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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文献中Selleckの製品使用例(410)

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 M2\WUGN6fG:2b4jpZ{BCe3OjeR?= MlfiO{Bl[Xm| M{e3[Fk2LSCHdF;I MUjJR|UxRTVwMUKg{txO M124VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{GzOVY4Lz5{M{exN|U3PzxxYU6=
human LNCAP NEjWTGFHfW6ldHnvckBCe3OjeR?= MUCxJO69VQ>? Mm[zSG1UVw>? MWTJcohq[mm2czDwdo9{fGG2ZTDzdIVkcW[rYzDhcpRq\2WwIIPlZ5JmfGmxbjDpckBpfW2jbjDMUmNCWCClZXzsd{BmgHC{ZYPzbY5oKGGwZILv[4VvKHKnY3XweI9zKGG2IEGwNE0yODBybl2= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODJzOEexO{c,OjB{MUi3NVc9N2F-
VCaP MoP4SpVv[3Srb36gRZN{[Xl? M164NFExKM7:TR?= NV;KUVF5OjRiaB?= NUjiVVNzTE2VTx?= NFSyc4dUfXCycnXzd4V{KGyrZ3Hu[E1u\WSrYYTl[EBCWi2ITDDzbYdv[Wyrbne= NYPkO29URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3NVA1OzZpPkKyO|ExPDN4PD;hQi=>
BCK4 MYDGeY5kfGmxbjDBd5NigQ>? M3nWd|ExKM7:TR?= NEOxSnM4KGSjeYO= MkHsSG1UVw>? M1nBSmlvcGmkaYTzJIV{fHKjZHnvcE1u\WSrYYTl[EBxem:uaX\ldoF1cW:w NIXKTnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES1NVExQSd-MkS0OVEyODl:L3G+
MCF7s M173c2Z2dmO2aX;uJGF{e2G7 NWT5bpFJOTBizszN NF;oZYo3KGSjeYO= M4DjNWROW09? NXe3VY1yUW6qaXLpeJMh\XO2cnHkbY9tNW2nZHnheIVlKHC{b3zp[oVz[XSrb36= MonGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2NUGxNFkoRjJ2NEWxNVA6RC:jPh?=
PC-3 MUHGeY5kfGmxbjDBd5NigQ>? MYexNEDPxE1? NFTZeFU4OiCq Mln2SG1UVw>? MmHvSI9meyCwb4SgbY5pcWKrdDDj[YxtKHC{b3zp[oVz[XSrb36= NFPnNVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO0OFg3PCd-MkWzOFQ5PjR:L3G+
CWR22Rv1 M2\DS2Z2dmO2aX;uJGF{e2G7 MnP2NVUh|ryP MoH3NlQhcA>? Ml[5SG1UVw>? MnnESI9meyCwb4SgZYZn\WO2IITo[UBnfWyuIHzlcod1cCCDUjDlfJBz\XO|aX;u NU\5eHJwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
LNCAP/AR M1T0WGFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= MoDnTWM2OCB;IECuNFIyKM7:TR?= MonnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd5MUe1OFQoRjJ5N{G3OVQ1RC:jPh?=
MDA-MB-453 NG\PWGlCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 NHWxVphGSzVyIE2gNE4xPDlizszN NYfqcpJORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
LNCAP NYT5fWpFSW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> NU\OfWYxPzJiaB?= M120NWlEPTBiPTCwMlA2KM7:TR?= NVH1fXE5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxPVMzOTVpPkOwNVk{OjF3PD;hQi=>
LNCAP NUnPeWFiSW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> MX23NkBp M3jqUGlEPTBiPTCwMlA6KM7:TR?= MmfPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzOUOyNVUoRjNyMUmzNlE2RC:jPh?=
LNCAP MnTSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXPHTVUxKD1iMD6xNkDPxE1? M4X5WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEGxNlE6Lz5{OECxNVIyQTxxYU6=
LNCAP NGTKRWFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MYSzJIRigXN? MUHJR|UxKD1iMD6xNlcyKM7:TR?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB2NkOxN{c,OjZyNE[zNVM9N2F-
LNCAP Ml75RY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= MX:2JIRigXN? M17zcWdKPTBiPTCwMlI6KM7:TR?= MkjnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyMUGyNVkoRjJ6MEGxNlE6RC:jPh?=
UAS-bla GripTite 293 MoHBRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= MV:xOkB1dyB{NDDo NIHqZ4xKSzVyIE2gNE4{PjFizszN M1nLZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5M{CxN|Y5Lz5{N{OwNVM3QDxxYU6=
mammalian expression system MmrLRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NVfsfY5[OjJidH:gNlQhcA>? M1KzTmVEPTBiPTCwMlQzKM7:TR?= Moj3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|OEW1NFMoRjJ6M{i1OVA{RC:jPh?=
VCaP M3\SVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1u5V|E1PCCq MXTHTVUxKD1iMD62NUDPxE1? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF{MUW4Okc,OjVzMkG1PFY9N2F-
LNCaP Mlv6RY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NG\4fYMzKGh? M4frPGVEPTBiPTCwMlkyPSEQvF2= NVWwWnJvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
COS7 MnrMRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= MnH1NlQhcA>? M{[zbmlEPTBiPTCxMlI3KM7:TR?= NWnubHZZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNVc5QTdpPkK5NVE4QDl5PD;hQi=>
AR LBD mutant M3jFdWFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= NVfCbVdwPCCq NEPaZ|NKSzVyIE2gNU4{PSEQvF2= NWjR[I1yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QDlpPkK3PFExPTh7PD;hQi=>
