Enzalutamide (MDV3100)

For research use only.

Catalog No.S1250

347 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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 300 In stock
USD 150 In stock
USD 270 In stock
USD 770 In stock
USD 1990 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Enzalutamide (MDV3100) has been cited by 347 publications

Purity & Quality Control

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 MULDfZRwfG:6aXOgRZN{[Xl? M2PjVlch\GG7cx?= M1L2Slk2LSCHdF;I NYjVb49tUUN3ME21MlEzKM7:TR?= NIj5fFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exN|U3Pyd-MkO3NVM2Pjd:L3G+
human LNCAP NWXFU3FPTnWwY4Tpc44hSXO|YYm= NGD5NoIyKM7:TR?= Ml7vSG1UVw>? NEW2TWdKdmirYnn0d{Bxem:|dHH0[UB{eGWlaX\pZ{BidnSrZ3XuJJNm[3KndHnvckBqdiCqdX3hckBNVkODUDDj[YxteyCneIDy[ZN{cW6pIHHu[JJw\2WwIILlZ4VxfG:{IHH0JFExOC1zMECwcm0> MkPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB{MUi3NVcoRjJyMkG4O|E4RC:jPh?=
VCaP NWHXc4E2TnWwY4Tpc44hSXO|YYm= MkLWNVAh|ryP Mny2NlQhcA>? M2q5WGROW09? NHfMRnhUfXCycnXzd4V{KGyrZ3Hu[E1u\WSrYYTl[EBCWi2ITDDzbYdv[Wyrbne= NXXUXWc5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3NVA1OzZpPkKyO|ExPDN4PD;hQi=>
BCK4 MWDGeY5kfGmxbjDBd5NigQ>? MkLnNVAh|ryP MWC3JIRigXN? NFLhcldFVVOR NYHI[lFuUW6qaXLpeJMh\XO2cnHkbY9tNW2nZHnheIVlKHC{b3zp[oVz[XSrb36= NYLrc2RbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0OVEyODlpPkK0OFUyOTB7PD;hQi=>
MCF7s Mn3lSpVv[3Srb36gRZN{[Xl? NGLCbJcyOCEQvF2= MnL4OkBl[Xm| NHXwdYZFVVOR M{nrdWlvcGmkaYTzJIV{fHKjZHnvcE1u\WSrYYTl[EBxem:uaX\ldoF1cW:w NHPZU5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES1NVExQSd-MkS0OVEyODl:L3G+
PC-3 NV7YTVVWTnWwY4Tpc44hSXO|YYm= NVn3W2VtOTBizszN MlfZO|IhcA>? NV3SXlR[TE2VTx?= NIDFVoZFd2W|IH7veEBqdmirYnn0JINmdGxicILvcIln\XKjdHnvci=> NX7DXodGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOFQ5PjRpPkK1N|Q1QDZ2PD;hQi=>
CWR22Rv1 M1uxZ2Z2dmO2aX;uJGF{e2G7 NV34d|JMOTVizszN NVHxcm1COjRiaB?= MUHEUXNQ MVLEc4V{KG6xdDDh[oZm[3RidHjlJIZ2dGxibHXu[5RpKEGUIHX4dJJme3Orb36= NXHPeWJoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
LNCAP/AR MWHBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 MnPETWM2OCB;IECuNFIyKM7:TR?= MnjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd5MUe1OFQoRjJ5N{G3OVQ1RC:jPh?=
MDA-MB-453 NWm3eYQ4SW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> NVPQW|Z4TUN3MDC9JFAvODR7IN88US=> MoPnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5MUO1OlcoRjJ|N{GzOVY4RC:jPh?=
LNCAP MkTPRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= MmSxO|IhcA>? MnPBTWM2OCB;IECuNFUh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODF7M{KxOUc,OzBzOUOyNVU9N2F-
LNCAP Mn2yRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NEL4cJg4OiCq NGrnemxKSzVyIE2gNE4xQSEQvF2= Mm\tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzOUOyNVUoRjNyMUmzNlE2RC:jPh?=
LNCAP MonxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV:zSmRxT0l3MDC9JFAvOTJizszN MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDBzMUKxPUc,OjhyMUGyNVk9N2F-
LNCAP M{HBe2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NWqzPHZDOyCmYYnz NGfVV3hKSzVyIE2gNE4yOjdzIN88US=> MnjrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNE[zNVMoRjJ4MES2N|E{RC:jPh?=
LNCAP M{jQdGFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= M3\x[VYh\GG7cx?= M4DmWmdKPTBiPTCwMlI6KM7:TR?= NFy0RVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECxNVIyQSd-MkiwNVEzOTl:L3G+
UAS-bla GripTite 293 NYPmZnp6SW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> MlzMNVYhfG9iMkSgbC=> M3LyUGlEPTBiPTCwMlM3OSEQvF2= M{DqUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5M{CxN|Y5Lz5{N{OwNVM3QDxxYU6=
mammalian expression system NY\Hc3M4SW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> NX\peopOOjJidH:gNlQhcA>? NGrRTm9GSzVyIE2gNE41OiEQvF2= MlTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh|OEW1NFMoRjJ6M{i1OVA{RC:jPh?=
VCaP MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVrWR2dIOTR2IHi= MoXnS2k2OCB;IECuOlEh|ryP NYHkcGFORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlE2QDZpPkK1NVIyPTh4PD;hQi=>
LNCaP MVvBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 MXyyJIg> MUTFR|UxKD1iMD65NVUh|ryP NU\xU2xTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
COS7 NEPITI5CdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 NIDtUpUzPCCq Ml[wTWM2OCB;IEGuNlYh|ryP MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFzN{i5O{c,OjlzMUe4PVc9N2F-
AR LBD mutant Mme1RY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= M2PmSVQhcA>? M{nBeGlEPTBiPTCxMlM2KM7:TR?= MnHUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PFkoRjJ5OEGwOVg6RC:jPh?=
LNCAP NYmwc4xmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4\we2dKPTBiPTCyMlg5KM7:TR?= NGDHZ4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOFE{OCd-MkW2N|QyOzB:L3G+
CWR22Rv1 NUHzOWlXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHLCc2hIUTVyIE2gN{4{PCEQvF2= NGm3clc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOFE{OCd-MkW2N|QyOzB:L3G+
LNCAP NUTx[llnS3m2b4TvfIlkcXS7IHHzd4F6 NFvOWYE4KGSjeYO= M3rvdWdKPTBiPTC1MlEzKM7:TR?= NHPoRoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exN|U3Pyd-MkO3NVM2Pjd:L3G+
PC3 NHHSR3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3XHTGdKPTBiPTC5MlE2KM7:TR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ|NEGzNEc,OjV4M{SxN|A9N2F-
CWR22Rv1 MlTmR4VtdCC|dYL2bZZidCCjc4PhfS=> NYPGNY4yOTR2IHi= NX[xSmZMUUN3MDC9JFkvPyEQvF2= NVjJSYd1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlE2QDZpPkK1NVIyPTh4PD;hQi=>
LNCAP M4jlbWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M3T1c|k3KGh? NFTVbHVKSzVyIE2gNVEvPDdizszN Mmf4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
LNCaP-hr MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MXWzJIRigXN? NWjJPZdCUUN3MDC9JFEzNjVizszN M4nIXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OEGwOVg6Lz5{N{ixNFU5QTxxYU6=
LNCAP MkH3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M1G2dlMh\GG7cx?= MlLUTWM2OCB;IEGyMlUh|ryP NFf2dHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGxO|g6Pyd-MkmxNVc5QTd:L3G+
LNCaP MnexRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= Ml;DNVQ1KGh? NG\JeIRIUTVyIE2gNVgvQDhizszN NV7TXXltRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyO|I5QTRpPkK4NlczQDl2PD;hQi=>
LNCaP-AR M{CycWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkO2NVQ1KGh? MmLsS2k2OCB;IEG4Mlkh|ryP NEfVN4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyNVU5Pid-MkWxNlE2QDZ:L3G+
C4-2B NUT4VJl{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MXexNkBp M{HUU2lEPTBiPTCyNE44PyEQvF2= MoftQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NUi1NVgoRjJ7N{W4OVE5RC:jPh?=
A31 MmKwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXi3NkBp MXzHTVUxKD1iMkeuOUDPxE1? Mk\kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyMUGyNVkoRjJ6MEGxNlE6RC:jPh?=
22Rv1 MoLqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? Mn70PVYhcA>? NIDFRopKSzVyIE2gN|EvPzZizszN NELsd5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OwNVM3QCd-MkezNFE{Pjh:L3G+
22Rv1 Mnq1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NIPPNWk6PiCq MXLJR|UxKD1iM{GuO|Yh|ryP NUTjNlFkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5OlU5PjJpPkK2PVY2QDZ{PD;hQi=>
DU145 MkXPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MW[5OkBp NF33fJVKSzVyIE2gN|IvOjdizszN MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzNyMUO2PEc,Ojd|MEGzOlg9N2F-
LNCAP MlX4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MXi3NkBp NGG2XIZKSzVyIE2gN|MvQDRizszN M2fUVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NES4NVM6Lz5{OUS0PFE{QTxxYU6=
CW22Rv1 Mo\sRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= MU[3NkBp MoPqTWM2OCB;IEO1Mlc2KM7:TR?= M4L6W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkeyPFk1Lz5{OEK3Nlg6PDxxYU6=
22Rv1 M1[4U2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NU[3dVk4PzJiaB?= MXnJR|UxKD1iM{[uOlYh|ryP MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2OEGzPUc,Ojl2NEixN|k9N2F-
22Rv1 MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M37IPFEzKGh? M3q4WWlEPTBiPTCzOk43PiEQvF2= M2K5RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{W4OVE5Lz5{OUe1PFUyQDxxYU6=
LNCAP M2\2fmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MYSxNkBp NYXLR4tkUUN3MDC9JFQzNjN5IN88US=> Mn74QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NUi1NVgoRjJ7N{W4OVE5RC:jPh?=
DU145 NXz0RoxnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NE\NdJI{KGSjeYO= NF7Ye4JKSzVyIE2gOFYvOSEQvF2= M13XS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OEGwOVg6Lz5{N{ixNFU5QTxxYU6=
DU145 MXjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NVzPPYhTOyCmYYnz MmLSTWM2OCB;IES2MlEh|ryP MlziQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMUe4PVcoRjJ7MUG3PFk4RC:jPh?=

