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-7NF;rNI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MkS5NU4{NTFyMECgcm0>MnHROFghcA>?Ml:0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>MonMNlQ6Pzl{OUS=
MCF-7/LTEDNYm3Xo9lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MmH6NU4{NTFyMECgcm0>NXnJOnA3PDhiaB?=NFzz[5ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?NHjTTnUzPDl5OUK5OC=>
HCC1428NFPWW4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1;Jd|EvOy1zMECwJI5OM1zreFQ5KGh?NVG1XmRFcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?NFzWflUzPDl5OUK5OC=>
HCC1428/LTEDNUXofFhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NG\NVlIyNjNvMUCwNEBvVQ>?MknNOFghcA>?M2DOc4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzNF60OVgzPDl5OUK5OC=>
LCC1NWD4Z|B{TnWwY4Tpc44hSXO|YYm=MoHCNVAxKG6PNVf2UYNjPDhvMUS0JIg>NIHneWJi[3SrdnH0[ZMhXVCUIIPp[45idGmwZx?=NYjqSlA4OjR6NUiyO|c>
LCC9Ml;5SpVv[3Srb36gRZN{[Xl?NI\FVm8yODBibl2=NHvxVIg1QC1zNESgbC=>MXvhZ5RqfmG2ZYOgWXBTKHOrZ37hcIlv\w>?MY[yOFg2QDJ5Nx?=
MCF-7 NYDlW5BvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHXGWYgyODBibl2=NWjGR2hpPSCmNYr0XWRocW6qaXLpeJMh[2WubDDndo94fGhidH:gNVDwxIV?M3;GWlI1QDF7NUWw
mesangial NFzpZm9HfW6ldHnvckBCe3OjeR?=MVGwMlEuOTByIH7NMWm0PEBpM2rY[JN2eHC{ZYPz[ZMhXEeILd8yNU1qdmS3Y3XkJJR6eGViSW[gZ49tdGGpZX6=MoOxNlQ4QTN4M{m=
MesangialM2LafWZ2dmO2aX;uJGF{e2G7MorzNE4yNTFyMDDuUS=>M4W3SVAvPSCqM{DVZolvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDTcYFlOiCyaH;zdIhwenmuYYTpc44hfmmjIFfQSXI>NEDGVoEzPDd7M{[zPS=>
ER+ MCF-7/2aNV;QcmpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MkHTTWM2OD1yLkCwOEDPxE1?NIXySZQyPTN{NEi4OC=>
ER+ MCF-7MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MlyyNlAxKGh?MXfJR|UxRTBwMkGgcm0>NF;qNWgyPTN{NEi4OC=>
MCF-7 NUPuT|J6TnWwY4Tpc44hSXO|YYm=M3rkelExyqCwTdMgMmfNO|IhcA>?MofrdoV3\XK|ZYOgeIhmKGW|dILv[4VvKGWoZnXjeEhKSzVyIEGuPUDEnyBzMPMIllkhVSl?NIfLeWszPDlyOE[1Ni=>
MCF-7 NIHrNYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MlLtTWM2OMLib3[gZZBxem:6aX3heIVtgSB{IH7NNXTxTmx1OjN2NEizOFY>
H1975 MkHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MUSzxsDPxE1?Mlz0NUBuMnPlbY5kemWjc3XzJJRp\SCpZX\peIlvcWJic3Xud4l1cX[rdImgc4YhUDF7N{WgZ4VtdHQEoB?=MYSyOFI3QDhzMB?=
H1975MYPGeY5kfGmxbjDBd5NigQ>?M3\TTlPDqM7:TR?=NXLxVmxROSCvNVPrWIdOfXC{ZXf1cIF1\XNidHjlJIxmfmWuIH;mJGxmfC15Yx?=NWXFc4FmOjR{Nki4NVA>
MCF-7 M2PpVGZ2dmO2aX;uJGF{e2G7MlTJNVAx6oDLbl5CpC=>NEfWN5I4OiCqMWny[ZZmenOnczD0bIUheHKxdHXjeIl3\SCnZn\lZ5Qhd2ZiRUNCpIlvKGOnbHygbY53[XOrb36=MXOyN|k{Pjd5Mx?=
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BT474-tet-shMED1M2jlPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnXBNE4yNTVizszNMWG3JIQ>NHm2NGZqdmO{ZXHz[ZMhM0SxeDDpcoR2[2WmIHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=M2O5TlI{QTN4MkO0
ZR75-1-tet-shMED1 M4rpPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MmfxNE4yNTVizszNNXe2So45PyCmM2rObolv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?=NE\uUXEzOzl|NkKzOC=>
MCF-7-tet-shMED1M{Xa[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1v2UlAvOS13IN88US=>NXHOfWE1PyCmMYLpcoNz\WG|ZYOgL2RwgCCrbnT1Z4VlKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?M1jRblI{QTN4MkO0
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MCF-7L MUDGeY5kfGmxbjDBd5NigQ>?M13lfVExOCCwTdMgMmfGOFghcA>?MVrpcoR2[2W|IIXwdoVofWyjdHnvckBw\iCvUl7BJI9nKEWJRmKgcIlo[W6mIFjCMWVITg>?NG[z[VYzOzZ6NkSxOi=>
MCF-7LM{XZVGZ2dmO2aX;uJGF{e2G7M4WzN|ExOCCwTdMgM3zmeVQ5KGh?Mn:4bY5lfWOnczDFS2ZTKG[jbXnsfUBu\W2kZYKgZYN1cX[jdHnvckBz\XG3aYLl[EBGWg>?NEX6bWYzOzZ6NkSxOi=>
C4-12 MkewSpVv[3Srb36gRZN{[Xl?MYGxNFAhdk4EoB?=MUe0PEBpNEnneZpqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWUNHH6cZYzOzZ6NkSxOi=>
MCF-7LNWW4PIxUTnWwY4Tpc44hSXO|YYm=MXOxNFAhdk4EoB?=NEnxeZAzPCCqMWHpcoR2[2W|IFXHSnIheGixc4Doc5J6dGG2aX;uJJJmeXWrcnXkJGhDNUWJRjDmeY5kfGmxbh?=NVvXd3BuOjN4OE[0NVY>
MMQ M{D0e2Z2dmO2aX;uJGF{e2G7M2XZOlAuPjJ3IH7NNHPMR284OiCqNWTTfFUz\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[g[ZN1em:pZX6gdoVk\XC2b4Kt{tEhMEWUzsGpMmS0NlM2OjN|NUe=
H1975 NVr6S3RuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mk\WNE4{OTJ3LUGwJO69VQ>?MV22JIQ>NFnUNW9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?NV3pPY1kOjN|OUm5OVc>
H1975 M{H6UWFxd3C2b4Ppd{BCe3OjeR?=Mk\YNlAxKG6PM2S1NFczKGh?MUHlcohidmOnczDldoxwfGmwaXKgbY5lfWOnZDDhdI9xfG:|aYO=M4fEUVI{Ozl7OUW3
MCF-7 NGHKV3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MV:xNE8yODBxMUCwNEBvVQ>?NH7r[4MzNzRxNjDkNYLYN2psTE2VTx?=MXHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCkb4ToJIRwe2VvIHHu[EB1cW2nLTDk[ZBmdmSnboSgcYFvdmW{MW[yN|MyOzVyNh?=
MCF-7 M3vPfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MYexNFAhdk1?MXu0JIQ>M{jOU2ROW09?MoHRbY5lfWOnczDhJIhq\2incjDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKHSqZTDHNUBxcGG|ZdMgM3HrZ|I{OzF|NUC2
MLO-Y4 MnLMSpVv[3Srb36gRZN{[Xl?NF\acWUyyqEQvF2=NV3N[3RuOSCqNWTPSnJpcW6qaXLpeJMhTTJvaX7keYNm\CCFeESzJIV5eHKnc4Ppc44>NFzVO44zOzJ2N{C1Oy=>
MCF-7NETVTphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NXuxWGZpOTByIH7NM{jnU|Q5KGh?MmmxZYJzd2ejdHXzJJRp\SCycn;sbYZmemG2aY\lJIVn\mWldDDv[kBud2SncnH0[UBvcXS{b4PheIl3\SC|dILld5M>NYPEcZE{OjN{MU[3OFQ>
TG1-1 NFLNbGtHfW6ldHnvckBCe3OjeR?=NX7PRYE6OcLizszNNWX1c3FSOjRiaB?=M{W3cYFjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhUEmILUJOtS=>M2P2WFI{ODh6NkC3
TG1-1 MWHGeY5kfGmxbjDBd5NigQ>?MUixxsDPxE1?NEG0boMzPCCqNGfQe3Vi[nKxZ3H0[ZMhTTMEoHnu[JVk\WRiYXPjeY12dGG2aX;uJI9nKFCLM1u=M1rIWFI{ODh6NkC3
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MCF-7 MY\GeY5kfGmxbjDBd5NigQ>?NXGyRpB[PiCqNW\qNoQ5TE2VTx?=MVXheJRmdnWjdHXzJJRp\SCobIXkbY95d26rbD2gc5Ih\mWwaHX4ZY1q\C2rbnT1Z4VlKGmwY4LlZZNmKGmwIH3pVk0zOSCneIDy[ZN{cW:wNIjOXIUzOzB3MkCzOi=>
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MCF-7NX[5eHI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NE[2[5QyODBibl2=NHPodm42KGR?MV\pcohq[mm2czD0bIUhe3SrbYXsZZRqd25ib3[g[pV{[XKrZXzpckBJMXSyNlk5Ojd4NR?=
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MCF-7NXfndllyTnWwY4Tpc44hSXO|YYm=M3vPfVExOCCwTR?=MVWxJIg>M1XaTWV1V0kEoB?=M{\wc5Ric2W|IH;uJIEheHWwY4TheIUhe3SjaX7pcocheGG2dHXyci=>NWTBTI9tOjJ6NkmxNFY>
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MCF7SNV3leopvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NX3zeYlrOC53L{Gg{txOMn7kO{BlNXrw[ooxTE2VTx?=M4e0UIRm[3KnYYPld{Bk\WyuIHX4dIFve2mxbh?=NVjUcHFKOjF3M{OxPVU>
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BT474 NGDJR2lHfW6ldHnvckBCe3OjeR?=NUW5To9{OTBibl2=NH;wc2w1OCCqM1znTIRwf26{ZXf1cIF1\XNiRWNOtUBxem:2ZXnuM3q2ZVIyPDhyM{mx
MCF7Ml3WSpVv[3Srb36gRZN{[Xl?MXyxNFAhdk1?MVW3JIQ>M2jiSpJm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk>MkHDNlE{QTZyOUS=
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MDAMB361NEnGV3dHfW6ldHnvckBCe3OjeR?=MVixNFAhdk1?NYi4N3pkPyCmM4jPTpJm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk>NH7vRngzOTN7NkC5OC=>
MCF7M4m0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NIP6WZMxNjBzLUGg{txONFO4WlQ4KGR?MnjadoVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7MoT3NlE{QTZyOUS=
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MMQMonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1fYR|AvODB6LU[yOUBvVQ>?MYG3NkBpMkTFbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYn;0bEB1cW2nLTDhcoQh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{M3q1fFIxPzByN{W1
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... 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 2016-07-30)

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 Active, not 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
2 years -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
In vivo 5% DMSO+95% Corn oil 30mg/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

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.

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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