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 394 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 NHTzb2pEgXSxdH;4bYMhSXO|YYm= M1n3Rlch\GG7cx?= MorwPVUmKEW2T1i= NVL0d2JrUUN3ME21MlEzKM7:TR?= NWm0SmdiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
human LNCAP M1LTXmZ2dmO2aX;uJGF{e2G7 NETXUYgyKM7:TR?= MWrEUXNQ MU\Jcohq[mm2czDwdo9{fGG2ZTDzdIVkcW[rYzDhcpRq\2WwIIPlZ5JmfGmxbjDpckBpfW2jbjDMUmNCWCClZXzsd{BmgHC{ZYPzbY5oKGGwZILv[4VvKHKnY3XweI9zKGG2IEGwNE0yODBybl2= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODJzOEexO{c,OjB{MUi3NVc9N2F-
VCaP NUjYWms2TnWwY4Tpc44hSXO|YYm= NHzqT2syOCEQvF2= NVSzTWxxOjRiaB?= M3nh[GROW09? M4fkVXN2eHC{ZYPz[ZMhdGmpYX7kMY1m\GmjdHXkJGFTNU[OIIPp[45idGmwZx?= NVrHbplYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3NVA1OzZpPkKyO|ExPDN4PD;hQi=>
BCK4 NFyzVHlHfW6ldHnvckBCe3OjeR?= NXLkO|NCOTBizszN MWK3JIRigXN? M2njdWROW09? NHjMXmNKdmirYnn0d{Bme3S{YXTpc4wudWWmaXH0[YQheHKxbHnm[ZJifGmxbh?= M2\YXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEWxNVA6Lz5{NES1NVExQTxxYU6=
MCF7s MYPGeY5kfGmxbjDBd5NigQ>? NE\jR4gyOCEQvF2= NEnCb3Y3KGSjeYO= NIWzWotFVVOR M1fBOmlvcGmkaYTzJIV{fHKjZHnvcE1u\WSrYYTl[EBxem:uaX\ldoF1cW:w MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR3MUGwPUc,OjR2NUGxNFk9N2F-
PC-3 NWjlWm5oTnWwY4Tpc44hSXO|YYm= MV2xNEDPxE1? NXvCSXpSPzJiaB?= M3yxRmROW09? NVXMXHJOTG:nczDuc5QhcW6qaXLpeEBk\WyuIIDyc4xq\mW{YYTpc44> NXfES|JbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzOFQ5PjRpPkK1N|Q1QDZ2PD;hQi=>
CWR22Rv1 MlT2SpVv[3Srb36gRZN{[Xl? NEjteHIyPSEQvF2= MYqyOEBp MnqzSG1UVw>? MnXNSI9meyCwb4SgZYZn\WO2IITo[UBnfWyuIHzlcod1cCCDUjDlfJBz\XO|aX;u NHr0OXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exN|U3Pyd-MkO3NVM2Pjd:L3G+
LNCAP/AR MXLBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 NWryN2FuUUN3MDC9JFAvODJzIN88US=> NWDDR4tZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke3NVc2PDRpPkK3O|E4PTR2PD;hQi=>
MDA-MB-453 MYnBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 MlGzSWM2OCB;IECuNFQ6KM7:TR?= NY[0[lhCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
LNCAP Mm\uRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= M3OyfFczKGh? MkLBTWM2OCB;IECuNFUh|ryP NIXCVpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG5N|IyPSd-M{CxPVMzOTV:L3G+
LNCAP MnPhRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= NVzaem5{PzJiaB?= NX34WFd5UUN3MDC9JFAvODlizszN M2jHSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMUmzNlE2Lz5|MEG5N|IyPTxxYU6=
LNCAP MlLFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3v4PWdKPTBiPTCwMlEzKM7:TR?= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDBzMUKxPUc,OjhyMUGyNVk9N2F-
LNCAP M4K1fmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NF\JSG8{KGSjeYO= NWHPTVYyUUN3MDC9JFAvOTJ5MTFOwG0> Ml7XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyNE[zNVMoRjJ4MES2N|E{RC:jPh?=
LNCAP MkjNRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= M3zHd|Yh\GG7cx?= NVTU[HFVT0l3MDC9JFAvOjlizszN M32zNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEGxNlE6Lz5{OECxNVIyQTxxYU6=
UAS-bla GripTite 293 MUjBcpRi\2:waYP0JIFkfGm4aYT5JIF{e2G7 M4jNNlE3KHSxIEK0JIg> MWHJR|UxKD1iMD6zOlEh|ryP MkK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
mammalian expression system Mnq3RY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= M134XFIzKHSxIEK0JIg> MVHFR|UxKD1iMD60NkDPxE1? M33nS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{i1OVA{Lz5{OEO4OVUxOzxxYU6=
VCaP MlHXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGrxVXQyPDRiaB?= NXH6RmNsT0l3MDC9JFAvPjFizszN MlfNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMkG1PFYoRjJ3MUKxOVg3RC:jPh?=
LNCaP M1PtN2FvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= MVGyJIg> NY\lc|UxTUN3MDC9JFAvQTF3IN88US=> NUj1cIJNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3NVM2PjdpPkKzO|E{PTZ5PD;hQi=>
COS7 M3TxW2FvfGGpb37pd5Qh[WO2aY\peJkh[XO|YYm= NEjVXogzPCCq NFrZ[|RKSzVyIE2gNU4zPiEQvF2= M33nN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUG3PFk4Lz5{OUGxO|g6PzxxYU6=
AR LBD mutant MnzIRY51[WexbnnzeEBi[3Srdnn0fUBie3OjeR?= M2PDNFQhcA>? M13m[2lEPTBiPTCxMlM2KM7:TR?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW4PUc,Ojd6MUC1PFk9N2F-
LNCAP NF3L[pZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1n5e2dKPTBiPTCyMlg5KM7:TR?= MlHBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4M{SxN|AoRjJ3NkO0NVMxRC:jPh?=
CWR22Rv1 MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHfI[3ZIUTVyIE2gN{4{PCEQvF2= NV\xV|N[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2N|QyOzBpPkK1OlM1OTNyPD;hQi=>
LNCAP MXfDfZRwfG:6aXPpeJkh[XO|YYm= NXjmO5NiPyCmYYnz NWG5TWxqT0l3MDC9JFUvOTJizszN M{O0TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{GzOVY4Lz5{M{exN|U3PzxxYU6=
PC3 NV;VflEyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUXHTVUxKD1iOT6xOUDPxE1? M4myRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkO0NVMxLz5{NU[zOFE{ODxxYU6=
CWR22Rv1 MonrR4VtdCC|dYL2bZZidCCjc4PhfS=> NVTSUWM5OTR2IHi= MYPJR|UxKD1iOT63JO69VQ>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF{MUW4Okc,OjVzMkG1PFY9N2F-
LNCAP MoLtRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M{H0fVk3KGh? MlvQTWM2OCB;IEGxMlQ4KM7:TR?= NGH5W|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{OwNVM3QCd-MkezNFE{Pjh:L3G+
LNCaP-hr NXj2NmI4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MWizJIRigXN? M{ftXWlEPTBiPTCxNk42KM7:TR?= NVixb5cyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QDlpPkK3PFExPTh7PD;hQi=>
LNCAP M3\wZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NV3ScIlpOyCmYYnz M3;kRmlEPTBiPTCxNk42KM7:TR?= M4joPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUG3PFk4Lz5{OUGxO|g6PzxxYU6=
LNCaP NHXVVXhCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 M2\nTVE1PCCq NY\WVGRyT0l3MDC9JFE5Njh6IN88US=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ5Mki5OEc,Ojh{N{K4PVQ9N2F-
LNCaP-AR Mk\NS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXPaUHA1OTR2IHi= M1nkPGdKPTBiPTCxPE46KM7:TR?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF{MUW4Okc,OjVzMkG1PFY9N2F-
C4-2B M4n5RmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MkO3NVIhcA>? NETYXIJKSzVyIE2gNlAvPzdizszN NVfKfldORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVg2OThpPkK5O|U5PTF6PD;hQi=>
A31 MknrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYO3NkBp M4nWeGdKPTBiPTCyO{42KM7:TR?= NGHkOm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECxNVIyQSd-MkiwNVEzOTl:L3G+
22Rv1 M1\rbmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 Mki1PVYhcA>? MWXJR|UxKD1iM{GuO|Yh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzNyMUO2PEc,Ojd|MEGzOlg9N2F-
22Rv1 Mli4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MV65OkBp MlXYTWM2OCB;IEOxMlc3KM7:TR?= MkHRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ7NkW4OlIoRjJ4OU[1PFYzRC:jPh?=
DU145 M2S1cGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 M{L1N|k3KGh? NHLVcW5KSzVyIE2gN|IvOjdizszN Mn\LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|MEGzOlgoRjJ5M{CxN|Y5RC:jPh?=
LNCAP MlLqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? NGTYe4I4OiCq MWfJR|UxKD1iM{OuPFQh|ryP MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2OEGzPUc,Ojl2NEixN|k9N2F-
CW22Rv1 NI\hUmxCdnSjZ3;ubZN1KGGldHn2bZR6KGG|c3H5 MYW3NkBp NFTqXYdKSzVyIE2gN|UvPzVizszN M1PJeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkeyPFk1Lz5{OEK3Nlg6PDxxYU6=
22Rv1 M1TrbmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MknhO|IhcA>? Mm\MTWM2OCB;IEO2MlY3KM7:TR?= NVLFRlBCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OFgyOzlpPkK5OFQ5OTN7PD;hQi=>
22Rv1 MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? M1n2XFEzKGh? NXHpc2ZTUUN3MDC9JFM3NjZ4IN88US=> NV3mcWhGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVg2OThpPkK5O|U5PTF6PD;hQi=>
LNCAP M4jFOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MWOxNkBp M2\vfmlEPTBiPTC0Nk4{PyEQvF2= NITn[mM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUe1PFUyQCd-Mkm3OVg2OTh:L3G+
DU145 NIXUS4NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M17TbFMh\GG7cx?= NGTWRo9KSzVyIE2gOFYvOSEQvF2= NYLUfYFtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QDlpPkK3PFExPTh7PD;hQi=>
DU145 NFrTSYVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M2ruN|Mh\GG7cx?= NEmw[lRKSzVyIE2gOFYvOSEQvF2= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTFzN{i5O{c,OjlzMUe4PVc9N2F-
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)

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

mg/kg g μL

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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
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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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