Fulvestrant

For research use only. Not for use in humans.

製品コードS1191 別名:ICI-182780, ZD 9238

Fulvestrant化学構造

CAS No. 129453-61-8

Fulvestrant (ICI-182780, ZD 9238) 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.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 12600 あり
JPY 13600 あり
JPY 46800 あり
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バルク問合せ

文献中Selleckの製品使用例(83)

製品安全説明書

Estrogen/progestogen Receptor阻害剤の選択性比較

生物活性

製品説明 Fulvestrant (ICI-182780, ZD 9238) 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.
ターゲット
ER [1]
(Cell-free assay)
0.94 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 Mn6wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHmd29zOS5|LUGwNFAhdk1? MWq0PEBp NVjPZ2hqcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4LsOVI1QTd7Mkm0
MCF-7/LTED M{nhUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWSxMlMuOTByMDDuUS=> NXyxeXFrPDhiaB?= MmnpbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVmyOFk4QTJ7NB?=
HCC1428 NU[3WlJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jV[FEvOy1zMECwJI5O MX:0PEBp NUThelVWcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Ml\SNlQ6Pzl{OUS=
HCC1428/LTED M1P0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYW0S45oOS5|LUGwNFAhdk1? M{jITVQ5KGh? M4[wSolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NInkVFkzPDl5OUK5OC=>
LCC1 M{HJXWZ2dmO2aX;uJGF{e2G7 MWexNFAhdk1? Ml3WOFguOTR2IHi= MXnhZ5RqfmG2ZYOgWXBTKHOrZ37hcIlv\w>? MX2yOFg2QDJ5Nx?=
LCC9 NEXoeHRHfW6ldHnvckBCe3OjeR?= MlP2NVAxKG6P Mmq5OFguOTR2IHi= M1PFRYFkfGm4YYTld{BWWFJic3nncoFtcW6p MYSyOFg2QDJ5Nx?=
MCF-7  NHXs[IJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX2xN3M1OTByIH7N MluzOUBl M2n6c4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSxIEGw89yG NUfE[5dHOjR6MUm1OVA>
mesangial  NF7UZ|BHfW6ldHnvckBCe3OjeR?= MVGwMlEuOTByIH7N M{HUe|Q5KGh? Ml\Nd5VxeHKnc4Pld{BVT0ZvzsKxMYlv\HWlZXSgeJlx\SCLVjDjc4xt[Wenbh?= M3TOU|I1Pzl|NkO5
Mesangial MYPGeY5kfGmxbjDBd5NigQ>? MmrJNE4yNTFyMDDuUS=> NF;m[nkxNjViaB?= NV;GdVMxcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJHNu[WR{IIDoc5NxcG:{eXzheIlwdiC4aXGgS3BGWg>? NVHyeJZbOjR5OUO2N|k>
ER+ MCF-7/2a M{\PRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVq0d3F{UUN3ME2wMlAxPCEQvF2= Mn[xNVU{OjR6OES=
ER+ MCF-7 M4LnOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\xbFIxOCCq MljTTWM2OD1yLkKxJI5O M4nJ[VE2OzJ2OEi0
MCF-7  NI\JeolHfW6ldHnvckBCe3OjeR?= MmjmNVDDqG6PwrC= NGPOd4c4OiCq NUXyWo9nemW4ZYLz[ZMhfGinIHXzeJJw\2WwIHXm[oVkfCiLQ{WwJFEvQSEFlzCxNQKJmjliTTm= MU[yOFkxQDZ3Mh?=
