Enzalutamide (MDV3100)

For research use only.

Catalog No.S1250

367 publications

Enzalutamide (MDV3100) Chemical Structure

CAS No. 915087-33-1

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

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Selleck's Enzalutamide (MDV3100) has been cited by 367 publications

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Choose Selective Androgen Receptor Inhibitors

Biological Activity

Description Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Targets
Androgen Receptor [1]
(LNCaP cells)
36 nM
In vitro

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human LNCAP NFPx[5lEgXSxdH;4bYMhSXO|YYm= MX:3JIRigXN? MYW5OUUhTXSRSB?= NEC3SG5KSzVyPUWuNVIh|ryP M1r1U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{GzOVY4Lz5{M{exN|U3PzxxYU6=
human LNCAP M2T1fGZ2dmO2aX;uJGF{e2G7 MYqxJO69VQ>? M3vHSGROW09? M{PGXWlvcGmkaYTzJJBzd3O2YYTlJJNx\WOrZnnjJIFvfGmpZX6gd4VkemW2aX;uJIlvKGi3bXHuJGxPS0GSIHPlcIx{KGW6cILld5NqdmdiYX7kdo9o\W5icnXj[ZB1d3JiYYSgNVAxNTFyMEDuUS=> MlP1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB{MUi3NVcoRjJyMkG4O|E4RC:jPh?=
VCaP MU\GeY5kfGmxbjDBd5NigQ>? Mki0NVAh|ryP MnX5NlQhcA>? MUXEUXNQ MV7TeZBxemW|c3XzJIxq\2GwZD3t[YRq[XSnZDDBVk1HVCC|aXfuZYxqdmd? M{S1PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{N{GwOFM3Lz5{MkexNFQ{PjxxYU6=
BCK4 MlrESpVv[3Srb36gRZN{[Xl? M{ToPFExKM7:TR?= M1rOSlch\GG7cx?= NFKz[nJFVVOR NV3YdYFoUW6qaXLpeJMh\XO2cnHkbY9tNW2nZHnheIVlKHC{b3zp[oVz[XSrb36= M1;TXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEWxNVA6Lz5{NES1NVExQTxxYU6=
MCF7s NIDabVZHfW6ldHnvckBCe3OjeR?= NEXWRooyOCEQvF2= MoPaOkBl[Xm| NIXKPVVFVVOR MUTJcohq[mm2czDld5Rz[WSrb3ytcYVlcWG2ZXSgdJJwdGmoZYLheIlwdg>? MlHMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2NUGxNFkoRjJ2NEWxNVA6RC:jPh?=
PC-3 M1vpfmZ2dmO2aX;uJGF{e2G7 NYj1T5dlOTBizszN MXy3NkBp Mo\DSG1UVw>? MUHEc4V{KG6xdDDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN2NEi2OEc,OjV|NES4OlQ9N2F-
CWR22Rv1 M4X0RWZ2dmO2aX;uJGF{e2G7 M13wZlE2KM7:TR?= NUT3eIJSOjRiaB?= MYTEUXNQ NGXKeGtFd2W|IH7veEBi\m[nY4SgeIhmKG[3bHygcIVv\3SqIFHSJIV5eHKnc4Ppc44> NHy4RlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exN|U3Pyd-MkO3NVM2Pjd:L3G+
LNCAP/AR M{TN[WFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= NVzDRnlqUUN3MDC9JFAvODJzIN88US=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzdzN{W0OEc,Ojd5MUe1OFQ9N2F-
MDA-MB-453 M3jmTGFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= MorUSWM2OCB;IECuNFQ6KM7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdzM{W2O{c,OjN5MUO1Olc9N2F-
LNCAP M1HFcGFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= MkixO|IhcA>? Mo\xTWM2OCB;IECuNFUh|ryP NH24cIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG5N|IyPSd-M{CxPVMzOTV:L3G+
LNCAP NGTqWlVCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 NFO2bHg4OiCq MWDJR|UxKD1iMD6wPUDPxE1? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODF7M{KxOUc,OzBzOUOyNVU9N2F-
LNCAP M3\aemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEHuXJVIUTVyIE2gNE4yOiEQvF2= NHjYXXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECxNVIyQSd-MkiwNVEzOTl:L3G+
LNCAP MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MmTUN{Bl[Xm| NUDOT|RLUUN3MDC9JFAvOTJ5MTFOwG0> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB2NkOxN{c,OjZyNE[zNVM9N2F-
LNCAP NEj2[JpCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 NWTVe25zPiCmYYnz M4LPfmdKPTBiPTCwMlI6KM7:TR?= NH;zO3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECxNVIyQSd-MkiwNVEzOTl:L3G+
UAS-bla GripTite 293 NGDxTGtCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 M3fo[lE3KHSxIEK0JIg> NUnyeGZkUUN3MDC9JFAvOzZzIN88US=> MmD4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
mammalian expression system NFTZXW5CdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 MkXnNlIhfG9iMkSgbC=> MoC3SWM2OCB;IECuOFIh|ryP Mmr5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|OEW1NFMoRjJ6M{i1OVA{RC:jPh?=
VCaP MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M17zRVE1PCCq MY\HTVUxKD1iMD62NUDPxE1? MoL5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMkG1PFYoRjJ3MUKxOVg3RC:jPh?=
LNCaP M4XycGFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= MlXoNkBp MkH1SWM2OCB;IECuPVE2KM7:TR?= MnzrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5MUO1OlcoRjJ|N{GzOVY4RC:jPh?=
COS7 NILQXXVCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 MYeyOEBp NF7udnpKSzVyIE2gNU4zPiEQvF2= NGW3TG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGxO|g6Pyd-MkmxNVc5QTd:L3G+
AR LBD mutant NGDBRYdCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 NWDCVIlRPCCq NHniXWZKSzVyIE2gNU4{PSEQvF2= NETYTHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU5QSd-Mke4NVA2QDl:L3G+
LNCAP MonlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkWyS2k2OCB;IEKuPFgh|ryP MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ|NEGzNEc,OjV4M{SxN|A9N2F-
