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
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客户使用Selleck生产的Enzalutamide (MDV3100)发表文献394篇:

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 NHTDXldEgXSxdH;4bYMhSXO|YYm= NEW0NnI4KGSjeYO= MX25OUUhTXSRSB?= MkfQTWM2OD13LkGyJO69VQ>? MlfSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5MUO1OlcoRjJ|N{GzOVY4RC:jPh?=
human LNCAP MojWSpVv[3Srb36gRZN{[Xl? MUmxJO69VQ>? MmXOSG1UVw>? NUTMTWxCUW6qaXLpeJMheHKxc4TheIUhe3CnY3nmbYMh[W62aXflckB{\WO{ZYTpc44hcW5iaIXtZY4hVE6FQWCgZ4VtdHNiZYjwdoV{e2mwZzDhcoRzd2enbjDy[YNmeHSxcjDheEAyODBvMUCwNI5O NXjseWNXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCyNVg4OTdpPkKwNlE5PzF5PD;hQi=>
VCaP MUjGeY5kfGmxbjDBd5NigQ>? M1vSfVExKM7:TR?= MV2yOEBp NYLGbmdZTE2VTx?= MYjTeZBxemW|c3XzJIxq\2GwZD3t[YRq[XSnZDDBVk1HVCC|aXfuZYxqdmd? M1u5R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{N{GwOFM3Lz5{MkexNFQ{PjxxYU6=
BCK4 NVHrdXk4TnWwY4Tpc44hSXO|YYm= MnrsNVAh|ryP M{[wbFch\GG7cx?= NY\Vd4d6TE2VTx?= NEXqbXdKdmirYnn0d{Bme3S{YXTpc4wudWWmaXH0[YQheHKxbHnm[ZJifGmxbh?= M{jicVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEWxNVA6Lz5{NES1NVExQTxxYU6=
MCF7s MmPiSpVv[3Srb36gRZN{[Xl? NEjHfGcyOCEQvF2= NIPmXWg3KGSjeYO= MUXEUXNQ NX;z[5FoUW6qaXLpeJMh\XO2cnHkbY9tNW2nZHnheIVlKHC{b3zp[oVz[XSrb36= MlfCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2NUGxNFkoRjJ2NEWxNVA6RC:jPh?=
PC-3 MkDBSpVv[3Srb36gRZN{[Xl? M1i4e|ExKM7:TR?= NV21ZotTPzJiaB?= M4LsNmROW09? MoDwSI9meyCwb4SgbY5pcWKrdDDj[YxtKHC{b3zp[oVz[XSrb36= NUW5OINtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOFQ5PjRpPkK1N|Q1QDZ2PD;hQi=>
CWR22Rv1 MmnhSpVv[3Srb36gRZN{[Xl? NF\2SnMyPSEQvF2= MYmyOEBp MXzEUXNQ Ml[wSI9meyCwb4SgZYZn\WO2IITo[UBnfWyuIHzlcod1cCCDUjDlfJBz\XO|aX;u MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdzM{W2O{c,OjN5MUO1Olc9N2F-
LNCAP/AR NI\xbnVCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 NXWyUYpuUUN3MDC9JFAvODJzIN88US=> NFnuZ4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{exO|U1PCd-Mke3NVc2PDR:L3G+
MDA-MB-453 NXf1Wmo4SW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> MYXFR|UxKD1iMD6wOFkh|ryP M3zHfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{GzOVY4Lz5{M{exN|U3PzxxYU6=
LNCAP MV;BcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 MYO3NkBp NEfJTmZKSzVyIE2gNE4xPSEQvF2= MkLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzOUOyNVUoRjNyMUmzNlE2RC:jPh?=
LNCAP MV\BcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 M1rhNVczKGh? MVLJR|UxKD1iMD6wPUDPxE1? NEHaRYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG5N|IyPSd-M{CxPVMzOTV:L3G+
LNCAP MkXHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVHmeGt1T0l3MDC9JFAvOTJizszN MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDBzMUKxPUc,OjhyMUGyNVk9N2F-
LNCAP MoLIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NH;OcHU{KGSjeYO= NX\QcVFrUUN3MDC9JFAvOTJ5MTFOwG0> NEe4TFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0OlMyOyd-Mk[wOFY{OTN:L3G+
LNCAP MkLqRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= MoeyOkBl[Xm| NVn6TXU1T0l3MDC9JFAvOjlizszN MkLWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyMUGyNVkoRjJ6MEGxNlE6RC:jPh?=
UAS-bla GripTite 293 M{W5b2FvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= M2rabVE3KHSxIEK0JIg> MnjDTWM2OCB;IECuN|YyKM7:TR?= NU[5NFJGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkezNFE{PjhpPkK3N|AyOzZ6PD;hQi=>
mammalian expression system MmfrRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NHP4Z5EzOiC2bzCyOEBp M3TweWVEPTBiPTCwMlQzKM7:TR?= NHrlWHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO4OVUxOyd-MkizPFU2ODN:L3G+
VCaP NUf4VooyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1LHeVE1PCCq NUiyfXNPT0l3MDC9JFAvPjFizszN NV3vcnN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlE2QDZpPkK1NVIyPTh4PD;hQi=>
LNCaP NUfPWWp1SW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> NGXseHMzKGh? MUfFR|UxKD1iMD65NVUh|ryP NVzV[ohLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
COS7 Mn\XRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= MofONlQhcA>? MWLJR|UxKD1iMT6yOkDPxE1? MnrUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMUe4PVcoRjJ7MUG3PFk4RC:jPh?=
AR LBD mutant NHL3dGFCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 NXjDNZJJPCCq NXTYVIM4UUN3MDC9JFEvOzVizszN NHrFWJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU5QSd-Mke4NVA2QDl:L3G+
LNCAP MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXPDTo9oT0l3MDC9JFIvQDhizszN NWLjNokyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2N|QyOzBpPkK1OlM1OTNyPD;hQi=>
CWR22Rv1 MlSwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn;0S2k2OCB;IEOuN|Qh|ryP M4X3fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkO0NVMxLz5{NU[zOFE{ODxxYU6=