MCF-7  M{njRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfrbFlKSzVywrDv[kBieHC{b4jpcYF1\Wy7IEKgcm0> NX7CeoFjOjN2NEizOFY>
H1975  M1[xdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUizxsDPxE1? NW\KXlE1OSCv NI\W[JZqdmO{ZXHz[ZMhfGinIHfl[ol1cW6rYjDz[Y5{cXSrdnn0fUBw\iCKMUm3OUBk\Wyuc9Mg MWqyOFI3QDhzMB?=
H1975 NVG2ZohOTnWwY4Tpc44hSXO|YYm= NID5UpE{yqEQvF2= NHrQUYYyKG1? MYn1dJJm\3WuYYTld{B1cGVibHX2[Ywhd2ZiTHX0MVdk NX3jWVlNOjR{Nki4NVA>
MCF-7  M{fNNmZ2dmO2aX;uJGF{e2G7 M2LnSlExOOLCiX7NxsA> NUTzNHVuPzJiaB?= M1vl[ZJmfmW{c3XzJJRp\SCycn;0[YN1cX[nIHXm[oVkfCCxZjDFNuKhcW5iY3XscEBqdn[jc3nvci=> MXyyN|k{Pjd5Mx?=
MCF-7  M17VS2Z2dmO2aX;uJGF{e2G7 MWGxNFDjiImwTdMg NF7FdIczPC92ODDo M3rjdoZi[2muaYTheIV{KGmwdnHzbY9vKHSqcn;1[4ghVU2SczegcY9lfWyjdHnvci=> NUPBOmxKOjN7M{[3O|M>
BT474-tet-shMED1 Mm[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH25dlkxNjFvNTFOwG0> MnWyO{Bl NU\BRlM2cW6lcnXhd4V{KCuGb4igbY5lfWOnZDDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MYeyN|k{PjJ|NB?=
ZR75-1-tet-shMED1  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[wMlEuPSEQvF2= MXW3JIQ> M1vOeolv[3KnYYPld{AsTG:6IHnu[JVk\WRiY3XscEBl\WG2aDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MVKyN|k{PjJ|NB?=
MCF-7-tet-shMED1 NEnrN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjycYsxNjFvNTFOwG0> NVzwPJdKPyCm MmDJbY5kemWjc3XzJEtFd3hiaX7keYNm\CClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M13uT|I{QTN4MkO0
HepG2  M3HSZmZ2dmO2aX;uJGF{e2G7 NFLKcGoxNjBzLUGwJO69VQ>? M2LHfFE5KGkEoB?= MVXhZ5RqfmG2ZYOgeIhmKEWURT3t[YRq[XSnZDD0doFve2O{aYD0bY9vKG:oIFHGNmVT NEjKT24zOzd|M{G4PC=>
MCF-7L  M2fXeGZ2dmO2aX;uJGF{e2G7 NX7QXHRzOTByIH7NxsA> M{LEN|ExKG2rbj:yOEBpNzR6IHi= NHrxSIRz\XO3bITzJIlvKEWJRmKsJGhGWjJiYX7kJGhGWjNicHjvd5Bpd3K7bHH0bY9vKGG2IIDyc4xwdmenZDDlfJBwe3W{ZR?= NVXkcIN7OjN4OE[0NVY>
MCF-7L  NXnBV5U2TnWwY4Tpc44hSXO|YYm= NX7RfYtCOTByIH7NxsA> Mn7lOFghcA>? M1jZWIlv\HWlZYOgeZBz\We3bHH0bY9vKG:oIH3SUmEhd2ZiRVfGVkBtcWejbnSgTGIuTUeI MlPLNlM3QDZ2MU[=
MCF-7L MV3GeY5kfGmxbjDBd5NigQ>? NXjOc4VMOTByIH7NxsA> M1zVOVQ5KGh? NGTJ[ndqdmS3Y3XzJGVITlJiZnHtbYx6KG2nbXLldkBi[3SrdnH0bY9vKHKncYXpdoVlKEWU NE\LdnEzOzZ6NkSxOi=>
C4-12  NFvrVINHfW6ldHnvckBCe3OjeR?= Mk\WNVAxKG6PwrC= MY[0PEBp NYXHSII1cW6mdXPld{BGT0[UIH\hcYltgSCvZX3i[ZIh[WO2aY\heIlwdiC{ZYH1bZJm\CCHUh?= Mmi3NlM3QDZ2MU[=
MCF-7L NEDiPZZHfW6ldHnvckBCe3OjeR?= NIPtZ3YyODBibl5CpC=> NHz5dHQzPCCq NXjMPVRHcW6mdXPld{BGT0[UIIDoc5NxcG:{eXzheIlwdiC{ZYH1bZJm\CCKQj3FS2Yh\nWwY4Tpc44> MX2yN|Y5PjRzNh?=
MMQ  NIX2TFJHfW6ldHnvckBCe3OjeR?= MYCwMVYzPSCwTR?= NVLKfFBkPzJiaB?= MmDp[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiZYP0do9o\W5icnXj[ZB1d3JvzsGgLGVT|rFr NIHrUIkzOzV{M{O1Oy=>
H1975  NHLoRZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnZNE4{OTJ3LUGwJO69VQ>? NYKwOolRPiCm NG\rVGJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NEX5VowzOzN7OUm1Oy=>
H1975  NFPxWG9CeG:ydH;zbZMhSXO|YYm= MVSyNFAhdk1? MlznO|IhcA>? MXnlcohidmOnczDldoxwfGmwaXKgbY5lfWOnZDDhdI9xfG:|aYO= MXOyN|M6QTl3Nx?=
MCF-7  NXK5ZlRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrNTGgyOC9zMECvNVAxOCCwTR?= NUXsPHVZOi92L{[g[C=> NWjLbZQ1TE2VTx?= M3\nPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHLveIgh\G:|ZT2gZY5lKHSrbXWtJIRmeGWwZHXueEBu[W6wZYK= NFrWNpUzOzNzM{WwOi=>
MCF-7  MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUixNFAhdk1? NEPEPHU1KGR? MXfEUXNQ NVuweZNWcW6mdXPld{BiKGirZ3jldkBxem:yb4L0bY9vKG:oIHPlcIx{KGmwIITo[UBIOSCyaHHz[eKh MV[yN|MyOzVyNh?=
MLO-Y4  MVvGeY5kfGmxbjDBd5NigQ>? M2m0SFHDqM7:TR?= NXnVeGpbOSCq NVW0SnBJcW6qaXLpeJMhTTJvaX7keYNm\CCFeESzJIV5eHKnc4Ppc44> MmPENlMzPDdyNUe=
MCF-7 NUfJV2t7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\ZRZloOTByIH7N MYe0PEBp NXe5VnlO[WK{b3fheIV{KHSqZTDwdo9tcW[ncnH0bZZmKGWoZnXjeEBw\iCvb3TldoF1\SCwaYTyc5NifGm4ZTDzeJJme3N? MnXnNlMzOTZ5NES=
TG1-1  NEPQe5lHfW6ldHnvckBCe3OjeR?= M2DBW|HDqM7:TR?= MnjtNlQhcA>? M3[1WYFjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhUEmILUJOtS=> MYOyN|A5QDZyNx?=
TG1-1  M3q4OWZ2dmO2aX;uJGF{e2G7 NVrQS|JROcLizszN NIPzflAzPCCq M{\jfYFjem:pYYTld{BGOsLiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhWEl|Sx?= M3j3T|I{ODh6NkC3
MCF7 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKxNFAhdk1? M4j2PVQ5KGh? M{XNUYxm[WS|IITvJIEhe2mvaXzhdkBtd3O|IHnuJJN2en[rdnHsJIF{KHerdHig[I95d3K3YnnjbY4h[WyxbnW= MUeyN|A4PzJ2OR?=
MCF7 MnjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPsWpMyODBibl2= MW[0PEBp MULlcohidmOnczDueZRtcW5vbXXkbYF1\WRiY3XscEBl\WG2aB?= MVWyN|A4PzJ2OR?=
MCF-7  MlruSpVv[3Srb36gRZN{[Xl? NFm2RVI3KGh? NHH6c4hFVVOR MoHaZZR1\W63YYTld{B1cGViZnz1[IlwgG:waXytJI9zKG[nbnjlfIFucWRvaX7keYNm\CCrbnPy[YF{\SCrbjDtbXIuOjFiZYjwdoV{e2mxbh?= MknqNlMxPTJyM{[=
MCF-7 M2HQdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmxNFAhdk1xMTFOwG0> MorjOUBl NF;hc3VqdmirYnn0d{B1cGVic4TpcZVt[XSrb36gc4YhOTgQsj3ld5Rz[WSrb3y= MWiyNlk5Ojd4NR?=