CWR22Rv1 MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3\GUWdKPTBiPTCzMlM1KM7:TR?= Mn3WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4M{SxN|AoRjJ3NkO0NVMxRC:jPh?=
LNCAP NUfRVWxWS3m2b4TvfIlkcXS7IHHzd4F6 MYm3JIRigXN? MX;HTVUxKD1iNT6xNkDPxE1? NGPyU4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exN|U3Pyd-MkO3NVM2Pjd:L3G+
PC3 NVXCXm1KT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWPhN5FzT0l3MDC9JFkvOTVizszN MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ|NEGzNEc,OjV4M{SxN|A9N2F-
CWR22Rv1 MlL2R4VtdCC|dYL2bZZidCCjc4PhfS=> NEmzO2UyPDRiaB?= M33sfGlEPTBiPTC5Mlch|ryP M1rOV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUKxOVg3Lz5{NUGyNVU5PjxxYU6=
LNCAP M4DLU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M2SwZVk3KGh? MYfJR|UxKD1iMUGuOFch|ryP NGHSTGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OwNVM3QCd-MkezNFE{Pjh:L3G+
LNCaP-hr NVuzT2E5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MVOzJIRigXN? Mn7jTWM2OCB;IEGyMlUh|ryP NXq3OldzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QDlpPkK3PFExPTh7PD;hQi=>
LNCAP MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NEXadIQ{KGSjeYO= NFe4RnJKSzVyIE2gNVIvPSEQvF2= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFzN{i5O{c,OjlzMUe4PVc9N2F-
LNCaP MYnBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 NYrlU|ZpOTR2IHi= MVTHTVUxKD1iMUiuPFgh|ryP NFftbGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK3Nlg6PCd-MkiyO|I5QTR:L3G+
LNCaP-AR MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVq1fWp2OTR2IHi= NUf0VJFIT0l3MDC9JFE5NjlizszN M1j1eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUKxOVg3Lz5{NUGyNVU5PjxxYU6=
C4-2B NF6xN4lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NVjZbZRIOTJiaB?= M4XGSGlEPTBiPTCyNE44PyEQvF2= M4rVRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{W4OVE5Lz5{OUe1PFUyQDxxYU6=
A31 MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUC3NkBp MWXHTVUxKD1iMkeuOUDPxE1? MoDMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyMUGyNVkoRjJ6MEGxNlE6RC:jPh?=
22Rv1 MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MkXGPVYhcA>? MlvLTWM2OCB;IEOxMlc3KM7:TR?= Mn2zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
22Rv1 NV[3eoU2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= M{S3TFk3KGh? MoDuTWM2OCB;IEOxMlc3KM7:TR?= M3;mdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OU[1PFYzLz5{Nkm2OVg3OjxxYU6=
DU145 MoXHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NFfLV3M6PiCq M4rObGlEPTBiPTCzNk4zPyEQvF2= MoGzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
LNCAP NGfPRo5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MUe3NkBp M12zemlEPTBiPTCzN{45PCEQvF2= M3KxfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NES4NVM6Lz5{OUS0PFE{QTxxYU6=
CW22Rv1 M3\xXWFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= MmPnO|IhcA>? M3TsUGlEPTBiPTCzOU44PSEQvF2= M1jScFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkeyPFk1Lz5{OEK3Nlg6PDxxYU6=
22Rv1 M4fTfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NH7Ye|A4OiCq MljTTWM2OCB;IEO2MlY3KM7:TR?= MkLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NEixN|koRjJ7NES4NVM6RC:jPh?=
22Rv1 NILaV5VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NGf1XZgyOiCq MUjJR|UxKD1iM{[uOlYh|ryP NFTveHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUe1PFUyQCd-Mkm3OVg2OTh:L3G+
LNCAP NH3jTJJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M{mwWFEzKGh? MYHJR|UxKD1iNEKuN|ch|ryP Ml;4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NUi1NVgoRjJ7N{W4OVE5RC:jPh?=
DU145 NHHURmhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NFz1NZQ{KGSjeYO= NFP5epZKSzVyIE2gOFYvOSEQvF2= NGDkZmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU5QSd-Mke4NVA2QDl:L3G+
DU145 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MkXHN{Bl[Xm| MoH2TWM2OCB;IES2MlEh|ryP NGrucZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGxO|g6Pyd-MkmxNVc5QTd:L3G+

... Click to View More Cell Line Experimental Data

Assay
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
In vivo Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1]

Protocol

Kinase Assay:[3]
- Collapse

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.
Cell Research:[1]
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  • Cell lines: LNCaP or LNCaP/AR cells
  • Concentrations: 0-10 μM
  • Incubation Time: 1-4 days
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Castration-resistant LNCaP/HR xenografts in male SCID mice
  • Dosages: 10 mg/kg
  • Administration: Administered via gavage daily
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 464.44
Formula

C21H16F4N4O2S

CAS No. 915087-33-1
Storage powder
in solvent
Synonyms 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID