Fulvestrant

For research use only. Not for use in humans.

目录号:S1191 别名: ICI-182780, ZD 9238 中文名称:氟维司琼

Fulvestrant Chemical Structure

CAS No. 129453-61-8

Fulvestrant (ICI-182780, ZD 9238)是一种Estrogen receptor(ER)拮抗剂, 无细胞试验中IC50为0.094 nM。Fulvestrant还可诱导自噬和凋亡并具有抗肿瘤的活性。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 647.01 现货
RMB 567.34 现货
RMB 2233.34 现货
RMB 7289.1 现货
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客户使用Selleck生产的Fulvestrant发表文献90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 (ICI-182780, ZD 9238)是一种Estrogen receptor(ER)拮抗剂, 无细胞试验中IC50为0.094 nM。Fulvestrant还可诱导自噬和凋亡并具有抗肿瘤的活性。
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 NHH6OHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nRblEvOy1zMECwJI5O NUnydJpsPDhiaB?= MVrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NF\NeYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3PVI6PCd-MkS5O|kzQTR:L3G+
MCF-7/LTED MleyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXqxMlMuOTByMDDuUS=> NGLscYs1QCCq MoXmbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHS5U2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3PVI6PCd-MkS5O|kzQTR:L3G+
HCC1428 M13xWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFj0e2UyNjNvMUCwNEBvVQ>? NFzoVmY1QCCq MUnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFjvUnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3PVI6PCd-MkS5O|kzQTR:L3G+
HCC1428/LTED M{fke2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvmNU4{NTFyMECgcm0> M2\ETVQ5KGh? NGX2U29qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{XDdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUe5Nlk1Lz5{NEm3PVI6PDxxYU6=
LCC1 NVfYPZJ[TnWwY4Tpc44hSXO|YYm= MXexNFAhdk1? MWC0PE0yPDRiaB?= M2DwS4FkfGm4YYTld{BWWFJic3nncoFtcW6p NISw[JY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi1PFI4Pyd-MkS4OVgzPzd:L3G+
LCC9 NEDCdplHfW6ldHnvckBCe3OjeR?= MmDyNVAxKG6P NInCWpQ1QC1zNESgbC=> MXjhZ5RqfmG2ZYOgWXBTKHOrZ37hcIlv\w>? MmPvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6NUiyO|coRjJ2OEW4Nlc4RC:jPh?=
MCF-7  NE\D[ZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6xNFAhdk1? NWHUc5cxPSCm MU\pcohq[mm2czDj[YxtKGe{b4f0bEB1dyBzMP-8iS=> M3HZcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEG5OVUxLz5{NEixPVU2ODxxYU6=
mesangial  NUnQOXBGTnWwY4Tpc44hSXO|YYm= MYmwMlEuOTByIH7N NHTtfHU1QCCq MoDVd5VxeHKnc4Pld{BVT0ZvzsKxMYlv\HWlZXSgeJlx\SCLVjDjc4xt[Wenbh?= M4TubVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{mzOlM6Lz5{NEe5N|Y{QTxxYU6=
Mesangial MYTGeY5kfGmxbjDBd5NigQ>? MWewMlEuOTByIH7N NVLKW5RCOC53IHi= NYC1UGt3cW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJHNu[WR{IIDoc5NxcG:{eXzheIlwdiC4aXGgS3BGWg>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd7M{[zPUc,OjR5OUO2N|k9N2F-
ER+ MCF-7/2a NVjLO3lWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYqyfYNbUUN3ME2wMlAxPCEQvF2= NVrjTINZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWzNlQ5QDRpPkG1N|I1QDh2PD;hQi=>
ER+ MCF-7 Ml;wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDkTmV3OjByIHi= NFnHV|lKSzVyPUCuNlEhdk1? MlzBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV|MkS4PFQoRjF3M{K0PFg1RC:jPh?=
MCF-7  MYPGeY5kfGmxbjDBd5NigQ>? MUWxNOKhdk4EoB?= MU[3NkBp NGH4Oldz\X[ncoPld{B1cGViZYP0do9o\W5iZX\m[YN1MEmFNUCgNU46KMPZIEGw5qiTQSCPKR?= M4n3elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC4OlUzLz5{NEmwPFY2OjxxYU6=
MCF-7  NHH6fJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGftTXFKSzVywrDv[kBieHC{b4jpcYF1\Wy7IEKgcm0> MmDLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEizOFYoRjJ|NES4N|Q3RC:jPh?=
H1975  NV:3blk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXzNXE{yqEQvF2= MnixNUBu MoW3bY5kemWjc3XzJJRp\SCpZX\peIlvcWJic3Xud4l1cX[rdImgc4YhUDF7N{WgZ4VtdHQEoB?= NHXKOoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK2PFgyOCd-MkSyOlg5OTB:L3G+
H1975 NXXWVXplTnWwY4Tpc44hSXO|YYm= NFLkNHE{yqEQvF2= M4HTPVEhdQ>? MVX1dJJm\3WuYYTld{B1cGVibHX2[Ywhd2ZiTHX0MVdk Mo\HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{Nki4NVAoRjJ2Mk[4PFExRC:jPh?=
MCF-7  MWDGeY5kfGmxbjDBd5NigQ>? NHHVfncyODEkgJnuUeKh MlvhO|IhcA>? NVXMOVM{emW4ZYLz[ZMhfGinIIDyc5Rm[3SrdnWg[YZn\WO2IH;mJGUzyqCrbjDj[YxtKGmwdnHzbY9v NWLyflg1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|Y4PzNpPkKzPVM3Pzd|PD;hQi=>
MCF-7  NFPqeIxHfW6ldHnvckBCe3OjeR?= M4W0XFExOOLCiX7NxsA> NV20NXJPOjRxNEigbC=> MXjmZYNqdGm2YYTld{Bqdn[jc3nvckB1cHKxdXfoJG1OWHNpIH3v[JVt[XSrb36= Ml\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{[3O|MoRjJ|OUO2O|c{RC:jPh?=
BT474-tet-shMED1 NFL5eVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPJXHB7OC5zLUWg{txO M17wTlch\A>? NHfje4pqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= Mof6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{[yN|QoRjJ|OUO2NlM1RC:jPh?=
ZR75-1-tet-shMED1  M{D0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\GWlQxNjFvNTFOwG0> NEP2UYI4KGR? NYPre3VYcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MnTUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{[yN|QoRjJ|OUO2NlM1RC:jPh?=
MCF-7-tet-shMED1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfmU5UxNjFvNTFOwG0> MmTrO{Bl Mn3LbY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|NkKzOEc,OjN7M{[yN|Q9N2F-
HepG2  M1LEbGZ2dmO2aX;uJGF{e2G7 M17n[|AvODFvMUCg{txO M17tPVE5KGkEoB?= NUHzSo1j[WO2aY\heIV{KHSqZTDFVmUudWWmaXH0[YQhfHKjboPjdolxfGmxbjDv[kBCTjKHUh?= NX\jS3hFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3N|MyQDhpPkKzO|M{OTh6PD;hQi=>
MCF-7L  MmnRSpVv[3Srb36gRZN{[Xl? M1zCVVExOCCwTdMg NXf2[2E4OTBibXnuM|I1KGhxNEigbC=> MXTy[ZN2dHS|IHnuJGVITlJuIFjFVlIh[W6mIFjFVlMheGixc4Doc5J6dGG2aX;uJIF1KHC{b3zvcodm\CCneIDvd5Vz\Q>? Mn[2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4OE[0NVYoRjJ|Nki2OFE3RC:jPh?=
MCF-7L  NF\Te2hHfW6ldHnvckBCe3OjeR?= M2\YUVExOCCwTdMg MXi0PEBp NUC4T4JxcW6mdXPld{B2eHKnZ4XsZZRqd25ib3[gcXJPSSCxZjDFS2ZTKGyrZ3Hu[EBJSi2HR1[= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ6NkSxOkc,OjN4OE[0NVY9N2F-
MCF-7L NIDxbI1HfW6ldHnvckBCe3OjeR?= M4HPdlExOCCwTdMg MkOyOFghcA>? NF\4[XRqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ6NkSxOkc,OjN4OE[0NVY9N2F-
C4-12  NIXnZolHfW6ldHnvckBCe3OjeR?= NUPsWXljOTByIH7NxsA> NXnLbGd1PDhiaB?= MnfWbY5lfWOnczDFS2ZTKG[jbXnsfUBu\W2kZYKgZYN1cX[jdHnvckBz\XG3aYLl[EBGWg>? NEmxO|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[4OlQyPid-MkO2PFY1OTZ:L3G+
MCF-7L NITwfoVHfW6ldHnvckBCe3OjeR?= NV3VXZo4OTByIH7NxsA> MkDKNlQhcA>? M1PGSolv\HWlZYOgSWdHWiCyaH;zdIhwenmuYYTpc44hemWzdXny[YQhUEJvRVfGJIZ2dmO2aX;u NEKyRXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[4OlQyPid-MkO2PFY1OTZ:L3G+
MMQ  NVv5WmxCTnWwY4Tpc44hSXO|YYm= NEe3XnYxNTZ{NTDuUS=> MnjtO|IhcA>? NGnh[GRld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDld5Rzd2enbjDy[YNmeHSxcj5OtUApTVMQsTm= NFzIWGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WyN|M2Pyd-MkO1NlM{PTd:L3G+
H1975  Mnu5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnOyNE4{OTJ3LUGwJO69VQ>? MoXLOkBl NITUcZVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NGrOenQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5PVk2Pyd-MkOzPVk6PTd:L3G+
H1975  M{TpNWFxd3C2b4Ppd{BCe3OjeR?= Mnr2NlAxKG6P NUDMR5pSPzJiaB?= MYrlcohidmOnczDldoxwfGmwaXKgbY5lfWOnZDDhdI9xfG:|aYO= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7OUm1O{c,OjN|OUm5OVc9N2F-
MCF-7  NGfEXGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGK4W|kyOC9zMECvNVAxOCCwTR?= NFWwWHczNzRxNjDk MXrEUXNQ NVrZ[4EycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCCmb4PlMUBidmRidHnt[U0h\GWyZX7k[Y51KG2jbn7ldi=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzNzM{WwOkc,OjN|MUO1NFY9N2F-
MCF-7  MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUixNFAhdk1? MljBOEBl NHzIOmhFVVOR M1fmSolv\HWlZYOgZUBpcWeqZYKgdJJweG:{dHnvckBw\iClZXzsd{BqdiC2aHWgS|EheGijc3ZCpC=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzNzM{WwOkc,OjN|MUO1NFY9N2F-
MLO-Y4  MnXJSpVv[3Srb36gRZN{[Xl? NF\LboIyyqEQvF2= MXixJIg> NUWwPIVYcW6qaXLpeJMhTTJvaX7keYNm\CCFeESzJIV5eHKnc4Ppc44> M1rONFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkS3NFU4Lz5{M{K0O|A2PzxxYU6=
MCF-7 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3ub40yODBibl2= NGLCXYM1QCCq M{jnU4Fjem:pYYTld{B1cGVicILvcIln\XKjdHn2[UBm\m[nY4Sgc4YhdW:mZYLheIUhdmm2cn;zZZRqfmVic4Ty[ZN{ M3jNUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkG2O|Q1Lz5{M{KxOlc1PDxxYU6=
TG1-1  NFO2OlZHfW6ldHnvckBCe3OjeR?= MX2xxsDPxE1? NYfwbIZpOjRiaB?= NIfvVJpi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKEiLRj2x{tE> NVXVempQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwPFg3ODdpPkKzNFg5PjB5PD;hQi=>
TG1-1  NX3zSHk1TnWwY4Tpc44hSXO|YYm= MXWxxsDPxE1? M3nKSVI1KGh? NWfkWodY[WK{b3fheIV{KEV{wrDpcoR2[2WmIHHjZ5VufWyjdHnvckBw\iCSSUPL NXXobHNxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOwPFg3ODdpPkKzNFg5PjB5PD;hQi=>
MCF7 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\rNVAxKG6P MYi0PEBp MX3s[YFleyC2bzDhJJNqdWmuYYKgcI9{eyCrbjDzeZJ3cX[jbDDhd{B4cXSqIHTvfI9zfWKrY3nuJIFtd26n MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB5N{K0PUc,OjNyN{eyOFk9N2F-
MCF7 MnPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUixNFAhdk1? NEPQdYs1QCCq MWTlcohidmOnczDueZRtcW5vbXXkbYF1\WRiY3XscEBl\WG2aB?= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB5N{K0PUc,OjNyN{eyOFk9N2F-
MCF-7  MmTXSpVv[3Srb36gRZN{[Xl? MmDvOkBp MXLEUXNQ MVnheJRmdnWjdHXzJJRp\SCobIXkbY95d26rbD2gc5Ih\mWwaHX4ZY1q\C2rbnT1Z4VlKGmwY4LlZZNmKGmwIH3pVk0zOSCneIDy[ZN{cW:w MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB3MkCzOkc,OjNyNUKwN|Y9N2F-
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MCF-7 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2q1blExOCCwTR?= MnG5OUBl M16xNYlvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kBnfXOjcnnlcIlvKEh? NELlbGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mkm4Nlc3PSd-MkK5PFI4PjV:L3G+
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T47D  MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXK0JI5O M3zxV|QxKGh? NH7wSnV{fXCycnXzd4V{KGOnbHyg[5Jwf3SqIH3v[IVz[XSnbIm= NULKU3JyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0PFA{QTFpPkKxOFgxOzlzPD;hQi=>
BT474  MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYW0JI5O MoTLOFAhcA>? NFvJN3p{fXCycnXzd4V{KGOnbHyg[5Jwf3SqIH3v[IVz[XSnbIm= NH\lRnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUS4NFM6OSd-MkG0PFA{QTF:L3G+
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MCF7 NVnoWmhvTnWwY4Tpc44h[XO|YYm= MY[xNEB2VQ>? MXuyOEBpenN? NWnmS5NSUW6mdXP0bY9vKG:oIIPlcIVkfGm4ZTDld5Rzd2enbjDy[YNmeHSxcjDhcJBp[SCmZXfyZYRifGmxbjDpckBpfW2jbjDNR2Y4KGOnbHzzJIF1KDFyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MkG2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3NkK3N|coRjJ7NU[yO|M4RC:jPh?=

... 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
  • 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

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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
NCT04544189 Not yet recruiting Drug: Alpelisib|Drug: Fulvestrant|Drug: Placebo Breast Neoplasms Novartis Pharmaceuticals|Novartis December 31 2020 Phase 2
NCT04567420 Not yet recruiting Drug: Palbociclib|Drug: Fulvestrant|Drug: Adjuvant Therapy Breast Cancer Criterium Inc. December 15 2020 Phase 2
NCT04524000 Recruiting Drug: Alpelisib|Drug: Fulvestrant Advanced Breast Cancer Novartis Pharmaceuticals|Novartis November 20 2020 Phase 2
NCT04483505 Recruiting Drug: Combination Rogaratinib + palbociclib + fulvestrant Breast Cancer Metastatic|Hormone Receptor Positive Malignant Neoplasm of Breast Fundacion CRIS de Investigación para Vencer el Cáncer|Bayer|Pfizer|Apices Soluciones S.L. November 25 2020 Phase 1
NCT04572295 Recruiting Drug: E7090|Drug: Fulvestrant|Drug: Exemestane Breast Neoplasms Eisai Co. Ltd.|Eisai Inc. October 9 2020 Phase 1
NCT04300790 Recruiting Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant Breast Cancer MedSIR|Novartis October 23 2020 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