MCF-7 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnuXJo4OTByIH7N MX:1JIQ> M1zWWYlvcGmkaYTzJJRp\SC|dHnteYxifGmxbjDv[kBnfXOjcnnlcIlvKEh? NIPY[4EzOjl6Mke2OS=>
1471.1 MVLGeY5kfGmxbjDBd5NigQ>? NIHB[5UyODBibl2= MlLFNUBp NHvKOXpGfE:KwrC= NX:0c41UfGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv NYD4NW9SOjJ6NkmxNFY>
MCF-7 MYDGeY5kfGmxbjDBd5NigQ>? NWTkZ|JvOTByIH7N NUL3cnBWOSCq NXjDbIY2TXSRSNMg MoHpeIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu MV[yNlg3QTFyNh?=
HeLa MlK4SpVv[3Srb36gRZN{[Xl? NIC4NnAyODBibl2= MWOxJIg> NYH6[nNUTXSRSNMg MnnGeIFs\XNib36gZUBxfW6ldHH0[UB{fGGrbnnu[{Bx[XS2ZYLu MmD1NlI5PjlzME[=
COS-7  NWrnUoZbTnWwY4Tpc44hSXO|YYm= MYCxNFAhdk1? MX[xJIg> NHLR[lVGfE:KwrC= NUe2cox1fGGtZYOgc44h[SCydX7jeIF1\SC|dHHpcolv\yCyYYT0[ZJv Ml\5NlI5PjlzME[=
BG1L-OHTLT  NV3jeWRlTnWwY4Tpc44hSXO|YYm= Ml;1NVDDqG6P NYHR[FFqOjUEoHlCpC=> MYXpcohq[mm2czDFVu6yKGW6cILld5Nqd25? M1PpU|IzPjV{NUW4
BG1L-ICILT M1\mTmZ2dmO2aX;uJGF{e2G7 NVL6NHNROTEEoH7N MV[yOOKhcMLi NICyT4NqdmirYnn0d{BGWs7zIHX4dJJme3Orb36= NUn1S5R[OjJ4NUK1OVg>
PC-9 M4j3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1n1S|AvODB|LUOwJO69VQ>? MVO0PEBp Ml3xbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3\hPFIzPTZyNkO0
H1650 NH:yOlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV2wMlAxOy1|MDFOwG0> MWC0PEBp M1HxfIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGDLW|AzOjV4ME[zOC=>
H1975 M1LxV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjhTnUxNjByMz2zNEDPxE1? MYS0PEBp NF;T[I9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M2S0TVIzPTZyNkO0
H1975 MWLGeY5kfGmxbjDBd5NigQ>? MWizxsDPxE1? NVLjeFI2OyCq MVHhZpJw\2G2ZYOgeIhmKHCqb4PwbI8uTUeIUjDpcoR2[3Srb36gZpkh\XO2cn;n[Y4> NHLv[mUzOjV4ME[zOC=>
H1975 MVvGeY5kfGmxbjDBd5NigQ>? NELJd3A{yqEQvF2= M4nMZ|ch\A>? NEfVNHNqdmS3Y3XzJGVITlJiZYjwdoV{e2mxbh?= NFTLPXUzOjV4ME[zOC=>
HTR-8 MXjGeY5kfGmxbjDBd5NigQ>? NGPoRlUyyqEQvF2= M2HpWVEuPDhiaB?= NHjDeHZld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDJS2ZDWDdibWLORS=> M2Hz[|IzOzh|MUGx
JEG-3 M4\qcmZ2dmO2aX;uJGF{e2G7 MWixxsDPxE1? MmrZNU01QCCq NWq0fnZR\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gTWdHSlB5IH3SUmE> NULGeJdjOjJ|OEOxNVE>
Huh7 NW\FPZZoTnWwY4Tpc44hSXO|YYm= M{fU[FUxyqEQvF2= MWq0PEBp NX7aUlJEcW6qaXLpeJMh\2WwaYP0[YlvNW2nZHnheIVlKFCRTkGgeJJidnOjY4TpeoF1cW:w MlqzNlI{ODR{OU[=
201T M4nXemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:4epFoPSEQvF2= MYC3NkBp MXTpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIghfmGwZHX0ZY5q[g>? M3X1UFIzOjV6NEe2
A549  NIT4OGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe5VJpjPSEQvF2= Mn63O|IhcA>? MYnpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7IHPvcYJqdmWmIIfpeIghfmGwZHX0ZY5q[g>? Mkn1NlIzPTh2N{[=
MCF-7 MVPGeY5kfGmxbjDBd5NigQ>? M4LBR|HDqM7:TR?= Mnz5NlQhcMLi MoLj[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uJIlv\HWlZXSgZpkhPC2RSD3UJOKh NVfrTnZuOjJyNEmzNVY>
HCC-1428 NUDDTVFjTnWwY4Tpc44hSXO|YYm= Mkj0NeKh|ryP NGryc4ozPCCqwrC= M4HUO4Rwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvckBqdmS3Y3XkJIJ6KDRvT1itWEDDqA>? NILoT4QzOjB2OUOxOi=>
MDA-361 NVH1[44{TnWwY4Tpc44hSXO|YYm= M3rLdlHDqM7:TR?= NUjIN3ptOjRiaNMg NHTjVYFld3ewcnXneYxifGW|IFXSJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSB2LV;IMXQhyqB? NHu2S5ozOjB2OUOxOi=>
ZR75-1 NH72emJHfW6ldHnvckBCe3OjeR?= MWWxxsDPxE1? NY\QZZBqOjRiaNMg NWX0Z3J2\G:5boLl[5Vt[XSnczDFVkBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliND3PTE1VKMLi MmTmNlIxPDl|MU[=
MCF-7 NHTXb|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XVVVHDqM7:TR?= NX;HdZhJPS1zMDDk M{TPS5N2eHC{ZYPz[ZMhTTJvaX7keYNm\CCpcn;3eIghcW6qaXLpeIlwdg>? NXP2SlRtOjJyNEmzNVY>
HCC-1428 NES5PWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnENeKh|ryP NXqze4Z1PS1zMDDk NXTBfotLe3WycILld5NmeyCHMj3pcoR2[2WmIHfyc5d1cCCrbnjpZol1cW:w NIP0VIEzOjB2OUOxOi=>
MDA-361 MonCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1m5PVHDqM7:TR?= NVLkcXdVPS1zMDDk MmDLd5VxeHKnc4Pld{BGOi2rbnT1Z4VlKGe{b4f0bEBqdmirYnn0bY9v Ml3KNlIxPDl|MU[=
ZR75-1 MkXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mon4NeKh|ryP NW[3UWJ3PS1zMDDk NHzS[4F{fXCycnXzd4V{KEV{LXnu[JVk\WRiZ4Lve5RpKGmwaHnibZRqd25? MlnJNlIxPDl|MU[=
MCF-7/AC-1 NFvWZndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrMXZQzOC1yLkKg{txO NHvheJg3KGR? M{\zOIlvcGmkaYTzJINmdGxiZ4Lve5RpKG2xZHXzeIx6 MUKyNlA1Ojd7Mh?=
MCF7 Ml7pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTLb3V2OTBiwsXN NV;xe5p3PDhiaB?= MljNbY5lfWOnczDj[YxtKGmwaHnibZRqd25id3jpZ4gh[2GwIHLlJIVvcGGwY3XkJIJ6KG[rYoLvZoxie3S| M4DIWFIzODRzOEi3
MMQ NUfNRnBvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorkNE03OjVibl2= M1TiUVczKGh? NXvSdYt4eHKxZIXj[ZMhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbtMg MVSyNlAyPTFyMR?=
MMQ NHzaSW1HfW6ldHnvckBCe3OjeR?= NX3LO5F6OC14MkWgcm0> NInJZ3E4OiCq M1viN5Bzd2S3Y3XzJIEhe3SjdHnzeIlk[WyueTDzbYdvcW[rY3HueEwh\G:|ZT3k[ZBmdmSnboSgdoVlfWO2aX;uJIlvKFCUTDDz[YNz\XSrb36= MlfLNlIxOTVzMEG=
