Enzalutamide (MDV3100)

Catalog No.S1250

For research use only.

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

Enzalutamide (MDV3100) Chemical Structure

CAS No. 915087-33-1

Selleck's Enzalutamide (MDV3100) has been cited by 390 publications

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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 M2DLUmN6fG:2b4jpZ{BCe3OjeR?= M2rzXVch\GG7cx?= M{jCR|k2LSCHdF;I MWHJR|UxRTVwMUKg{txO NHrM[Jc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exN|U3Pyd-MkO3NVM2Pjd:L3G+
human LNCAP MYDGeY5kfGmxbjDBd5NigQ>? NYrsbGM2OSEQvF2= MVPEUXNQ MoLQTY5pcWKrdIOgdJJwe3SjdHWgd5Bm[2moaXOgZY51cWenbjDz[YNz\XSrb36gbY4hcHWvYX6gUG5ESVBiY3XscJMh\XiycnXzd4lv\yCjbnTyc4dmdiC{ZXPldJRweiCjdDCxNFAuOTByMH7N MoX3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB{MUi3NVcoRjJyMkG4O|E4RC:jPh?=
VCaP MojMSpVv[3Srb36gRZN{[Xl? M4XXVFExKM7:TR?= M2S1OlI1KGh? NH\LUlFFVVOR NGm4TW1UfXCycnXzd4V{KGyrZ3Hu[E1u\WSrYYTl[EBCWi2ITDDzbYdv[Wyrbne= NUXle|I1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3NVA1OzZpPkKyO|ExPDN4PD;hQi=>
BCK4 M3TENWZ2dmO2aX;uJGF{e2G7 MXuxNEDPxE1? NWC3Wlk5PyCmYYnz NHL3eFlFVVOR NULBenpUUW6qaXLpeJMh\XO2cnHkbY9tNW2nZHnheIVlKHC{b3zp[oVz[XSrb36= M2D6dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEWxNVA6Lz5{NES1NVExQTxxYU6=
MCF7s MWXGeY5kfGmxbjDBd5NigQ>? MnTaNVAh|ryP MmHxOkBl[Xm| MojOSG1UVw>? NEPNXZNKdmirYnn0d{Bme3S{YXTpc4wudWWmaXH0[YQheHKxbHnm[ZJifGmxbh?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR3MUGwPUc,OjR2NUGxNFk9N2F-
PC-3 NH\TeG9HfW6ldHnvckBCe3OjeR?= NITiR|MyOCEQvF2= NE\rN5c4OiCq NYG5NWRLTE2VTx?= Ml;JSI9meyCwb4SgbY5pcWKrdDDj[YxtKHC{b3zp[oVz[XSrb36= NGjpUVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO0OFg3PCd-MkWzOFQ5PjR:L3G+
CWR22Rv1 NVe1eYF{TnWwY4Tpc44hSXO|YYm= NH7RenQyPSEQvF2= MlfyNlQhcA>? M1TYWmROW09? MknWSI9meyCwb4SgZYZn\WO2IITo[UBnfWyuIHzlcod1cCCDUjDlfJBz\XO|aX;u NXTmUIJiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
LNCAP/AR NXjQcJRYSW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> NXTFZZF{UUN3MDC9JFAvODJzIN88US=> NWX2S4l[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke3NVc2PDRpPkK3O|E4PTR2PD;hQi=>
MDA-MB-453 M1rHTWFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= MWfFR|UxKD1iMD6wOFkh|ryP Ml7wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5MUO1OlcoRjJ|N{GzOVY4RC:jPh?=
LNCAP NF\EOIxCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 MkDzO|IhcA>? Mn2yTWM2OCB;IECuNFUh|ryP NXjqNWZDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxPVMzOTVpPkOwNVk{OjF3PD;hQi=>
LNCAP M17jOWFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= M2DKOFczKGh? M1rVdWlEPTBiPTCwMlA6KM7:TR?= NGLNdlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG5N|IyPSd-M{CxPVMzOTV:L3G+
LNCAP MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHnYTXlIUTVyIE2gNE4yOiEQvF2= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDBzMUKxPUc,OjhyMUGyNVk9N2F-
LNCAP M{DRT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MWizJIRigXN? NGn2fpVKSzVyIE2gNE4yOjdzIN88US=> NHfsWHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC0OlMyOyd-Mk[wOFY{OTN:L3G+
LNCAP M1LkcmFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= NVrjWJFjPiCmYYnz MmjwS2k2OCB;IECuNlkh|ryP MmXGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyMUGyNVkoRjJ6MEGxNlE6RC:jPh?=
UAS-bla GripTite 293 MnzFRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NFfKfJIyPiC2bzCyOEBp NF3lO4tKSzVyIE2gNE4{PjFizszN NGfMVIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OwNVM3QCd-MkezNFE{Pjh:L3G+
mammalian expression system MX3BcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 NEHafFEzOiC2bzCyOEBp MVTFR|UxKD1iMD60NkDPxE1? NYHiNYdPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizPFU2ODNpPkK4N|g2PTB|PD;hQi=>
VCaP NWrRZXBuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn3SNVQ1KGh? MlPRS2k2OCB;IECuOlEh|ryP NIXkNYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyNVU5Pid-MkWxNlE2QDZ:L3G+
LNCaP NWDGdog5SW62YXfvcol{fCCjY4Tpeol1gSCjc4PhfS=> MVKyJIg> M2XoNmVEPTBiPTCwMlkyPSEQvF2= MmTaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5MUO1OlcoRjJ|N{GzOVY4RC:jPh?=
COS7 M4\oTGFvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= M{XrXVI1KGh? M1Th[mlEPTBiPTCxMlI3KM7:TR?= NXzaNmRiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxNVc5QTdpPkK5NVE4QDl5PD;hQi=>
AR LBD mutant MWjBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 NYLMcI9mPCCq MVzJR|UxKD1iMT6zOUDPxE1? M4G4OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OEGwOVg6Lz5{N{ixNFU5QTxxYU6=
LNCAP NXvIR2ZCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWPHTVUxKD1iMj64PEDPxE1? NVvJW2VjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2N|QyOzBpPkK1OlM1OTNyPD;hQi=>
CWR22Rv1 NXzad3dQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXL2coZXT0l3MDC9JFMvOzRizszN NEnNSZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOFE{OCd-MkW2N|QyOzB:L3G+
LNCAP MVzDfZRwfG:6aXPpeJkh[XO|YYm= M1nGOlch\GG7cx?= MlToS2k2OCB;IEWuNVIh|ryP M4\kVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{GzOVY4Lz5{M{exN|U3PzxxYU6=
PC3 MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEjCdYpIUTVyIE2gPU4yPSEQvF2= M2Xrc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkO0NVMxLz5{NU[zOFE{ODxxYU6=
CWR22Rv1 MXvD[YxtKHO3co\peoFtKGG|c3H5 MkGyNVQ1KGh? MojZTWM2OCB;IEmuO{DPxE1? M{PqUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUKxOVg3Lz5{NUGyNVU5PjxxYU6=
LNCAP MXjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NGXDOZY6PiCq Mny3TWM2OCB;IEGxMlQ4KM7:TR?= MmniQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
LNCaP-hr NFv4UGVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NX[ydFg3OyCmYYnz MXHJR|UxKD1iMUKuOUDPxE1? NYPlZ|FMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QDlpPkK3PFExPTh7PD;hQi=>
LNCAP MnzSRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MonvN{Bl[Xm| Ml\wTWM2OCB;IEGyMlUh|ryP NH:y[2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGxO|g6Pyd-MkmxNVc5QTd:L3G+
LNCaP MU\BcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 M1vWbFE1PCCq NFv3RW5IUTVyIE2gNVgvQDhizszN NEOzW4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK3Nlg6PCd-MkiyO|I5QTR:L3G+
LNCaP-AR MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlzaNVQ1KGh? M{PLb2dKPTBiPTCxPE46KM7:TR?= NH3zRXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyNVU5Pid-MkWxNlE2QDZ:L3G+
C4-2B NHTCSmNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NF3TWHUyOiCq MWDJR|UxKD1iMkCuO|ch|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd3OEWxPEc,Ojl5NUi1NVg9N2F-
A31 MmHBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn21O|IhcA>? MVnHTVUxKD1iMkeuOUDPxE1? MlOyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyMUGyNVkoRjJ6MEGxNlE6RC:jPh?=
22Rv1 M{\1PGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MUO5OkBp NVPWXm0{UUN3MDC9JFMyNjd4IN88US=> Mo\RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
22Rv1 M{jHfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MYK5OkBp MV;JR|UxKD1iM{GuO|Yh|ryP NXmwWnJRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5OlU5PjJpPkK2PVY2QDZ{PD;hQi=>
DU145 MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NEnWTVU6PiCq NGf0XJZKSzVyIE2gN|IvOjdizszN Mki1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
LNCAP Mn[zRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MnnTO|IhcA>? M2TUVWlEPTBiPTCzN{45PCEQvF2= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2OEGzPUc,Ojl2NEixN|k9N2F-
CW22Rv1 NF7EO3ZCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 M{HBe|czKGh? MlThTWM2OCB;IEO1Mlc2KM7:TR?= MmfnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{N{K4PVQoRjJ6MkeyPFk1RC:jPh?=
22Rv1 MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MWm3NkBp MYjJR|UxKD1iM{[uOlYh|ryP NHT1b5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS0PFE{QSd-Mkm0OFgyOzl:L3G+
22Rv1 NGHsU5NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MoDWNVIhcA>? Mkn2TWM2OCB;IEO2MlY3KM7:TR?= Mkn3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NUi1NVgoRjJ7N{W4OVE5RC:jPh?=
LNCAP M4rIfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NVXrZlVVOTJiaB?= MUDJR|UxKD1iNEKuN|ch|ryP NFrGSVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUe1PFUyQCd-Mkm3OVg2OTh:L3G+
DU145 Mn;PRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MorZN{Bl[Xm| M4SzVWlEPTBiPTC0Ok4yKM7:TR?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW4PUc,Ojd6MUC1PFk9N2F-
DU145 NIrYdWdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M2\ZN|Mh\GG7cx?= M2rXSWlEPTBiPTC0Ok4yKM7:TR?= MljkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMUe4PVcoRjJ7MUG3PFk4RC:jPh?=
Assay
Methods Test Index PMID
Western blot AR / ERG / NOTCH1 / PSA / Cleaved PARP1 / Cleaved caspase 7 ; AR-FL / AR-v7 / pAR(S213) / pAkt(S473) / pMdm2(S166) ; CXCR7 28607007 26378044 29277895
Growth inhibition assay Cell proliferation 28115200
Immunofluorescence AR ; pAKT(S473) ; CXCR7 27588408 29277895
ELISA osteoprotegerin 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 (from reference)

Kinase Assay:[3]
  • 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]
  • 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]
  • 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
(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 3 years -20°C powder
2 years -80°C in solvent
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)

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%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT04475601 Terminated Drug: Enzalutamide Pill COVID-19|Corona Virus Infection Andreas Josefsson|Umeå University|Sahlgrenska University Hospital Sweden|University Hospital Umeå|Uppsala University Hospital|Skane University Hospital|Jonkoping County Hospital|Sundsvall Hospital|Helsingborgs Hospital|Göteborg University|Astellas Pharma Europe Ltd.|Norrlands University Hospital|Västerbotten County Council July 15 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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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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