Enzalutamide (MDV3100)

For research use only. Not for use in humans.

製品コードS1250

Enzalutamide (MDV3100)化学構造

CAS No. 915087-33-1

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

サイズ 価格(税別)  
JPY 26900
JPY 46800
JPY 129800
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製品安全説明書

Androgen Receptor阻害剤の選択性比較

生物活性

製品説明 Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
ターゲット
Androgen Receptor [1]
(LNCaP cells)
36 nM
体外試験

Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[18F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys). [1] Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human LNCAP M37EfmN6fG:2b4jpZ{BCe3OjeR?= NECyUYk4KGSjeYO= MWq5OUUhTXSRSB?= NXTvVJdFUUN3ME21MlEzKM7:TR?= M3SyTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{GzOVY4Lz5{M{exN|U3PzxxYU6=
human LNCAP MYrGeY5kfGmxbjDBd5NigQ>? MojFNUDPxE1? M4[yTmROW09? Ml75TY5pcWKrdIOgdJJwe3SjdHWgd5Bm[2moaXOgZY51cWenbjDz[YNz\XSrb36gbY4hcHWvYX6gUG5ESVBiY3XscJMh\XiycnXzd4lv\yCjbnTyc4dmdiC{ZXPldJRweiCjdDCxNFAuOTByMH7N MoK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB{MUi3NVcoRjJyMkG4O|E4RC:jPh?=
VCaP NYPhZnhsTnWwY4Tpc44hSXO|YYm= NVzyNGppOTBizszN MknSNlQhcA>? NHfuWW5FVVOR NYXwd5MzW3WycILld5NmeyCuaXfhcoQudWWmaXH0[YQhSVJvRlygd4lodmGuaX7n NFXiSlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkexNFQ{Pid-MkK3NVA1OzZ:L3G+
BCK4 M4O2PGZ2dmO2aX;uJGF{e2G7 M{nnclExKM7:TR?= MYW3JIRigXN? MYXEUXNQ Mm\xTY5pcWKrdIOg[ZN1emGmaX;sMY1m\GmjdHXkJJBzd2yrZnXyZZRqd25? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR3MUGwPUc,OjR2NUGxNFk9N2F-
MCF7s NIrZdVJHfW6ldHnvckBCe3OjeR?= NUnoTGdMOTBizszN NEW1UI83KGSjeYO= NInQV|ZFVVOR NFv0OoJKdmirYnn0d{Bme3S{YXTpc4wudWWmaXH0[YQheHKxbHnm[ZJifGmxbh?= NYnQSVRRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OVEyODlpPkK0OFUyOTB7PD;hQi=>
PC-3 NV60eHZoTnWwY4Tpc44hSXO|YYm= MoLnNVAh|ryP M3vlOVczKGh? MXfEUXNQ NIPKVllFd2W|IH7veEBqdmirYnn0JINmdGxicILvcIln\XKjdHnvci=> MlHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NES4OlQoRjJ3M{S0PFY1RC:jPh?=
CWR22Rv1 Mm\QSpVv[3Srb36gRZN{[Xl? NXmxXZlvOTVizszN M{PxO|I1KGh? Mn\iSG1UVw>? M2q0WGRw\XNibn;0JIFn\mWldDD0bIUh\nWubDDs[Y5ofGhiQWKg[ZhxemW|c3nvci=> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdzM{W2O{c,OjN5MUO1Olc9N2F-
LNCAP/AR MlLoRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NYTodZBtUUN3MDC9JFAvODJzIN88US=> NF\hVos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{exO|U1PCd-Mke3NVc2PDR:L3G+
MDA-MB-453 Mn61RY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NH3vbHpGSzVyIE2gNE4xPDlizszN MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdzM{W2O{c,OjN5MUO1Olc9N2F-
LNCAP MWPBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 MVu3NkBp NG\iN5BKSzVyIE2gNE4xPSEQvF2= NXTmNYE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxPVMzOTVpPkOwNVk{OjF3PD;hQi=>
LNCAP MWTBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 MYm3NkBp Mm\qTWM2OCB;IECuNFkh|ryP MmPxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzOUOyNVUoRjNyMUmzNlE2RC:jPh?=
LNCAP M1zHcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFnBPYZIUTVyIE2gNE4yOiEQvF2= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDBzMUKxPUc,OjhyMUGyNVk9N2F-
LNCAP M4nCbmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M2jaU|Mh\GG7cx?= NYS5N4o1UUN3MDC9JFAvOTJ5MTFOwG0> M3K2d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MES2N|E{Lz5{NkC0OlMyOzxxYU6=
LNCAP MUfBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 NE[xUWw3KGSjeYO= MmTKS2k2OCB;IECuNlkh|ryP M3LsWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEGxNlE6Lz5{OECxNVIyQTxxYU6=
UAS-bla GripTite 293 M1TiemFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= MUSxOkB1dyB{NDDo NVfIfG9NUUN3MDC9JFAvOzZzIN88US=> NIjqVZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OwNVM3QCd-MkezNFE{Pjh:L3G+
mammalian expression system MUfBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 MUeyNkB1dyB{NDDo MknpSWM2OCB;IECuOFIh|ryP MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDN6NUWwN{c,Ojh|OEW1NFM9N2F-
VCaP NVrveIloT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEXU[5QyPDRiaB?= MnG2S2k2OCB;IECuOlEh|ryP M{LMc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUKxOVg3Lz5{NUGyNVU5PjxxYU6=
LNCaP MWHBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 M37YXFIhcA>? MmjISWM2OCB;IECuPVE2KM7:TR?= M{PkOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{GzOVY4Lz5{M{exN|U3PzxxYU6=
COS7 NXvze3U{SW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> NVrsfHpEOjRiaB?= MX7JR|UxKD1iMT6yOkDPxE1? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFzN{i5O{c,OjlzMUe4PVc9N2F-
AR LBD mutant NHPie|dCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 MkL3OEBp MW\JR|UxKD1iMT6zOUDPxE1? Ml3HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PFkoRjJ5OEGwOVg6RC:jPh?=
LNCAP NGnWTHhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3vCSGdKPTBiPTCyMlg5KM7:TR?= NHW2OoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOFE{OCd-MkW2N|QyOzB:L3G+
CWR22Rv1 NHj0UmlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUfHTVUxKD1iMz6zOEDPxE1? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ|NEGzNEc,OjV4M{SxN|A9N2F-
LNCAP MYDDfZRwfG:6aXPpeJkh[XO|YYm= MVq3JIRigXN? MV\HTVUxKD1iNT6xNkDPxE1? NUHwXndRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
PC3 M4HqOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVjrd|AyT0l3MDC9JFkvOTVizszN NHvF[3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOFE{OCd-MkW2N|QyOzB:L3G+
CWR22Rv1 MoriR4VtdCC|dYL2bZZidCCjc4PhfS=> M1PyTVE1PCCq M3;Be2lEPTBiPTC5Mlch|ryP MkHFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMkG1PFYoRjJ3MUKxOVg3RC:jPh?=
LNCAP MYXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NYnrb2dDQTZiaB?= NIHkS4hKSzVyIE2gNVEvPDdizszN MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzNyMUO2PEc,Ojd|MEGzOlg9N2F-
LNCaP-hr MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MWmzJIRigXN? NGS5b|ZKSzVyIE2gNVIvPSEQvF2= NHHJRo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU5QSd-Mke4NVA2QDl:L3G+
LNCAP NX\oZXJzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MVizJIRigXN? MnTJTWM2OCB;IEGyMlUh|ryP M3:yPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUG3PFk4Lz5{OUGxO|g6PzxxYU6=
LNCaP MofVRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= MoT0NVQ1KGh? M2TkdmdKPTBiPTCxPE45QCEQvF2= NXewc4d4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyO|I5QTRpPkK4NlczQDl2PD;hQi=>
LNCaP-AR NY\2XXBYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUWxOFQhcA>? M4nrXmdKPTBiPTCxPE46KM7:TR?= NEnSNZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyNVU5Pid-MkWxNlE2QDZ:L3G+
C4-2B NIW5NYtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NVXsflJZOTJiaB?= M1HNeWlEPTBiPTCyNE44PyEQvF2= MojDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NUi1NVgoRjJ7N{W4OVE5RC:jPh?=
A31 MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3vQUVczKGh? NVntdpltT0l3MDC9JFI4NjVizszN MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDBzMUKxPUc,OjhyMUGyNVk9N2F-
22Rv1 MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MmLDPVYhcA>? MXPJR|UxKD1iM{GuO|Yh|ryP NIrR[JE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OwNVM3QCd-MkezNFE{Pjh:L3G+
22Rv1 NGDuSHVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NGrYSmY6PiCq M1n2O2lEPTBiPTCzNU44PiEQvF2= Mk\aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7NkW4OlIoRjJ4OU[1PFYzRC:jPh?=
DU145 MnTWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MlXDPVYhcA>? M3vmOWlEPTBiPTCzNk4zPyEQvF2= MoHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
LNCAP NFqyNpFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MVO3NkBp MY\JR|UxKD1iM{OuPFQh|ryP NVnteYhKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OFgyOzlpPkK5OFQ5OTN7PD;hQi=>
CW22Rv1 MkLTRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NV\0d5dMPzJiaB?= Ml6xTWM2OCB;IEO1Mlc2KM7:TR?= NHTRboE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK3Nlg6PCd-MkiyO|I5QTR:L3G+
22Rv1 MnT6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M4PvXFczKGh? NFizTJFKSzVyIE2gN|YvPjZizszN MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2OEGzPUc,Ojl2NEixN|k9N2F-
22Rv1 NELuT|RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MVmxNkBp MXXJR|UxKD1iM{[uOlYh|ryP M2\aWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{W4OVE5Lz5{OUe1PFUyQDxxYU6=
LNCAP NUjTdFFQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M4PWRlEzKGh? NFe2NXNKSzVyIE2gOFIvOzdizszN NXO4d2ZXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVg2OThpPkK5O|U5PTF6PD;hQi=>
DU145 M1[1PGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NWnyXXY{OyCmYYnz M2P2PWlEPTBiPTC0Ok4yKM7:TR?= MluzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PFkoRjJ5OEGwOVg6RC:jPh?=
DU145 NFfxR41CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NFvSV5k{KGSjeYO= MXPJR|UxKD1iNE[uNUDPxE1? NWCzV|VtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNVc5QTdpPkK5NVE4QDl5PD;hQi=>

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
AR-FL / AR-v7 / pAR(S213) / pAkt(S473) / pMdm2(S166); 

PubMed: 26378044     


LNCaP95 (LN95) cells were maintained in medium containing 5% CSS and then treated with 5μM of enzalutamide (ENZ) for 0-24 hours. Whole cell lyses were extracted. AR-FL, AR-v7, phosphor-AR(ser213), phosphorAkt(ser473), total Akt, total PP-1, phosphor-Mdm2(ser166), total Mdm2 and β-actin were measured by immunoblotting.

AR / ERG / NOTCH1 / PSA / Cleaved PARP1 / Cleaved caspase 7; 

PubMed: 28607007     


Treatment of VCaP cells with NOTCH inhibitor, GSI-1, in combination with Enzalutamide (Enz) augmentes its effects on the inhibition of AR, ERG, PSA, NOTCH1 and NOTCH2 expression and induces cleavage of PARP1 and Caspase 7

CXCR7; 

PubMed: 29277895     


Western blotting is used to analyze CXCR7 protein levels in VCaP and C4-2B cells.

26378044 28607007 29277895
Growth inhibition assay
Cell proliferation; 

PubMed: 28115200     


Proliferation of the LNCaP prostate cancer cell line, the Ramos Burkitt's cell line, and the Granta, Jeko-1, Rec-1 and Maver-1 MCL cell lines plated in charcoal stripped serum for 96 hours in the absence or presence of enzalutamide (10uM). Data are representative of 3 independent experiments.

28115200
Immunofluorescence
CXCR7; 

PubMed: 29277895     


Immunofluorescence staining is used to analyze CXCR7 protein levels in prostate cancer cells.

pAKT(S473); 

PubMed: 27588408     


Representative immunofluorescent images of subcellular localization of pAKT S473 expression in PC3 cells expressing AR-V7 that were treated with vehicle control (Ctrl), enzalutamide, ISA-2011B and combination of enzalutamide and ISA-2011B (ENZ+ISA2011B). The cancer cells are indicated by the arrows.

AR; 

PubMed: 27588408     


Representative immunofluorescent images show the expression and subcellular localization of AR in 22Rv1 cells overexpressing PIP5K1α that were treated with vehicle control, enzalutamide, ISA-2011B and combination of enzalutamide and ISA-2011B.

29277895 27588408
ELISA
osteoprotegerin; 

PubMed: 27015557     


MDA-MB-231 cells were treated with 10 μM enzalutamide or vehicle for 48 hours. Levels of OPG (osteoprotegerin) in the supernatant of MDA-MB-231 cells as determined by ELISA. Data are representative of 2 independent experiments.

27015557
体内試験 Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[3]
- 合併

AR reporter assay:

Enzalutamide is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of Enzalutamide is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to Enzalutamide treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of Enzalutamide. After two days of incubation, reporter activities are assayed.
細胞試験: [1]
- 合併
  • 細胞株: LNCaP or LNCaP/AR cells
  • 濃度: 0-10 μM
  • 反応時間: 1-4 days
  • 実験の流れ: Enzalutamide is diluted in DMSO. LNCaP or LNCaP/AR cells (104 cells/well) are androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells are challenged with various concentrations of Enzalutamide in media containing 5-10% charcoal-stripped serum.
    (参考用のみ)
動物試験:[1]
- 合併
  • 動物モデル: Castration-resistant LNCaP/HR xenografts in male SCID mice
  • 投薬量: 10 mg/kg
  • 投与方法: Administered via gavage daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 92 mg/mL (198.08 mM)
Water Insoluble
Ethanol Insoluble

* 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 464.44
化学式

C21H16F4N4O2S

CAS No. 915087-33-1
Storage powder
in solvent
別名 N/A
Smiles CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C

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SDS/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SDS/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
NCT04335682 Recruiting Drug: Darolutamide|Drug: Enzalutamide Metastatic Prostate Cancer|Prostate Cancer Metastatic|Prostate Cancer|Castrate Resistant Prostate Cancer Alliance Foundation Trials LLC.|Bayer August 17 2021 Phase 2
NCT04655365 Not yet recruiting Drug: Enzalutamide capsule Prostate Cancer CHU de Quebec-Universite Laval|Astellas Pharma Europe Ltd. January 4 2021 Phase 2
NCT04475601 Terminated Drug: Enzalutamide Pill COVID-19|Corona Virus Infection Andreas Josefsson|Umeå University|Sahlgrenska University Hospital Sweden|University Hospital Umeå|Uppsala University Hospital|Skane University Hospital|Jonkoping County Hospital|Sundsvall Hospital|Helsingborgs Hospital|Göteborg University|Astellas Pharma Europe Ltd.|Norrlands University Hospital|Västerbotten County Council July 15 2020 Phase 2
NCT04456049 Not yet recruiting Drug: Enzalutamide COVID-19 Infection Ricardo Pereira Mestre|Oncology Institute of Southern Switzerland|Institute of Oncology Research|Institute for Research in Biomedicine|Ente Ospedaliero Cantonale Bellinzona July 2020 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

Androgen Receptorシグナル伝達経路

Androgen Receptor Inhibitors with Unique Features

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