LNCAP MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGf5fYRIUTVyIE2gNk45QCEQvF2= NGrBOWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOFE{OCd-MkW2N|QyOzB:L3G+
CWR22Rv1 MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWjXe|g4T0l3MDC9JFMvOzRizszN NEHLOoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOFE{OCd-MkW2N|QyOzB:L3G+
LNCAP Mme3R5l1d3SxeHnjbZR6KGG|c3H5 MYC3JIRigXN? MX\HTVUxKD1iNT6xNkDPxE1? NY\KPVl{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
PC3 NU[ybmo3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV3HTVUxKD1iOT6xOUDPxE1? M{PKdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkO0NVMxLz5{NU[zOFE{ODxxYU6=
CWR22Rv1 MWHD[YxtKHO3co\peoFtKGG|c3H5 NGPjWVgyPDRiaB?= M3vRVmlEPTBiPTC5Mlch|ryP NIPpbYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyNVU5Pid-MkWxNlE2QDZ:L3G+
LNCAP NGjHOFVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NYftOmdGQTZiaB?= MXnJR|UxKD1iMUGuOFch|ryP NEfoc289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OwNVM3QCd-MkezNFE{Pjh:L3G+
LNCaP-hr MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NVLsNolWOyCmYYnz MWXJR|UxKD1iMUKuOUDPxE1? MoDmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PFkoRjJ5OEGwOVg6RC:jPh?=
LNCAP Mn2wRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NGjmVI0{KGSjeYO= MXfJR|UxKD1iMUKuOUDPxE1? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFzN{i5O{c,OjlzMUe4PVc9N2F-
LNCaP MmjhRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= MUixOFQhcA>? M4HGXmdKPTBiPTCxPE45QCEQvF2= NFT6S489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK3Nlg6PCd-MkiyO|I5QTR:L3G+
LNCaP-AR MmPkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{T2cFE1PCCq MWTHTVUxKD1iMUiuPUDPxE1? M4PqeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUKxOVg3Lz5{NUGyNVU5PjxxYU6=
C4-2B MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MVmxNkBp M3e3NGlEPTBiPTCyNE44PyEQvF2= NV;HbW5IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVg2OThpPkK5O|U5PTF6PD;hQi=>
A31 M{DKcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlvnO|IhcA>? M4fkOmdKPTBiPTCyO{42KM7:TR?= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDBzMUKxPUc,OjhyMUGyNVk9N2F-
22Rv1 NF7ZclBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NHrifFY6PiCq M3yzS2lEPTBiPTCzNU44PiEQvF2= NUTnZZpuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkezNFE{PjhpPkK3N|AyOzZ6PD;hQi=>
22Rv1 M4\qU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NFPTcFE6PiCq MUHJR|UxKD1iM{GuO|Yh|ryP NEDqOWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm2OVg3Oid-Mk[5OlU5PjJ:L3G+
DU145 NGnwfG5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NYfDXpY3QTZiaB?= MWfJR|UxKD1iM{KuNlch|ryP NHfuVmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OwNVM3QCd-MkezNFE{Pjh:L3G+
LNCAP MkHDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NUXXRXhKPzJiaB?= NYW4c|BHUUN3MDC9JFM{Njh2IN88US=> MnG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NEixN|koRjJ7NES4NVM6RC:jPh?=
CW22Rv1 NXPrW4tHSW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> MY[3NkBp Mk\1TWM2OCB;IEO1Mlc2KM7:TR?= NV;sNnV4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyO|I5QTRpPkK4NlczQDl2PD;hQi=>
22Rv1 MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MXq3NkBp M4nW[2lEPTBiPTCzOk43PiEQvF2= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2OEGzPUc,Ojl2NEixN|k9N2F-
22Rv1 NHvmWYVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= Mm[wNVIhcA>? NEDqbFhKSzVyIE2gN|YvPjZizszN MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd3OEWxPEc,Ojl5NUi1NVg9N2F-
LNCAP NHTYR2xCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NInWZWsyOiCq M13mWGlEPTBiPTC0Nk4{PyEQvF2= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd3OEWxPEc,Ojl5NUi1NVg9N2F-
DU145 NEHMWFlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NHHQcmY{KGSjeYO= NEW4bIJKSzVyIE2gOFYvOSEQvF2= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW4PUc,Ojd6MUC1PFk9N2F-
DU145 NGrCUGpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NHTUfZI{KGSjeYO= MUTJR|UxKD1iNE[uNUDPxE1? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFzN{i5O{c,OjlzMUe4PVc9N2F-

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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
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

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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