... 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
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]
- Collapse
  • 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]
- Collapse
  • 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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

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)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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 )

  • C1
    V1
    C2
    V2

* 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

  • Serial Dilutions

  • Computed Result

  • 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):
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
NCT04655365 Not yet recruiting Drug: Enzalutamide capsule Prostate Cancer CHU de Quebec-Universite Laval|Astellas Pharma Europe Ltd. January 4 2021 Phase 2
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 September 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
NCT04443062 Recruiting Drug: 177Lu-PSMA-I&T Prostate Cancer Radboud University|Prostaatkankerstichting July 20 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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    I would like to inquire about the usage or solubility of S1250, Enzalutamide.

  • Answer:

    For in vivo experiment, S1250 can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 5mg/ml as a suspension for oral gavage. And it can be dissolved in 15% DMSO+85% PEG 300 at 10mg/ml as a clear solution. When prepare the solution, please dissolve the compound in DMSO clearly first, then add PEG.

Androgen Receptor Signaling Pathway Map

Androgen Receptor Inhibitors with Unique Features

Related Androgen Receptor Products

Tags: buy Enzalutamide (MDV3100) | Enzalutamide (MDV3100) supplier | purchase Enzalutamide (MDV3100) | Enzalutamide (MDV3100) cost | Enzalutamide (MDV3100) manufacturer | order Enzalutamide (MDV3100) | Enzalutamide (MDV3100) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID