Fulvestrant (ICI-182780)

Catalog No.S1191 Synonyms: ZD 9238, ZM 182780

For research use only.

Fulvestrant (ICI-182780, ZD 9238, ZM 182780) is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.

Fulvestrant (ICI-182780) Chemical Structure

CAS No. 129453-61-8

Selleck's Fulvestrant (ICI-182780) has been cited by 112 publications

Purity & Quality Control

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Biological Activity

Description Fulvestrant (ICI-182780, ZD 9238, ZM 182780) is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.
Targets
ER [1]
(Cell-free assay)
0.94 nM
In vitro

Fulvestrant is an effective inhibitor of the growth of ER-positive MCF-7 (with IC50 of 0.29 nM) but with no effect on the growth of ER-negative BT-20 human breast cancer cells. Fulvestrant causes accumulation of cells in G0/G1 and also reduces the proportion of cells capable of continued DNA synthesis. [1] Fulvestrant competitively inhibits binding of oestradiol to the estrogen receptor. Fulvestrant blocks nuclear localization of the ER through impairing receptor dimerisation, and energy-dependent nucleo-cytoplasmic shuttling. Because of the instability of fulvestrant-ER complex, the binding of Fulvestrant with ER finally results in accelerated degradation of the ER protein. [2] Fulvestrant (10 nM) not only decreases IGF-IR mRNA levels but also decreases the half-life. [3] Treatment with 100 μM Fulvestrant leads to a time dependent increase of TNFR1 and TRADD steady-state mRNA levels in MCF-7 cells. [4] Fulvestrant is capable of down-regulating androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells. Fulvestrant also significantly attenuates R1881-stimulated growth by 70%. [5] Fulvestrant is able to modulate mitosis and cell death in immature cerebellar neurons via rapid activation of MAPK. [6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrYNU4{NTFyMECgcm0> NVjaWFNqPDhiaB?= Mnr2bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NF7k[|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3PVI6PCd-MkS5O|kzQTR:L3G+
MCF-7/LTED M4CybWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLncmQyNjNvMUCwNEBvVQ>? MkKwOFghcA>? MVnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MofKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{myPVQoRjJ2OUe5Nlk1RC:jPh?=
HCC1428 NH;iNnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHXWIQxOS5|LUGwNFAhdk1? MmP4OFghcA>? Mn3lbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NIezbY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3PVI6PCd-MkS5O|kzQTR:L3G+
HCC1428/LTED MmnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXUeoEyNjNvMUCwNEBvVQ>? MWG0PEBp MX7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mn62QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{myPVQoRjJ2OUe5Nlk1RC:jPh?=
LCC1 M3;wVWZ2dmO2aX;uJGF{e2G7 NWjIWY85OTByIH7N MY[0PE0yPDRiaB?= NHXzenJi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= NGe2bnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi1PFI4Pyd-MkS4OVgzPzd:L3G+
LCC9 NX\LRVFETnWwY4Tpc44hSXO|YYm= NHPW[oEyODBibl2= NWHpcYw6PDhvMUS0JIg> NGfPPVVi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?= NVuzT|FXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OVgzPzdpPkK0PFU5Ojd5PD;hQi=>
MCF-7  NV;nb|FzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlG1NVAxKG6P NHz4Z5M2KGR? MljZbY5pcWKrdIOgZ4VtdCCpcn;3eIghfG9iMUFvwKU> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhzOUW1NEc,OjR6MUm1OVA9N2F-
mesangial  MUXGeY5kfGmxbjDBd5NigQ>? MkHjNE4yNTFyMDDuUS=> NIi1WoQ1QCCq M1TDb5N2eHC{ZYPz[ZMhXEeILd8yNU1qdmS3Y3XkJJR6eGViSW[gZ49tdGGpZX6= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd7M{[zPUc,OjR5OUO2N|k9N2F-
Mesangial NVLDSI9tTnWwY4Tpc44hSXO|YYm= M3nTbFAvOS1zMECgcm0> M2PnWVAvPSCq MkfFbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIGPtZYQzKHCqb4PwbI9zgWyjdHnvckB3cWFiR2DFVi=> NX62N5RRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3PVM3OzlpPkK0O|k{PjN7PD;hQi=>
ER+ MCF-7/2a MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvRRplmUUN3ME2wMlAxPCEQvF2= M3LxdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3M{K0PFg1Lz5zNUOyOFg5PDxxYU6=
ER+ MCF-7 M2DLTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLNSJMzODBiaB?= MXnJR|UxRTBwMkGgcm0> NXG0NnQ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWzNlQ5QDRpPkG1N|I1QDh2PD;hQi=>
MCF-7  M2\vfGZ2dmO2aX;uJGF{e2G7 NIftNo4yOMLibl5CpC=> NXrLbod[PzJiaB?= NWC2N|RQemW4ZYLz[ZMhfGinIHXzeJJw\2WwIHXm[oVkfCiLQ{WwJFEvQSEFlzCxNQKJmjliTTm= MoTjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEi2OVIoRjJ2OUC4OlUzRC:jPh?=
MCF-7  NF36PI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXSfXZ[UUN3MNMgc4Yh[XCycn;4bY1ifGWueTCyJI5O NGLmWJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S0PFM1Pid-MkO0OFg{PDZ:L3G+
H1975  NIHKbW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPDN:Kh|ryP NIH2eVIyKG1? M1nP[olv[3KnYYPld{B1cGViZ3XmbZRqdmmkIIPlcpNqfGm4aYT5JI9nKEhzOUe1JINmdGy|wrC= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ4OEixNEc,OjR{Nki4NVA9N2F-
H1975 NE\IV4pHfW6ldHnvckBCe3OjeR?= M2n4U|PDqM7:TR?= Mnq4NUBu Ml:weZBz\We3bHH0[ZMhfGinIHzleoVtKG:oIFzleE04[w>? NEXob2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK2PFgyOCd-MkSyOlg5OTB:L3G+
MCF-7  M1Lw[mZ2dmO2aX;uJGF{e2G7 NXTx[GZZOTBy4pEJcm3DqA>? Mk\oO|IhcA>? MVry[ZZmenOnczD0bIUheHKxdHXjeIl3\SCnZn\lZ5Qhd2ZiRUNCpIlvKGOnbHygbY53[XOrb36= NVHGVnZQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|Y4PzNpPkKzPVM3Pzd|PD;hQi=>
MCF-7  M3jM[mZ2dmO2aX;uJGF{e2G7 M4nVdVExOOLCiX7NxsA> NU\PVGlbOjRxNEigbC=> NHX1SI5n[WOrbHn0ZZRmeyCrbo\hd4lwdiC2aILveYdpKE2PUIOnJI1w\HWuYYTpc44> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|Nke3N{c,OjN7M{[3O|M9N2F-
BT474-tet-shMED1 Mke4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzVVFIxNjFvNTFOwG0> NVTDXZlFPyCm NFruTmhqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NVjzZW5NRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N|YzOzRpPkKzPVM3OjN2PD;hQi=>
ZR75-1-tet-shMED1  MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:wMlEuPSEQvF2= NFHMTVc4KGR? MXvpcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M{\XV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO2NlM1Lz5{M{mzOlI{PDxxYU6=
MCF-7-tet-shMED1 NYO0bohzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmX5NE4yNTVizszN MX23JIQ> M3fYZolv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M4jrTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OUO2NlM1Lz5{M{mzOlI{PDxxYU6=
HepG2  NV2xU3ZTTnWwY4Tpc44hSXO|YYm= MXWwMlAyNTFyIN88US=> MmnKNVghcMLi MVvhZ5RqfmG2ZYOgeIhmKEWURT3t[YRq[XSnZDD0doFve2O{aYD0bY9vKG:oIFHGNmVT NHfod5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{ezN|E5QCd-MkO3N|MyQDh:L3G+
MCF-7L  NXm2UmxYTnWwY4Tpc44hSXO|YYm= MXKxNFAhdk4EoB?= NWPidVc{OTBibXnuM|I1KGhxNEigbC=> MWTy[ZN2dHS|IHnuJGVITlJuIFjFVlIh[W6mIFjFVlMheGixc4Doc5J6dGG2aX;uJIF1KHC{b3zvcodm\CCneIDvd5Vz\Q>? M1e3NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nki2OFE3Lz5{M{[4OlQyPjxxYU6=
MCF-7L  M2\HV2Z2dmO2aX;uJGF{e2G7 NUDlRnlKOTByIH7NxsA> MXi0PEBp NV64d2llcW6mdXPld{B2eHKnZ4XsZZRqd25ib3[gcXJPSSCxZjDFS2ZTKGyrZ3Hu[EBJSi2HR1[= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ6NkSxOkc,OjN4OE[0NVY9N2F-
MCF-7L MV\GeY5kfGmxbjDBd5NigQ>? Mn\ZNVAxKG6PwrC= NFq5dVk1QCCq MVfpcoR2[2W|IFXHSnIh\mGvaXz5JI1mdWKncjDhZ5RqfmG2aX;uJJJmeXWrcnXkJGVT NV[2cHp3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2PFY1OTZpPkKzOlg3PDF4PD;hQi=>
C4-12  MkLhSpVv[3Srb36gRZN{[Xl? M1\rWlExOCCwTdMg MYq0PEBp NFrXUZVqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU NEiyO4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[4OlQyPid-MkO2PFY1OTZ:L3G+
MCF-7L NYrFUZM{TnWwY4Tpc44hSXO|YYm= NUTQcHFDOTByIH7NxsA> M37W[VI1KGh? NGjxZpFqdmS3Y3XzJGVITlJicHjvd5Bpd3K7bHH0bY9vKHKncYXpdoVlKEiELVXHSkBnfW6ldHnvci=> MkfJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4OE[0NVYoRjJ|Nki2OFE3RC:jPh?=
MMQ  MkDkSpVv[3Srb36gRZN{[Xl? MkXpNE03OjVibl2= NH25T4w4OiCq MoLX[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiZYP0do9o\W5icnXj[ZB1d3JvzsGgLGVT|rFr NGC1N5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{WyN|M2Pyd-MkO1NlM{PTd:L3G+
H1975  NXjKeVFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPlXWcxNjNzMkWtNVAh|ryP NFjiUmE3KGR? MkezbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7OUm1O{c,OjN|OUm5OVc9N2F-
H1975  NXexNVFQSXCxcITvd4l{KEG|c3H5 MXmyNFAhdk1? M3vPfFczKGh? MYnlcohidmOnczDldoxwfGmwaXKgbY5lfWOnZDDhdI9xfG:|aYO= NHv3bII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5PVk2Pyd-MkOzPVk6PTd:L3G+
MCF-7  MkCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXSxNE8yODBxMUCwNEBvVQ>? M4q1W|IwPC94IHS= NFK1TmhFVVOR MXLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{ NVjYVm1MRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNVM2ODZpPkKzN|E{PTB4PD;hQi=>
MCF-7  NWfGVHNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXMNVAxKG6P MWS0JIQ> MYLEUXNQ NGrTb3NqdmS3Y3XzJIEhcGmpaHXyJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5idHjlJGcyKHCqYYPlxsA> NGXRSo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OxN|UxPid-MkOzNVM2ODZ:L3G+
MLO-Y4  NHPhV5ZHfW6ldHnvckBCe3OjeR?= MnHtNeKh|ryP M33yd|EhcA>? NHnHT41qdmirYnn0d{BGOi2rbnT1Z4VlKEO6NEOg[ZhxemW|c3nvci=> NGSzUlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K0O|A2Pyd-MkOyOFcxPTd:L3G+
MCF-7 NXTFdXY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rkWFExOCCwTR?= Mlf2OFghcA>? M{nIToFjem:pYYTld{B1cGVicILvcIln\XKjdHn2[UBm\m[nY4Sgc4YhdW:mZYLheIUhdmm2cn;zZZRqfmVic4Ty[ZN{ NXfRbHgyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyNVY4PDRpPkKzNlE3PzR2PD;hQi=>
TG1-1  M4fofWZ2dmO2aX;uJGF{e2G7 NUTkO|czOcLizszN MXyyOEBp Mn\RZYJzd2ejdHXzJGUzyqCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBJUUZvMd8x NFPEfVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C4PFYxPyd-MkOwPFg3ODd:L3G+
TG1-1  NEm4dXRHfW6ldHnvckBCe3OjeR?= NXLHVnlbOcLizszN NWe1O2NmOjRiaB?= MV;hZpJw\2G2ZYOgSVLDqGmwZIXj[YQh[WOldX31cIF1cW:wIH;mJHBKO0t? M2LMb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEi4OlA4Lz5{M{C4PFYxPzxxYU6=
MCF7 NHPqVINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfjdpJTOTByIH7N NW\nXZdVPDhiaB?= MUDs[YFleyC2bzDhJJNqdWmuYYKgcI9{eyCrbjDzeZJ3cX[jbDDhd{B4cXSqIHTvfI9zfWKrY3nuJIFtd26n MoLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyN{eyOFkoRjJ|MEe3NlQ6RC:jPh?=
MCF7 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHze2VvOTByIH7N MVG0PEBp MY\lcohidmOnczDueZRtcW5vbXXkbYF1\WRiY3XscEBl\WG2aB?= NFWxZoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C3O|I1QSd-MkOwO|czPDl:L3G+
MCF-7  NXPVT5c{TnWwY4Tpc44hSXO|YYm= M1rle|YhcA>? NXfvU4k2TE2VTx?= NFfYe4hifHSnboXheIV{KHSqZTDmcJVlcW:6b37pcE0hd3JiZnXubIV5[W2rZD3pcoR2[2WmIHnuZ5Jm[XOnIHnuJI1qWi1{MTDlfJBz\XO|aX;u MoTqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNUKwN|YoRjJ|MEWyNFM3RC:jPh?=
MCF-7 NWi2W3gxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXGxNFAhdk1xMTFOwG0> NWDBZ212PSCm NEHmbWZqdmirYnn0d{B1cGVic4TpcZVt[XSrb36gc4YhOTgQsj3ld5Rz[WSrb3y= NFP5Upo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mkm4Nlc3PSd-MkK5PFI4PjV:L3G+
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Assay
Methods Test Index PMID
Western blot MDM2 / ER ; p-ErbB3 Y1289 / ErbB3 / p-ErbB4 Y1056 / ErbB4 / p-AKT / AKT / p-ERK / ERK ; ErbB3 ; ERα 24747123 21396094 23999432 19815064
Immunofluorescence IGF-1R / Erα ; Snail / E-cadherin 19815064 23936773
Growth inhibition assay Cell viability 29787591
In vivo Fulvestrant is devoid of uterotropic activity, and when co-administered with estradiol, it effectively blocks the uterotropic action of estradiol with ED50 of 0.06 mg/kg/day s.c. in immature female rats. A single s.c. injection of 5 mg of Fulvestrant suspension blocks completely the growth of MCF-7 xenografts. The growth of transplants of the BrlO human breast tumor is also suppressed effectively by 10 μM Fulvestrant. [1] Fulvestrant (10 mg/rat, s.c.) reduces the androgen receptor expression, ERK1/2 phosphorylation and cell proliferation in the rat ventral prostate. [7] Fulvestrant also displays anti-angiogenesis in the chick egg chorioallantoic membrane. [8]

Protocol (from reference)

Cell Research:[1]
  • Cell lines: MCF-7 breast cancer cells
  • Concentrations: 2.9 nM
  • Incubation Time: 5 days
  • Method: MCF-7 cells are cultured in multiwell plates (24-well, seeding density 4 × 104) in minimal essential medium containing phenol red, insulin (10 μg/mL), and 5% charcoal-stripped fetal calf serum without additional estradiol. Fulvestrant and/or estradiol are added in fresh medium 2 days after seeding. Cultures are maintained for 5 days with one further medium change and growth is assessed by measurement of total cell protein at the beginning and end of treatment and compared with that of controls treated with ethanol (0.1%) alone.
Animal Research:[6]
  • Animal Models: The human breast cancer xenografts MCF-7 in nude mice
  • Dosages: 5 mg/mouse
  • Administration: s.c. injection

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

0.4mg/mL

Chemical Information

Molecular Weight 606.77
Formula

C32H47F5O3S

CAS No. 129453-61-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05191004 Not yet recruiting Drug: NUV-422|Drug: Fulvestrant Advanced Breast Cancer|Metastatic Breast Cancer|Breast Cancer|Breast Carcinoma|Cancer of the Breast|Cancer of Breast|Malignant Tumor of Breast|Breast Tumor Nuvation Bio Inc. March 2022 Phase 1|Phase 2
NCT05082025 Not yet recruiting Drug: Copanlisib|Drug: fulvestrant Endometrial Cancer|Ovarian Cancer M.D. Anderson Cancer Center|Bayer February 28 2022 Phase 2
NCT05181033 Not yet recruiting Drug: Lenvatinib + Letrozole|Drug: Fulvestrant Breast Cancer National University Hospital Singapore|Eisai Co. Ltd. January 2022 Phase 2
NCT05135104 Not yet recruiting Drug: Palbociclib Metastatic Breast Cancer Asociatia Oncohelp - Centrul de Oncologie Oncohelp|MDX Research November 15 2021 --
NCT05022342 Recruiting Other: alpelisib plus fulvestrant Breast Cancer Novartis Pharmaceuticals|Novartis October 27 2021 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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Frequently Asked Questions

Question 1:
Is there any information for the half-life of fulvestrant (Cat No.S1191)?

Answer:
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.

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