Enzalutamide (MDV3100)

For research use only. Not for use in humans.

目录号:S1250 中文名称:恩杂鲁胺

Enzalutamide (MDV3100) Chemical Structure

CAS No. 915087-33-1

Enzalutamide (MDV3100)是一种androgen-receptor (AR)拮抗剂,在 LNCaP细胞中IC50为36 nM。研究证明 Enzalutamide 可促进自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2444.41 现货
RMB 1221.51 现货
RMB 2224.43 现货
RMB 6297.61 现货
RMB 16298.1 现货
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产品安全说明书

Androgen Receptor抑制剂选择性比较

生物活性

产品描述 Enzalutamide (MDV3100)是一种androgen-receptor (AR)拮抗剂,在 LNCaP细胞中IC50为36 nM。研究证明 Enzalutamide 可促进自噬。
靶点
Androgen Receptor [1]
(LNCaP cells)
36 nM
体外研究

Enzalutamide是雄激素受体(AR)拮抗剂,IC50为36 nM。在加入16β-[18F]氟-5α-DHT (18-FDHT)的竞争性实验中发现作用于AR时Enzalutamide比bicalutamide具有更高的亲和力。而Enzalutamide作用于LNCaP/AR(AR-过量表达)前列腺细胞时没有效果。在亲本LNCaP细胞中,Enzalutamide抑制前列腺特异性抗原(PSA)和跨膜丝氨酸蛋白酶2(TMPRSS2) 的产生,及抑制它们与合成的雄激素R1881 结合。Enzalutamide可抑制突变AR蛋白(W741C, 741位上的Trp突变为Cys)的翻译活性。[1]MDV310也阻断核转位和配位受体复合物招募辅激活因子。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human LNCAP M3r2RmN6fG:2b4jpZ{BCe3OjeR?= NGPuZ4Y4KGSjeYO= Ml;XPVUmKEW2T1i= NUnp[oFoUUN3ME21MlEzKM7:TR?= NGDQS4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exN|U3Pyd-MkO3NVM2Pjd:L3G+
human LNCAP M2fzR2Z2dmO2aX;uJGF{e2G7 MXWxJO69VQ>? MYrEUXNQ NVnVVmdLUW6qaXLpeJMheHKxc4TheIUhe3CnY3nmbYMh[W62aXflckB{\WO{ZYTpc44hcW5iaIXtZY4hVE6FQWCgZ4VtdHNiZYjwdoV{e2mwZzDhcoRzd2enbjDy[YNmeHSxcjDheEAyODBvMUCwNI5O NWT3e4o3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCyNVg4OTdpPkKwNlE5PzF5PD;hQi=>
VCaP NWnlRXRZTnWwY4Tpc44hSXO|YYm= NFr0Z5QyOCEQvF2= MX:yOEBp MkXpSG1UVw>? NX\WVohUW3WycILld5NmeyCuaXfhcoQudWWmaXH0[YQhSVJvRlygd4lodmGuaX7n M{jrcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{N{GwOFM3Lz5{MkexNFQ{PjxxYU6=
BCK4 NUfLPZZoTnWwY4Tpc44hSXO|YYm= MXqxNEDPxE1? MXS3JIRigXN? MYfEUXNQ MVzJcohq[mm2czDld5Rz[WSrb3ytcYVlcWG2ZXSgdJJwdGmoZYLheIlwdg>? M3jI[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEWxNVA6Lz5{NES1NVExQTxxYU6=
MCF7s NHXOW5JHfW6ldHnvckBCe3OjeR?= Mmq5NVAh|ryP NF3TeW83KGSjeYO= M4DEPGROW09? Mmi3TY5pcWKrdIOg[ZN1emGmaX;sMY1m\GmjdHXkJJBzd2yrZnXyZZRqd25? NXHwc|VCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OVEyODlpPkK0OFUyOTB7PD;hQi=>
PC-3 MnToSpVv[3Srb36gRZN{[Xl? Mm\yNVAh|ryP MX[3NkBp NVPKOGxHTE2VTx?= NX7XS29HTG:nczDuc5QhcW6qaXLpeEBk\WyuIIDyc4xq\mW{YYTpc44> Mk\nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NES4OlQoRjJ3M{S0PFY1RC:jPh?=
CWR22Rv1 NXzm[5BmTnWwY4Tpc44hSXO|YYm= NVPkOlNFOTVizszN MnqyNlQhcA>? NGDSWFNFVVOR MmfnSI9meyCwb4SgZYZn\WO2IITo[UBnfWyuIHzlcod1cCCDUjDlfJBz\XO|aX;u Mn6xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5MUO1OlcoRjJ|N{GzOVY4RC:jPh?=
LNCAP/AR MWPBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 NIqzWpJKSzVyIE2gNE4xOjFizszN MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzdzN{W0OEc,Ojd5MUe1OFQ9N2F-
MDA-MB-453 MorkRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= M1HQWWVEPTBiPTCwMlA1QSEQvF2= NGPBeY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exN|U3Pyd-MkO3NVM2Pjd:L3G+
LNCAP NHTFPZVCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 NXXiUGR2PzJiaB?= MVfJR|UxKD1iMD6wOUDPxE1? Mn;EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzOUOyNVUoRjNyMUmzNlE2RC:jPh?=
LNCAP MWjBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 MXi3NkBp Mki4TWM2OCB;IECuNFkh|ryP M3TvPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMUmzNlE2Lz5|MEG5N|IyPTxxYU6=
LNCAP M4fnPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUHHTVUxKD1iMD6xNkDPxE1? NWTlbpNFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiwNVEzOTlpPkK4NFEyOjF7PD;hQi=>
LNCAP MlzaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MoLZN{Bl[Xm| MmrmTWM2OCB;IECuNVI4OSEQvF2= NITLVnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0OlMyOyd-Mk[wOFY{OTN:L3G+
LNCAP NWm3[lIySW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> NUj2XIt1PiCmYYnz M376UGdKPTBiPTCwMlI6KM7:TR?= NF61PZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECxNVIyQSd-MkiwNVEzOTl:L3G+
UAS-bla GripTite 293 NUnjUYtMSW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> MonGNVYhfG9iMkSgbC=> MWHJR|UxKD1iMD6zOlEh|ryP MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzNyMUO2PEc,Ojd|MEGzOlg9N2F-
mammalian expression system NYDqToZHSW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> M2DBO|IzKHSxIEK0JIg> M{jFZmVEPTBiPTCwMlQzKM7:TR?= NVy5dWdiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizPFU2ODNpPkK4N|g2PTB|PD;hQi=>
VCaP M1n0cGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX[xOFQhcA>? M{f4dWdKPTBiPTCwMlYyKM7:TR?= NUezXHVWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlE2QDZpPkK1NVIyPTh4PD;hQi=>
LNCaP NXfDSHZDSW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> NWPSSnhvOiCq M{fOeGVEPTBiPTCwMlkyPSEQvF2= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdzM{W2O{c,OjN5MUO1Olc9N2F-
COS7 MmTyRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NYXiXG4yOjRiaB?= MXfJR|UxKD1iMT6yOkDPxE1? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFzN{i5O{c,OjlzMUe4PVc9N2F-
AR LBD mutant M33kcGFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= MkjvOEBp NEHhUJpKSzVyIE2gNU4{PSEQvF2= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW4PUc,Ojd6MUC1PFk9N2F-
LNCAP M4LjbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHXuOlVIUTVyIE2gNk45QCEQvF2= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ|NEGzNEc,OjV4M{SxN|A9N2F-
CWR22Rv1 NXfpSoFYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUTHTVUxKD1iMz6zOEDPxE1? MoX3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4M{SxN|AoRjJ3NkO0NVMxRC:jPh?=
LNCAP MVLDfZRwfG:6aXPpeJkh[XO|YYm= NHroT2I4KGSjeYO= MXLHTVUxKD1iNT6xNkDPxE1? M3TQflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{GzOVY4Lz5{M{exN|U3PzxxYU6=
PC3 NVvpVG95T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmezS2k2OCB;IEmuNVUh|ryP MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ|NEGzNEc,OjV4M{SxN|A9N2F-
CWR22Rv1 MXfD[YxtKHO3co\peoFtKGG|c3H5 MXmxOFQhcA>? NYn4bW8yUUN3MDC9JFkvPyEQvF2= NHPLVIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyNVU5Pid-MkWxNlE2QDZ:L3G+
LNCAP M4T6VGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M2nLVlk3KGh? MlPuTWM2OCB;IEGxMlQ4KM7:TR?= NEDWcHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OwNVM3QCd-MkezNFE{Pjh:L3G+
LNCaP-hr NFu5fpdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MlXxN{Bl[Xm| NFL2b4VKSzVyIE2gNVIvPSEQvF2= MoG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PFkoRjJ5OEGwOVg6RC:jPh?=
LNCAP NUjZ[IxMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MlqyN{Bl[Xm| NWjKOFh2UUN3MDC9JFEzNjVizszN MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFzN{i5O{c,OjlzMUe4PVc9N2F-
LNCaP MmfmRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NYfNTlRyOTR2IHi= NX2xZWFCT0l3MDC9JFE5Njh6IN88US=> M1Tr[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkeyPFk1Lz5{OEK3Nlg6PDxxYU6=
LNCaP-AR Mnn0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFT5W5YyPDRiaB?= NEjudHZIUTVyIE2gNVgvQSEQvF2= M{XXclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUKxOVg3Lz5{NUGyNVU5PjxxYU6=
C4-2B NYn4WZQ3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NX;zbWpOOTJiaB?= M1TyZmlEPTBiPTCyNE44PyEQvF2= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd3OEWxPEc,Ojl5NUi1NVg9N2F-
A31 M{[y[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2rvdlczKGh? NUfkTHhOT0l3MDC9JFI4NjVizszN NVL0Rm02RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiwNVEzOTlpPkK4NFEyOjF7PD;hQi=>
22Rv1 NFniXIZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MUi5OkBp Mn7KTWM2OCB;IEOxMlc3KM7:TR?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzNyMUO2PEc,Ojd|MEGzOlg9N2F-
22Rv1 M1;6fmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M4KyOlk3KGh? MWPJR|UxKD1iM{GuO|Yh|ryP MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl4NUi2Nkc,OjZ7NkW4OlI9N2F-
DU145 MmHwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MVS5OkBp NYfWR5ZlUUN3MDC9JFMzNjJ5IN88US=> NGTaW2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OwNVM3QCd-MkezNFE{Pjh:L3G+
LNCAP MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MXm3NkBp MULJR|UxKD1iM{OuPFQh|ryP MoW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NEixN|koRjJ7NES4NVM6RC:jPh?=
CW22Rv1 MVTBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 MoHkO|IhcA>? M1HONWlEPTBiPTCzOU44PSEQvF2= NUDiUJVMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyO|I5QTRpPkK4NlczQDl2PD;hQi=>
22Rv1 NX;4OZRKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NWXoeHpYPzJiaB?= MV;JR|UxKD1iM{[uOlYh|ryP M13UWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NES4NVM6Lz5{OUS0PFE{QTxxYU6=
22Rv1 MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M3HkOVEzKGh? MUDJR|UxKD1iM{[uOlYh|ryP NXS2cGt1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVg2OThpPkK5O|U5PTF6PD;hQi=>
LNCAP MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NF;oSIcyOiCq MofuTWM2OCB;IESyMlM4KM7:TR?= M2fjfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{W4OVE5Lz5{OUe1PFUyQDxxYU6=
DU145 MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MkjFN{Bl[Xm| NWPRcoR2UUN3MDC9JFQ3NjFizszN MmfiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PFkoRjJ5OEGwOVg6RC:jPh?=
DU145 MnPYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NFG4WYQ{KGSjeYO= MnTUTWM2OCB;IES2MlEh|ryP MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFzN{i5O{c,OjlzMUe4PVc9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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

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.

CXCR7; 

PubMed: 29277895     


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

28607007 26378044 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
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.

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.

CXCR7; 

PubMed: 29277895     


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

27588408 29277895
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
体内研究 Enzalutamide处理携带LNCaP/AR移植瘤的阉割雄鼠,按鼠体重,每千克处理10mg MDV310,可诱导肿瘤的明显退化。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[3]
- 合并

AR受体实验:

在抗激素的前列腺癌细胞系中通过人工AR反应报告分子系统测定Enzalutamide。在这个系统中,前列腺癌LNCaP细胞稳定表达AR,表达的AR水平比体内自身产生的AR水平高5倍多。外界合成的AR和体内自身产生的AR有着相似的特性,都能稳定与合成的雄激素R1881作用。AR过量表达的细胞也能含有AR反应报告分子,这些细胞的报告分子活性显示抗激素前列腺癌的特性。在含100 pM R1881时测定Enzalutamide的抗性。LNCaP细胞供养在含有10%胎牛血清的Iscove's培养基中。在用Enzalutamide处理的前两天,细胞在含活性炭处理的胎牛血清(CS-FBS)Iscove's培养基中生长,用于除去雄激素。细胞在培养基上分裂和生长,培养基含有10% CS-FBS,100 pM R1881,及增加浓度的Enzalutamide。温育两天后,测定报告分子活性。
细胞实验:[1]
- 合并
  • Cell lines: LNCaP或LNCaP/AR细胞
  • Concentrations: 10 μM 左右
  • Incubation Time: 1-4天
  • Method: 用DMSO稀释Enzalutamide。LNCaP或LNCaP/AR细胞(104细胞/每孔)缺乏雄激素,在含有5-10%活性炭处理的血清培养基上生长3到5天。然后在5-10%活性炭处理的血清培养基中加入不同浓度(1到10000 nM)Enzalutamide处理细胞。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 雄激素非依赖性LNCaP/HR移植瘤雄性SCID鼠
  • Dosages: 10 mg/kg
  • Administration: 每天饲喂处理
    (Only for Reference)

溶解度 (25°C)

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

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 464.44
化学式

C21H16F4N4O2S

CAS号 915087-33-1
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04335682 Not yet recruiting Drug: Darolutamide|Drug: Enzalutamide Metastatic Prostate Cancer|Prostate Cancer Metastatic|Prostate Cancer|Castrate Resistant Prostate Cancer Alliance Foundation Trials LLC.|Bayer April 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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID