExKGR? NEGzbpd{fXCycnXzd4V{KEV{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? NFLSPJAzOjB2OUOxOi=>
MDA-361 MlPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmxxsDPxE1? M37QXlUuOTBiZB?= NEDSZlN{fXCycnXzd4V{KEV{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? MXSyNlA1QTNzNh?=
ZR75-1 M{foT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjHNeKh|ryP NGPYS2U2NTFyIHS= MVHzeZBxemW|c3XzJGUzNWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44> MW[yNlA1QTNzNh?=
MCF-7/AC-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\Hc5FGOC1yLkKg{txO MVK2JIQ> M4XWc4lvcGmkaYTzJINmdGxiZ4Lve5RpKG2xZHXzeIx6 NHHOfZMzOjB2Mke5Ni=>
MCF7 NUjKPFlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPwNVAhyrWP NXHHVXh2PDhiaB?= NFTxOWFqdmS3Y3XzJINmdGxiaX7obYJqfGmxbjD3bIlkcCClYX6gZoUh\W6qYX7j[YQh[nliZnnido9jdGG|dIO= NVT5UI43OjJyNEG4PFc>
MMQ MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVKwMVYzPSCwTR?= M1XNRlczKGh? M1juRpBzd2S3Y3XzJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd28EoB?= NInzWpMzOjBzNUGwNS=>
MMQ MmjTSpVv[3Srb36gRZN{[Xl? MnnPNE03OjVibl2= NHK5O4k4OiCq NXjYXohSeHKxZIXj[ZMh[SC|dHH0bZN1cWOjbHz5JJNq\26rZnnjZY51NCCmb4PlMYRmeGWwZHXueEBz\WS3Y4Tpc44hcW5iUGLMJJNm[3KndHnvci=> NWjEPG9GOjJyMUWxNFE>
MCF7 MoewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTQRlBuOC1zIN88US=> MlntNlQuOTJyIHi= Moj5bY5pcWKrdIOgeIhmKGe{b4f0bEBw\iCPQ1[3MXlDNTIEoB?= MnO2NlE5PjN{NUi=
HepG2 M3zlWmFxd3C2b4Ppd{BCe3OjeR?= MVWwMlHDqM7:TR?= MWWyOEBp M2TjZ4Fjd2yrc3jld{B1cGViZYP0do9o\W5vaX7keYNm\CC3cD3y[Yd2dGG2aX;uJI9nKGGyb1HJJIFv\CCjcH;N M{HXRlIyQDF4MkOz
MCF7–iFR3 Mkn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[yNE0yODBibl2= MnLkPVYhcA>? MlHT[Y5p[W6lZYOgRXAucW6mdXPl[EBk\WyuIHfyc5d1cCCrbnjpZol1cW:w MXSyNVc6Ojh6OR?=
MCF7S Mn\JSpVv[3Srb36gRZN{[Xl? NEHXZZYyyqEQvF2= NYnSSJNnPDhiaB?= M33jeIRwf26{ZXf1cIF1\XNib4\ldoFtdCCHUt8xJJBzd3SnaX6gcIV3\Wy| Mmr5NlE2OzNzOUW=
MCF7 NEjLR5hHfW6ldHnvckBCe3OjeR?= MVixxsDPxE1? M4DJPVQ5KGh? NWPXN21D\G:5boLl[5Vt[XSnczDveoVz[WyuIFXS{tEheHKxdHXpckBt\X[nbIO= NUPMUHBtOjF3M{OxPVU>
MCF7S NGXCXXpHfW6ldHnvckBCe3OjeR?= MonvNeKh|ryP MVW3JIQ> M1fPeIF1fGWwdXH0[ZMhfHWvb4LzdIhmemViZn;ycYF1cW:wIHHu[EBxem:uaX\ldoF1cW:w M4O4flIyPTN|MUm1
MCF7S NIXLTHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUT1d2VEOC53L{Gg{txO NX7nPZZbPyCm NIHoeYxFVVOR MUHk[YNz\WG|ZYOgZ4VtdCCneIDhcpNqd25? MnPQNlE2OzNzOUW=
T47D  MoDHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV33[FJnPCCwTR?= M2LVWVQxKGh? MV\zeZBxemW|c3XzJINmdGxiZ4Lve5RpKG2xZHXyZZRmdHl? NVLrZlhQOjF2OECzPVE>
BT474  NYHpNmNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWe0JI5O M1;j[|QxKGh? MmPFd5VxeHKnc4Pld{Bk\WyuIHfyc5d1cCCvb3TldoF1\Wy7 M{PsRVIyPDhyM{mx
T47D  NGPEPGFHfW6ldHnvckBCe3OjeR?= NV7uXW9jOTBibl2= MlnWOFAhcA>? Mmm4[I94dnKnZ4XsZZRmeyCHUt8xJJBzd3SnaX6= NUn4c2ZEOjF2OECzPVE>
BT474  Mn21SpVv[3Srb36gRZN{[Xl? NF;LVZYyOCCwTR?= MXW0NEBp NXfkPGlI\G:5boLl[5Vt[XSnczDFVu6yKHC{b4TlbY4> NITobVIzOTR6MEO5NS=>
MCF7 M1vT[WZ2dmO2aX;uJGF{e2G7 NWm2XHJ2OTByIH7N M{TyTlch\A>? M2fVb5Jm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> MUeyNVM6PjB7NB?=
T47D  NVnCNm8xTnWwY4Tpc44hSXO|YYm= NVvxcoRrOTByIH7N NUfyNHpuPyCm NFTYRYZz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6 MYmyNVM6PjB7NB?=
BT474  NUm0[nh5TnWwY4Tpc44hSXO|YYm= MnXRNVAxKG6P M1LMUFch\A>? NW[1Ro1CemWmdXPld{BGWs7zIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? NULnXnJmOjF|OU[wPVQ>
MDAMB361 M2TQZWZ2dmO2aX;uJGF{e2G7 MmjQNVAxKG6P NVHINIs5PyCm MlzDdoVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> M{PPVVIyOzl4MEm0
