Fulvestrant

Catalog No.S1191

Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay.

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Fulvestrant Chemical Structure

Fulvestrant Chemical Structure
Molecular Weight: 606.77

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Related Compound Libraries

Fulvestrant is available in the following compound libraries:

Estrogen/progestogen Receptor Inhibitors with Unique Features

  • Pan ER Antagonist

    Bazedoxifene HCl Pan-ER antagonist, ERα, IC50=23 nM; Erβ, IC50=89 nM.

  • Most Potent ER Agonist

    Hexestrol ERα, EC50=0.07 nM; ERβ, EC50=0.175 nM.

  • FDA-approved ER Inhibitor

    Tamoxifen Citrate Approved by FDA for breast cancer.

  • Classic ER Agonist

    Erteberel (LY500307) Potent, selective estrogen receptor β agonist with EC50 of 0.66 nM, 32-fold selectivity against estrogen receptor α. Phase 2.

Product Information

  • Compare Estrogen/progestogen Receptor Chemicals
    Compare Estrogen/progestogen Receptor Products
  • Research Area

Product Description

Biological Activity

Description Fulvestrant is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay.
Targets ER [1]
(Cell-free assay)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MCF-7NITieJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFfxSo8yNjNvMUCwNEBvVQ>?MlXGOFghcA>?MkLTbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>Ml;0NlQ6Pzl{OUS=
MCF-7/LTEDM1fZbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NICzPZEyNjNvMUCwNEBvVQ>?MmXoOFghcA>?NHHuVWRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?M3LIXVI1QTd7Mkm0
HCC1428M2jMcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NILjfFYyNjNvMUCwNEBvVQ>?NYi3fmVCPDhiaB?=M2fWWIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzNGXpNW8zPDl5OUK5OC=>
HCC1428/LTEDMUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NIi5S5kyNjNvMUCwNEBvVQ>?NVPHSol5PDhiaB?=MXTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>MYOyOFk4QTJ7NB?=
LCC1NID5UoNHfW6ldHnvckBCe3OjeR?=M3T1d|ExOCCwTR?=MVu0PE0yPDRiaB?=MVThZ5RqfmG2ZYOgWXBTKHOrZ37hcIlv\w>?Mo\kNlQ5PTh{N{e=
LCC9M{G0d2Z2dmO2aX;uJGF{e2G7MWKxNFAhdk1?NGTyeI01QC1zNESgbC=>M33LO4FkfGm4YYTld{BWWFJic3nncoFtcW6pNEntPVEzPDh3OEK3Oy=>
MCF-7 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MV[xNFAhdk1?NF\oXZA2KGR?NUfaNmtLcW6qaXLpeJMh[2WubDDndo94fGhidH:gNVDwxIV?Mnz6NlQ5OTl3NUC=
mesangial NVniOZZ2TnWwY4Tpc44hSXO|YYm=M3HzS|AvOS1zMECgcm0>NWXlRZB1PDhiaB?=M2jOfJN2eHC{ZYPz[ZMhXEeILd8yNU1qdmS3Y3XkJJR6eGViSW[gZ49tdGGpZX6=MmLKNlQ4QTN4M{m=
MesangialMUDGeY5kfGmxbjDBd5NigQ>?MnLCNE4yNTFyMDDuUS=>NWLLUpNXOC53IHi=M{TI[YlvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDTcYFlOiCyaH;zdIhwenmuYYTpc44hfmmjIFfQSXI>MknMNlQ4QTN4M{m=
ER+ MCF-7/2aM3fZZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnLXTWM2OD1yLkCwOEDPxE1?NF;yTpgyPTN{NEi4OC=>
ER+ MCF-7NIfBPFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1X6cVIxOCCqMVfJR|UxRTBwMkGgcm0>M2ftUFE2OzJ2OEi0
MCF-7 NH;VVmhHfW6ldHnvckBCe3OjeR?=MnfqNVDDqG6PwrC=NV7SSZJoPzJiaB?=MlvDdoV3\XK|ZYOgeIhmKGW|dILv[4VvKGWoZnXjeEhKSzVyIEGuPUDEnyBzMPMIllkhVSl?MV6yOFkxQDZ3Mh?=
MCF-7 M2HVSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NGfQWHBKSzVywrDv[kBieHC{b4jpcYF1\Wy7IEKgcm0>M4fjfFI{PDR6M{S2
H1975 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXqzxsDPxE1?NWLUVGM5OSCvMWDpcoNz\WG|ZYOgeIhmKGenZnn0bY5q[iC|ZX7zbZRqfmm2eTDv[kBJOTl5NTDj[Yxte8LiNGDqbpczPDJ4OEixNC=>
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MCF-7-tet-shMED1NEW2dYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXrHTZFiOC5zLUWg{txONHfCUYQ4KGR?NWrIT5hYcW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyMW[yN|k{PjJ|NB?=
HepG2 M1Oze2Z2dmO2aX;uJGF{e2G7M2HxT|AvODFvMUCg{txONGr4fXoyQCCqwrC=NIHIdIhi[3SrdnH0[ZMhfGinIFXSSU1u\WSrYYTl[EB1emGwc3PybZB1cW:wIH;mJGFHOkWUNGO3Z|QzOzd|M{G4PC=>
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MCF-7LNIDG[YRHfW6ldHnvckBCe3OjeR?=MWOxNFAhdk4EoB?=NF;xPVY1QCCqMoKwbY5lfWOnczDFS2ZTKG[jbXnsfUBu\W2kZYKgZYN1cX[jdHnvckBz\XG3aYLl[EBGWg>?NUH5fWxrOjN4OE[0NVY>
C4-12 MoLYSpVv[3Srb36gRZN{[Xl?NHvGRZoyODBibl5CpC=>NHzwVXY1QCCqNHuzSXhqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWUNIPLWWIzOzZ6NkSxOi=>
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H1975 NHP2eWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MUCwMlMyOjVvMUCg{txOMWW2JIQ>M1XEbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzNVjvOIVTOjN|OUm5OVc>
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MCF-7 NVfUV5dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MWSxNFAhdk1?Ml;QOEBlNVfZRYVUTE2VTx?=MkfkbY5lfWOnczDhJIhq\2incjDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKHSqZTDHNUBxcGG|ZdMgMmjWNlM{OTN3ME[=
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MCF-7MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{HTT|ExOCCwTR?=NFjBR5Q1QCCqM2H1PYFjem:pYYTld{B1cGVicILvcIln\XKjdHn2[UBm\m[nY4Sgc4YhdW:mZYLheIUhdmm2cn;zZZRqfmVic4Ty[ZN{NHnTXYgzOzJzNke0OC=>
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MCF-7/AC-1Mn:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M37N[lAuOC5{IN88US=>NH\KWYc3KGR?NELWSpBqdmirYnn0d{Bk\WyuIHfyc5d1cCCvb3Tld5RtgQ>?MWeyNlA1Ojd7Mh?=
MCF7NUXWdJV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2jv[lExKML3TR?=M2nRT|Q5KGh?MUHpcoR2[2W|IHPlcIwhcW6qaXLpeIlwdiC5aHnjbEBk[W5iYnWg[Y5p[W6lZXSgZpkh\mmkcn;icIF{fHN?MYKyNlA1OTh6Nx?=
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MMQNG\kTWRHfW6ldHnvckBCe3OjeR?=Mnv5NE03OjVibl2=Mn3VO|IhcA>?MmnpdJJw\HWlZYOgZUB{fGG2aYP0bYNidGy7IIPp[45q\mmlYX70MEBld3OnLXTldIVv\GWwdDDy[YR2[3Srb36gbY4hWFKOIIPlZ5JmfGmxbh?=MXuyNlAyPTFyMR?=
MCF7NH[zfXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3[wb|AuOSEQvF2=NYntZZhsOjRvMUKwJIg>NXiy[YRMcW6qaXLpeJMhfGinIHfyc5d1cCCxZjDNR2Y4NVmELUJCpC=>NXPNZ|dsOjF6NkOyOVg>
HepG2MnXGRZBweHSxc3nzJGF{e2G7M{TUSlAvOcLizszNMYeyOEBpMnXKZYJwdGm|aHXzJJRp\SCnc4Tyc4dmdi2rbnT1Z4VlKHWyLYLl[5Vt[XSrb36gc4Yh[XCxQVmgZY5lKGGyb12=NULtNphvOjF6MU[yN|M>
MCF7–iFR3MnLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mor5NlAuOTByIH7NNHzOeHI6PiCqNWX1TVVy\W6qYX7j[ZMhSVBvaX7keYNm\CClZXzsJIdzd3e2aDDpcohq[mm2aX;uMkPvNlE4QTJ6OEm=
MCF7SMliwSpVv[3Srb36gRZN{[Xl?NIXoTYEyyqEQvF2=MYm0PEBpNWPTe5hG\G:5boLl[5Vt[XSnczDveoVz[WyuIFXS{tEheHKxdHXpckBt\X[nbIO=NUXwd5V[OjF3M{OxPVU>
MCF7MVXGeY5kfGmxbjDBd5NigQ>?MmPiNeKh|ryPMX60PEBpMnXr[I94dnKnZ4XsZZRmeyCxdnXyZYxtKEWUzsGgdJJwfGWrbjDs[ZZmdHN?MkHGNlE2OzNzOUW=
MCF7SMmjoSpVv[3Srb36gRZN{[Xl?MnvVNeKh|ryPNUK0b4tmPyCmNH;OeW1ifHSnboXheIV{KHS3bX;yd5Bp\XKnIH\vdo1ifGmxbjDhcoQheHKxbHnm[ZJifGmxbh?=NUn2eFBSOjF3M{OxPVU>
MCF7SNXfBd2RpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M4fCRlAvPS9zIN88US=>NEfQWZg4KGR?NUezSldqTE2VTx?=NUnXSVh3\GWlcnXhd4V{KGOnbHyg[Zhx[W6|aX;uMXuyNVU{OzF7NR?=
T47D M4PoU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MlrDOEBvVQ>?Mn6wOFAhcA>?MoTkd5VxeHKnc4Pld{Bk\WyuIHfyc5d1cCCvb3TldoF1\Wy7MYqyNVQ5ODN7MR?=
BT474 NXraTINOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Ml\uOEBvVQ>?NIexems1OCCqMoLzd5VxeHKnc4Pld{Bk\WyuIHfyc5d1cCCvb3TldoF1\Wy7NIjHOmwzOTR6MEO5NS=>
T47D M3zMW2Z2dmO2aX;uJGF{e2G7Mnu1NVAhdk1?NVTRRZVOPDBiaB?=NXTINVBC\G:5boLl[5Vt[XSnczDFVu6yKHC{b4TlbY4>NWnkd|VQOjF2OECzPVE>
BT474 M{\1ZWZ2dmO2aX;uJGF{e2G7NHrDT3IyOCCwTR?=NF\ZZoM1OCCqMlG1[I94dnKnZ4XsZZRmeyCHUt8xJJBzd3SnaX6=MmHUNlE1QDB|OUG=
MCF7NHuwU2dHfW6ldHnvckBCe3OjeR?=MX2xNFAhdk1?Mn3QO{BlMUHy[YR2[2W|IFXS{tEh\XiycnXzd4lwdiC|aXfubYZq[2GwdHz5NVrqbW5kOjF|OU[wPVQ>
T47D Moq3SpVv[3Srb36gRZN{[Xl?NIDxOIwyODBibl2=MmrzO{BlMmf5doVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=>M1rJXVIyOzl4MEm0
BT474 M4mxS2Z2dmO2aX;uJGF{e2G7NFXabJoyODBibl2=MnftO{BlNIfoN2dz\WS3Y3XzJGVT|rFiZYjwdoV{e2mxbjDzbYdvcW[rY3HueIx6NGOyZ4MzOTN7NkC5OC=>
MDAMB361MVHGeY5kfGmxbjDBd5NigQ>?M2XtblExOCCwTR?=M17Xb|ch\A>?MkX0doVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=>M3:xc|IyOzl4MEm0
MCF7NU\aSWFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MViwMlAyNTFizszNNUj3dVBFPyCmNV3aR|J1emWmdXPld{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5M2W3V|IyOzl4MEm0
T47D NVLYcmxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUeyRnUzOC5yMT2xJO69VQ>?M1m2WVch\A>?MoTxdoVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7MWCyNVM6PjB7NB?=
BT474 M2m3[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MWCwMlAyNTFizszNMkLlO{BlMm[5doVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7MWKyNVM6PjB7NB?=
MDAMB361MlfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NETaXmIxNjBzLUGg{txONHO1OpI4KGR?NUDWe2RtemWmdXPld{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5MlmzNlE{QTZyOUS=
MCF7NVH1U3BITnWwY4Tpc44hSXO|YYm=NV3GS4tyOTByIH7NMXy3JIQ>NWjTc3l7cW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=>M4[xVFIyOzl4MEm0
T47D MVLGeY5kfGmxbjDBd5NigQ>?NFvvVosyODBibl2=NUPnXlV5PyCmM4\0d4lv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne=MWSyNVM6PjB7NB?=
BT474 NUDwTYhZTnWwY4Tpc44hSXO|YYm=NVTmdJNzOTByIH7NMlLZO{BlM1qwXolv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne=M1;MTVIyOzl4MEm0
MDAMB361NHO3UHpHfW6ldHnvckBCe3OjeR?=NYT6V|loOTByIH7NM4i2Olch\A>?NGfPO4RqdmS3Y3XzJI9nKEW{YlKzJIFv\CCHcnLCOEBz\WOncITvdkBmgHC{ZYPzbY9vKGGwZDDzbYdv[WyuaX7nM3:ySFIyOzl4MEm0
MCF7M2jTOGZ2dmO2aX;uJGF{e2G7NWfkSoNzOTBibl2=NYDlZoQzQTZiaB?=NFr5Omhld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc47DqA>?NHj0TW8zOTN5OEOzNy=>
MDA-MB-231NE\DNZRHfW6ldHnvckBCe3OjeR?=NFHjcIcyOCCwTR?=MYS5OkBpM3y3UIRwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvcuKhMn7sNlE{Pzh|M{O=
SK-BR-3NXTPN4tsTnWwY4Tpc44hSXO|YYm=Mo\wNVAhdk1?NETXWok6PiCqMUTkc5dvemWpdXzheIV{KEWUIHX4dJJme3Orb39CpC=>M3KxN|IyOzd6M{Oz
MCF-7NG\nVHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NHLMbJIyODBibl2=MmL0O|IwQTZiaB?=NIm0ZVlk[XW|ZYOgZ4VtdCCleXPs[UBienKnc4S=NXjSVJk5OjF{OUm4OlI>
MMQMn\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NVmwTYd[OC5yMEitOlI2KG6PNHLmcos4OiCqM4T1XYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIghfGmvZT2gZY5lKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=NIq4WpYzODdyMEe1OS=>
MMQNHqzbmFHfW6ldHnvckBCe3OjeR?=NF7aTGsxNjByOD22NlUhdk1?MnnSO|IhcA>?M2PvOYlvcGmkaYTzJHBTVCC|ZXPy[ZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?NUWzVld4OjB5MEC3OVU>
MMQNXHOeIhLTnWwY4Tpc44hSXO|YYm=MVywMlA1NTZ{NTDuUS=>MWq3NkBpMmPtbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:wNIS2cY4zODdyMEe1OS=>
MMQNYX2dZNqTnWwY4Tpc44hSXO|YYm=NU\iVodxOC5yND22NlUhdk1?MWi3NkBpMWL1dJJm\3WuYYTld{BVT0cQskOgZY5lKFSJRt8yVmlKKGW6cILld5Nqd25?NWC1NYdUOjB5MEC3OVU>

... Click to View More Cell Line Experimental Data

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]
Features

Protocol(Only for Reference)

Cell Assay: [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 Study: [6]

Animal Models The human breast cancer xenografts MCF-7 in nude mice
Formulation 50 mg/mL in arachis oil
Dosages 5 mg/mouse
Administration s.c. injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Wakeling AE, et al. Cancer Res, 1991, 51(15), 3867-3873.

[2] Osborne CK. Br J Cancer, 2004, 90 Suppl 1, S2-6.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02763566 Not yet recruiting Breast Cancer Eli Lilly and Company October 2016 Phase 3
NCT02476786 Not yet recruiting Breast Cancer|Cancer of Breast|Breast Neoplasms|Cancer of the Breast Washington University School of Medicine|Genomic Health®,  ...more Washington University School of Medicine|Genomic Health®, Inc. October 2016 Phase 2
NCT02738866 Not yet recruiting Metastatic Breast Cancer Sidney Kimmel Comprehensive Cancer Center|Pfizer July 2016 Phase 2
NCT02795039 Recruiting Healthy Fresenius Kabi June 2016 Phase 1
NCT02756364 Not yet recruiting Breast Neoplasms Millennium Pharmaceuticals, Inc. June 2016 Phase 2

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Chemical Information

Download Fulvestrant SDF
Molecular Weight (MW) 606.77
Formula

C32H47F5O3S

CAS No. 129453-61-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms ICI-182780, ZD 9238
Solubility (25°C) * In vitro DMSO 100 mg/mL (164.8 mM)
Ethanol 100 mg/mL warming (164.8 mM)
Water <1 mg/mL (<1 mM)
In vivo 5% DMSO+95% Corn oil 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 7-​[9-​[(4,​4,​5,​5,​5-​pentafluoropentyl)​sulfinyl]​nonyl]​-​ (7α,​17β)​-estra-​1,​3,​5(10)​-​triene-​3,​17-​diol

Customer Product Validation(3)


Click to enlarge
Rating
Source Mol Cancer Ther 2014 13(1), 230-8. Fulvestrant purchased from Selleck
Method Colony formation
Cell Lines T47D, MCF-7 cells
Concentrations 10, 100 nM
Incubation Time 2 weeks
Results Resultant cells were cultured with and without TAM for about 2 weeks for their colony forming activities as previously described. PTPH1 overexpression in both cell lines significantly increases the growth inhibition by fulvestrant as compared with their respective controls.

Click to enlarge
Rating
Source PLoS One 2011 6, e21112. Fulvestrant purchased from Selleck
Method crystal violet staining
Cell Lines MCF-7 cells
Concentrations 100 nM
Incubation Time 21 day
Results Compared with the control MCF7-R73 cells transduced with the NF-KB p65-only retrovirus (hereafter referred to as MCF-238 cells), the MCF7-R73 cells transduced with six of the 46 unique ZF-TFs demonstrated survival and growth in the presence of 100 nM fulvestrant.

Click to enlarge
Rating
Source PLoS One 2011 6, e21112. Fulvestrant purchased from Selleck
Method Growth Assays
Cell Lines MCF-7/T47D cells
Concentrations 100 nM
Incubation Time 15 day
Results Similar to what was observed with MCF7-R73 cells, the six ZF-TFs conferred resistance to fulvestrant-induced growth inhibition in T47D cells (Figure C).

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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