LNCAP M3XjPWN6fG:2b4jpZ4l1gSCjc4PhfS=> M2Hq[lch\GG7cx?= Mn2wS2k2OCB;IEWuNVIh|ryP MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdzM{W2O{c,OjN5MUO1Olc9N2F-
PC3 M1XMdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX\ESmhiT0l3MDC9JFkvOTVizszN MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ|NEGzNEc,OjV4M{SxN|A9N2F-
CWR22Rv1 MmfsR4VtdCC|dYL2bZZidCCjc4PhfS=> NWnHfmZHOTR2IHi= M13vdmlEPTBiPTC5Mlch|ryP NGTobHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyNVU5Pid-MkWxNlE2QDZ:L3G+
LNCAP MkDxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MonRPVYhcA>? NHXZeFhKSzVyIE2gNVEvPDdizszN Mnq3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
LNCaP-hr NVPzblVRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= Mom4N{Bl[Xm| MVHJR|UxKD1iMUKuOUDPxE1? NELFWlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU5QSd-Mke4NVA2QDl:L3G+
LNCAP NFHLR3RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NWHVbG04OyCmYYnz MW\JR|UxKD1iMUKuOUDPxE1? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFzN{i5O{c,OjlzMUe4PVc9N2F-
LNCaP NV\uUI5ZSW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> NHjlcZgyPDRiaB?= NUXUbGJOT0l3MDC9JFE5Njh6IN88US=> M2DnblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkeyPFk1Lz5{OEK3Nlg6PDxxYU6=
LNCaP-AR MnLIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlG0NVQ1KGh? NUnDNVVTT0l3MDC9JFE5NjlizszN NH\seXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyNVU5Pid-MkWxNlE2QDZ:L3G+
C4-2B Mn;GRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MnzlNVIhcA>? Mlv1TWM2OCB;IEKwMlc4KM7:TR?= NWftempGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVg2OThpPkK5O|U5PTF6PD;hQi=>
A31 NHfGeVVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVjYTGpFPzJiaB?= Mk\iS2k2OCB;IEK3MlUh|ryP MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDBzMUKxPUc,OjhyMUGyNVk9N2F-
22Rv1 M1jMV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M33GZ|k3KGh? M3G1cWlEPTBiPTCzNU44PiEQvF2= MkTkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
22Rv1 NXLSUIJoSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NGXv[W86PiCq NH\FOpRKSzVyIE2gN|EvPzZizszN MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl4NUi2Nkc,OjZ7NkW4OlI9N2F-
DU145 NVjOXm8{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MXe5OkBp NF\2VZZKSzVyIE2gN|IvOjdizszN MonBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
LNCAP NYjNWmpySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= Mmm3O|IhcA>? M3TGRWlEPTBiPTCzN{45PCEQvF2= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2OEGzPUc,Ojl2NEixN|k9N2F-
CW22Rv1 MkPQRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= MWi3NkBp M{m1S2lEPTBiPTCzOU44PSEQvF2= NYftN29YRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyO|I5QTRpPkK4NlczQDl2PD;hQi=>
22Rv1 MkjSRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NX7i[ZV4PzJiaB?= MVjJR|UxKD1iM{[uOlYh|ryP MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2OEGzPUc,Ojl2NEixN|k9N2F-
22Rv1 MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NUHEWVZnOTJiaB?= MlzXTWM2OCB;IEO2MlY3KM7:TR?= M1GyUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{W4OVE5Lz5{OUe1PFUyQDxxYU6=
LNCAP NGrxemRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MXGxNkBp NWfTcXhtUUN3MDC9JFQzNjN5IN88US=> M2K0PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{W4OVE5Lz5{OUe1PFUyQDxxYU6=
DU145 MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NVn1VIx3OyCmYYnz MVjJR|UxKD1iNE[uNUDPxE1? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW4PUc,Ojd6MUC1PFk9N2F-
DU145 MnjiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MUSzJIRigXN? M37vOGlEPTBiPTC0Ok4yKM7:TR?= MUG8ZUB1[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 (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、SDS / 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、SDS / 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
NCT05191017 Not yet recruiting Drug: NUV-422|Drug: Enzalutamide Prostate Cancer|Prostatic Cancer|Cancer of Prostate|Cancer of the Prostate|Prostate Neoplasm|Castrate Resistant Prostate Cancer|Castration Resistant Prostatic Cancer|Castration Resistant Prostatic Neoplasms Nuvation Bio Inc. April 2022 Phase 1|Phase 2
NCT05081193 Not yet recruiting Drug: Testosterone Undecanoate|Drug: Enzalutamide Prostate Cancer|Castration-resistant Prostate Cancer|Metastatic Castration-resistant Prostate Cancer Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Clarus Therapeutics February 15 2022 Phase 2
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
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