MCF7 NYnSfWI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXJNE4xOS1zIN88US=> MXq3JIQ> Mn;VdoVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NYLIXYl5OjF|OU[wPVQ>
T47D  M2rWSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrsW5hnOC5yMT2xJO69VQ>? NXfVfmU6PyCm NXLDUXV1emWmdXPld{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NX31UXgyOjF|OU[wPVQ>
BT474  NV60Z4xmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLIZmsxNjBzLUGg{txO NGTxZmw4KGR? MVry[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? MYGyNVM6PjB7NB?=
MDAMB361 Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vRT|AvODFvMTFOwG0> M{f6TFch\A>? MVLy[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? MlPpNlE{QTZyOUS=
MCF7 MXzGeY5kfGmxbjDBd5NigQ>? NYPxO|AzOTByIH7N MWm3JIQ> NUPnV5JicW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=> MmXDNlE{QTZyOUS=
T47D  M1[yNmZ2dmO2aX;uJGF{e2G7 MljZNVAxKG6P NFu0b5A4KGR? NYXvUG43cW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=> MV:yNVM6PjB7NB?=
BT474  NGXUeFRHfW6ldHnvckBCe3OjeR?= NF3BdHcyODBibl2= MUG3JIQ> Ml;EbY5lfWOnczDv[kBGemKEMzDhcoQhTXKkQkSgdoVk\XC2b4Kg[ZhxemW|c3nvckBidmRic3nncoFtdGmwZx?= MlXiNlE{QTZyOUS=
MDAMB361 MmXSSpVv[3Srb36gRZN{[Xl? NY\2SFV1OTByIH7N MXy3JIQ> MVPpcoR2[2W|IH;mJGVz[kJ|IHHu[EBGemKENDDy[YNmeHSxcjDlfJBz\XO|aX;uJIFv\CC|aXfuZYxtcW6p NHLQdoQzOTN7NkC5OC=>
MCF7 M{PIeGZ2dmO2aX;uJGF{e2G7 MnPQNVAhdk1? MljHPVYhcA>? NIXLUVBld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc47DqA>? NUfkR5RiOjF|N{izN|M>
MDA-MB-231 M2LHXmZ2dmO2aX;uJGF{e2G7 NGTR[GYyOCCwTR?= NG[0RVI6PiCq MYXkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb39CpC=> MYKyNVM4QDN|Mx?=
SK-BR-3 NUm2[mFiTnWwY4Tpc44hSXO|YYm= MWqxNEBvVQ>? NHXNTGk6PiCq MVvkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb39CpC=> MYqyNVM4QDN|Mx?=
MCF-7 NXTRT|BCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrsfYtnOTByIH7N MX:3Nk86PiCq M4SzTINifXOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NIXoV3kzOTJ7OUi2Ni=>
MMQ NYPwUm44T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnX1NE4xODhvNkK1JI5O NXLMVIdsPzJiaB?= MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M37GSVIxPzByN{W1
MMQ M4\xTmZ2dmO2aX;uJGF{e2G7 NFnoRnUxNjByOD22NlUhdk1? MorEO|IhcA>? M376dolvcGmkaYTzJHBTVCC|ZXPy[ZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3\GW|IxPzByN{W1
MMQ MnzZSpVv[3Srb36gRZN{[Xl? NFzBN3ExNjB2LU[yOUBvVQ>? MnTUO|IhcA>? MofDbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w MYKyNFcxODd3NR?=
MMQ M3iycWZ2dmO2aX;uJGF{e2G7 Mk\sNE4xPC14MkWgcm0> Ml32O|IhcA>? M4XYS5VxemWpdXzheIV{KFSJRt8yN{BidmRiVFfG{tJTUUliZYjwdoV{e2mxbh?= MV[yNFcxODd3NR?=

... 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]
- 合并
  • 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]
- 合并
  • 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 粉状
溶于溶剂
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 (mg) = 浓度 (mM) x 体积 (mL) 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04024436 Not yet recruiting Drug: TAS-120|Drug: Fulvestrant Metastatic Breast Cancer|FGFR2 Amplification Taiho Oncology Inc. August 30 2019 Phase 2
NCT03854903 Recruiting Drug: Palbociclib|Drug: Bosutinib|Drug: Fulvestrant 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 Drug: Venetoclax|Drug: Fulvestrant 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 Drug: Pembrolizumab|Drug: Fulvestrant Breast Cancer Nancy Chan MD|Merck Sharp & Dohme Corp.|Big Ten Cancer Research Consortium January 29 2018 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