MCF7 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3lNE0yKM7:TR?= MoPzNlQuOTJyIHi= MnSybY5pcWKrdIOgeIhmKGe{b4f0bEBw\iCPQ1[3MXlDNTIEoB?= Mkn2NlE5PjN{NUi=
HepG2 M{WzcGFxd3C2b4Ppd{BCe3OjeR?= MoniNE4yyqEQvF2= NFPmeYMzPCCq M2npZ4Fjd2yrc3jld{B1cGViZYP0do9o\W5vaX7keYNm\CC3cD3y[Yd2dGG2aX;uJI9nKGGyb1HJJIFv\CCjcH;N M4\zU|IyQDF4MkOz
MCF7–iFR3 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjLRlIzOC1zMECgcm0> NXzufWE3QTZiaB?= NXjOXm13\W6qYX7j[ZMhSVBvaX7keYNm\CClZXzsJIdzd3e2aDDpcohq[mm2aX;u M2Po[VIyPzl{OEi5
MCF7S NXfUZmxFTnWwY4Tpc44hSXO|YYm= Mny1NeKh|ryP MVu0PEBp M3\YRoRwf26{ZXf1cIF1\XNib4\ldoFtdCCHUt8xJJBzd3SnaX6gcIV3\Wy| NE\2UG8zOTV|M{G5OS=>
MCF7 M4f3OmZ2dmO2aX;uJGF{e2G7 NUfSOpliOcLizszN NWnoPGU4PDhiaB?= NGWwVGhld3ewcnXneYxifGW|IH;2[ZJidGxiRWNOtUBxem:2ZXnuJIxmfmWucx?= NXzISIhsOjF3M{OxPVU>
MCF7S MXnGeY5kfGmxbjDBd5NigQ>? NFjrZVIyyqEQvF2= NHj3VHE4KGR? NFTxSWZifHSnboXheIV{KHS3bX;yd5Bp\XKnIH\vdo1ifGmxbjDhcoQheHKxbHnm[ZJifGmxbh?= M1:3elIyPTN|MUm1
MCF7S NUTq[5hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTTNE42NzFizszN MXG3JIQ> NH\ueYdFVVOR MoCy[IVkemWjc3XzJINmdGxiZYjwZY5{cW:w NUfid2ZYOjF3M{OxPVU>
T47D  NXXGNpBzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL3fow1KG6P MXy0NEBp M37C[5N2eHC{ZYPz[ZMh[2WubDDndo94fGhibX;k[ZJifGWueR?= NXHTUFlPOjF2OECzPVE>
BT474  Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUi0JI5O MUC0NEBp MnvTd5VxeHKnc4Pld{Bk\WyuIHfyc5d1cCCvb3TldoF1\Wy7 NXjuZ2I6OjF2OECzPVE>
T47D  NXfLblR4TnWwY4Tpc44hSXO|YYm= MoLhNVAhdk1? MY[0NEBp M3jQN4Rwf26{ZXf1cIF1\XNiRWNOtUBxem:2ZXnu M4ryUVIyPDhyM{mx
BT474  MonkSpVv[3Srb36gRZN{[Xl? M3\RfVExKG6P NWe1N5A1PDBiaB?= NFHtWJhld3ewcnXneYxifGW|IFXS{tEheHKxdHXpci=> NUP3e4ZKOjF2OECzPVE>
MCF7 NHLU[ndHfW6ldHnvckBCe3OjeR?= NIPlcFIyODBibl2= MX23JIQ> NYG4UpF{emWmdXPld{BGWs7zIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? M1zrfVIyOzl4MEm0
T47D  MUDGeY5kfGmxbjDBd5NigQ>? MWWxNFAhdk1? NHT0UXo4KGR? M2HESJJm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> M{DqflIyOzl4MEm0
BT474  MV7GeY5kfGmxbjDBd5NigQ>? NGjhUIYyODBibl2= NH;rbWM4KGR? Ml6ydoVlfWOnczDFVu6yKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> MmPyNlE{QTZyOUS=
MDAMB361 MXrGeY5kfGmxbjDBd5NigQ>? NFLQcIgyODBibl2= NH;ZeZk4KGR? M4rNOZJm\HWlZYOgSXLPuSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> M2GwWlIyOzl4MEm0
MCF7 M{\Se2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPkNE4xOS1zIN88US=> MoixO{Bl Mm\4doVlfWOnczDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M{jIfFIyOzl4MEm0
T47D  MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1z1Z|AvODFvMTFOwG0> MoHYO{Bl NH\OZW5z\WS3Y3XzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MnPyNlE{QTZyOUS=
BT474  NYC2cHB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUOwMlAyNTFizszN NVjMTpJvPyCm MUDy[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? MUWyNVM6PjB7NB?=
MDAMB361 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TyWVAvODFvMTFOwG0> NVHkeIU3PyCm MX;y[YR2[2W|IHPlcIwh\3Kxd4ToJJNq\26rZnnjZY51dHl? MVyyNVM6PjB7NB?=
MCF7 NVexeY9xTnWwY4Tpc44hSXO|YYm= MnrkNVAxKG6P MlLEO{Bl NYD0eJBCcW6mdXPld{Bw\iCHcnLCN{BidmRiRYLiRlQhemWlZYD0c5Ih\XiycnXzd4lwdiCjbnSgd4lodmGubHnu[y=> MU[yNVM6PjB7NB?=
T47D  NET4NXJHfW6ldHnvckBCe3OjeR?= MX:xNFAhdk1? NHfIS5g4KGR? NFXqZW5qdmS3Y3XzJI9nKEW{YlKzJIFv\CCHcnLCOEBz\WOncITvdkBmgHC{ZYPzbY9vKGGwZDDzbYdv[WyuaX7n NV7zXHA5OjF|OU[wPVQ>
BT474  MlrjSpVv[3Srb36gRZN{[Xl? M3[4cVExOCCwTR?= MlnjO{Bl MkLqbY5lfWOnczDv[kBGemKEMzDhcoQhTXKkQkSgdoVk\XC2b4Kg[ZhxemW|c3nvckBidmRic3nncoFtdGmwZx?= NHnuZ3QzOTN7NkC5OC=>
MDAMB361 MljhSpVv[3Srb36gRZN{[Xl? MmLPNVAxKG6P NWO3ZY9EPyCm M4\wSYlv\HWlZYOgc4YhTXKkQkOgZY5lKEW{YlK0JJJm[2WydH;yJIV5eHKnc4Ppc44h[W6mIIPp[45idGyrbne= MWWyNVM6PjB7NB?=
MCF7 NX\xZ|lxTnWwY4Tpc44hSXO|YYm= M2rvTlExKG6P NVK0ZYhoQTZiaB?= M3XrZ4Rwf26{ZXf1cIF1\XNiRWKg[ZhxemW|c3nvcuKh MlPxNlE{Pzh|M{O=
MDA-MB-231 MlTVSpVv[3Srb36gRZN{[Xl? MUOxNEBvVQ>? MVy5OkBp Mke2[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uxsA> MXqyNVM4QDN|Mx?=
SK-BR-3 M1nNdGZ2dmO2aX;uJGF{e2G7 MXqxNEBvVQ>? NWLFeVZCQTZiaB?= MkDY[I94dnKnZ4XsZZRmeyCHUjDlfJBz\XO|aX;uxsA> NFHtRlkzOTN5OEOzNy=>
MCF-7 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfTTocyODBibl2= MkLDO|IwQTZiaB?= M1XwNYNifXOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M{nxS|IyOjl7OE[y
MMQ M3PUZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPLbnVnOC5yMEitOlI2KG6P NUnad29GPzJiaB?= NWP3foYzcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZo91cCC2aX3lMUBidmRiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M3H6V|IxPzByN{W1
MMQ Mo[3SpVv[3Srb36gRZN{[Xl? MoT4NE4xODhvNkK1JI5O NYLRemdVPzJiaB?= NYfSXHRxcW6qaXLpeJMhWFKOIIPlZ5JmfGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NHr5dlEzODdyMEe1OS=>
MMQ NWS4VY9jTnWwY4Tpc44hSXO|YYm= Ml;PNE4xPC14MkWgcm0> MUS3NkBp MnLXbY5pcWKrdIOgSXLPuSCneIDy[ZN{cW:w MW[yNFcxODd3NR?=
MMQ MX7GeY5kfGmxbjDBd5NigQ>? MoHFNE4xPC14MkWgcm0> MWK3NkBp MWj1dJJm\3WuYYTld{BVT0cQskOgZY5lKFSJRt8yVmlKKGW6cILld5Nqd25? M2S1SlIxPzByN{W1

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験: [1]
- 合併
  • 細胞株: MCF-7 breast cancer cells
  • 濃度: 2.9 nM
  • 反応時間: 5 days
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[6]
- 合併
  • 動物モデル: The human breast cancer xenografts MCF-7 in nude mice
  • 投薬量: 5 mg/mouse
  • 投与方法: s.c. injection
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (164.8 mM)
Water Insoluble
Ethanol ''100 mg/mL warmed ''100
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
0.4mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 606.77
化学式

C32H47F5O3S

CAS No. 129453-61-8
Storage powder
in solvent
別名 ICI-182780, ZD 9238
Smiles CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04524000 Not yet recruiting Drug: Alpelisib|Drug: Fulvestrant Advanced Breast Cancer Novartis Pharmaceuticals|Novartis October 1 2020 Phase 2
NCT04483505 Not yet 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. October 1 2020 Phase 1
NCT04300790 Not yet recruiting Drug: Alpelisib|Drug: Metformin|Drug: Fulvestrant Breast Cancer MedSIR|Novartis June 30 2020 Phase 2
NCT04024436 Recruiting Drug: TAS-120|Drug: Fulvestrant Metastatic Breast Cancer|FGFR2 Amplification Taiho Oncology Inc. December 15 2019 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問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.

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Estrogen/progestogen Receptor Inhibitors with Unique Features

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Tags: Fulvestrantを買う | Fulvestrant ic50 | Fulvestrant供給者 | Fulvestrantを購入する | Fulvestrant費用 | Fulvestrant生産者 | オーダーFulvestrant | Fulvestrant化学構造 | Fulvestrant分子量 | Fulvestrant代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID