GW4064

For research use only.

Catalog No.S2782

20 publications

GW4064 Chemical Structure

CAS No. 278779-30-9

GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.

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Selleck's GW4064 has been cited by 20 publications

Purity & Quality Control

Choose Selective FXR Inhibitors

Biological Activity

Description GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.
Targets
FXR [1]
(CV1)
65 nM(EC50)
In vitro

GW 4064 is a full agonist with EC50 values of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors and an established reporter gene. There is no activity of GW 4064 on other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. Thus, GW 4064 is a potent and selective nonsteroidal FXR agonist. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 NVuzNFFvTnWwY4Tpc44h[XO|YYm= NHXMRnVC\2:waYP0bYMh[WO2aY\peJkh[XRiRmjSJIlvKEiHS{K5N{Bk\WyuczDifUBISUx2IITyZY5{[WO2aY\heIlwdiCjY4Tpeol1gSxiRVO1NEA:KDBwMEeg{txONg>? MoKyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd{OUK2NVAoRjF5MkmyOlExRC:jPh?=
CV1 MnzxSpVv[3Srb36gZZN{[Xl? NXO0ZmdbSWexbnnzeEBi[3Srdnn0fUBifCCIWGKg[ZhxemW|c3XkJIlvKGGocnnjZY4h\3KnZX6gcY9vc2W7IFPWNUBk\WyuczDifUBtfWOrZnXyZZNmKHKncH;yeIVzKHS{YX7zbYVvfCC2cnHud4Zm[3Srb36gZZN{[XluIFXDOVAhRSByLkC2OUDPxE1w NFjOWIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOE[yNVUzOyd-MUi2NlE2OjN:L3G+
CV1 NGTFeHZHfW6ldHnvckBie3OjeR?= MYXB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIF\YVkB1emGwc3\lZ5Rm\CCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEXjFiY3XscJMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKHS{YX7zbYVvfCC2cnHud4Zm[3Srb36gZZN{[XluIFXDOVAhRSByLkC2OUDPxE1w MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTRzMES2NEc,OTl2MUC0OlA9N2F-
CV1 Mlm1SpVv[3Srb36gZZN{[Xl? NGPOT3BKdmO{ZXHz[UBqdiCqdX3hckBHYFJvbXXkbYF1\WRidILhcpNq\W62IITyZY5{[3KrcITpc44hd2ZibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKHS{YX7z[oVkfGWmIHnuJIFnemmlYX6g[5Jm\W5ibX;ub4V6KEOYMTDj[YxteyxiRVO1NEA:KDBwME[1JO69VS5? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTV6Nke2PUc,OTl3OE[3Olk9N2F-
HEK293 MoPHSpVv[3Srb36gZZN{[Xl? MlmyRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDmeYxtKGynbnf0bEBHYFJidILhcpNn\WO2ZXSgbY4hUEWNMkmzJINmdGy|IHPv[ZhxemW|c3nu[{BxXFKneFTld5QweEeOMoDyc41wfG:{IHHzd4V{e2WmIHHzJIx2[2moZYLhd4Uh[WO2aY\peJkh[nliZHny[YN1KHKncH;yeIVzKGOnbHz1cIFzKGG|c3H5MEBGSzVyIE2gNE4xOyEQvF2u MkHvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4M{iyO|goRjJyNkO4Nlc5RC:jPh?=
HEK293 NFHRVIRHfW6ldHnvckBie3OjeR?= M1;DZmFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gS3NVNW[3c3XkJGZZWiCOQlSg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDjc4V5eHKnc4PpcochT0GOND3EUmEh[mmwZHnnJIRwdWGrbjDhcoQheE[UbIXjJIJ6KG2jbX3hcIlidiCxbnWtbJljemmmIHHzd4F6NCCHQ{WwJF0hOC5yM{Wg{txONg>? M1zvfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkO4Nlc5Lz5{ME[zPFI4QDxxYU6=
CV-1 M{K2XGZ2dmO2aX;uJIF{e2G7 NGnMbJVC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGZZWiCOQlSgbYV5eHKnc4Pl[EBqdiCvb37r[ZkhS1ZvMTDj[YxteyCjc4Pld5Nm\CCjczD0doFve2GldHn2ZZRqd25ib3[gcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHX4dJJme3Orb36sJGVEPTBiPTCwMlA3PSEQvF2u MlewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{NU[wNFUoRjJzMkW2NFA2RC:jPh?=
CV1 MX7GeY5kfGmxbjDhd5NigQ>? MXPB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIF\YVkBNSkRidILhcpNn\WO2ZXSgbY4h[W[{aXPhckBoemWnbjDtc45s\XliQ2[xJINmdGy|IHHmeIVzKG:4ZYLubYdpfCCrbnP1ZoF1cW:wIHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NEA:KDBwME[1JO69VS5? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTh7MEO1Okc,OjF6OUCzOVY9N2F-
HEK293 MVXGeY5kfGmxbjDhd5NigQ>? MX7B[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIILlZ49u[mmwYX70JGZZWiCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGOxZYjwdoV{e2mwZzDDUXguT0GONF6gZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxKD1iMD6wO{DPxE1w MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV6M{[xO{c,OjJ3OEO2NVc9N2F-
HEK293 M3uxTWZ2dmO2aX;uJIF{e2G7 NI\idGdC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGZZWiCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3MDC9JFAvODJ4IN88UU4> NVOxeox7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNFU3QDhpPkK1N|A2Pjh6PD;hQi=>
CV1 MXTGeY5kfGmxbjDhd5NigQ>? MkDHRYdwdmm|dDDhZ5Rqfmm2eTDheEBHYFJiKIXub45wf25ib4Lp[4lvMSC2cnHud4Zm[3SnZDDpcpRwKGGocnnjZY4h\3KnZX6gcY9vc2W7IFPWNUBk\WyuczDhd5Nme3OnZDDhd{BtcWejbnStcYVlcWG2ZXSgeJJidnOlcnnweIlwdiCkeTDseYNq\mW{YYPlJJJmeG:{dHXyM{B1emGwc3nlcpQhfHKjboPm[YN1cW:wIHHzd4F6NCCHQ{WwJF0hOC5yNkWg{txONg>? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR7OUi4N{c,OjV2OUm4PFM9N2F-
HeLa M2rFXWZ2dmO2aX;uJIF{e2G7 NHyweHgzPCCqcoO= M{P3VGFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6g[pVtdCCuZX7neIghTliUIHX4dJJme3OnZDDpckBJ\UyjIHPlcIx{KGOxdILhcpNn\WO2ZXSge4l1cCCyU1e1MYh2dWGwIGLYVkBi\nSncjCyOEBpenNiYomgSJVidC2JbH:gcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwJF0hOC53MTFOwG0v NWPlcIpsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5N|QzOjdpPkK1PVM1OjJ5PD;hQi=>
HEK293 MkG0SpVv[3Srb36gZZN{[Xl? MWLB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIF\YVkB1emGwc3\lZ5Rm\CCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3MDC9JFAvOzd|IN88UU4> M1\jXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4NVQ1Lz5{NkW2PFE1PDxxYU6=
HEK-293 NHfndotHfW6ldHnvckBie3OjeR?= MY\B[49vcXO2IHHjeIl3cXS7IHH0JGMufGW{bXnuZYwhT2GuND30ZYdo\WRiaIXtZY4hTliUIDixPFchfG9iNEeyJJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iSFXLMVI6OyClZXzsd{Bkdy2neIDy[ZN{cW6pIIDGVox2[yCkeTDtZY1u[WyrYX6gc45mKGi7YoLp[EBie3OjeTygSWM2OCB;IECuNFM2KM7:TT6= M2DnNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5Mk[4Olk3Lz5{N{K2PFY6PjxxYU6=
insect cells NELiOJpHfW6ldHnvckBie3OjeR?= MWSxJIhz MorERYdwdmm|dDDhZ5Rqfmm2eTDheEBz\WOxbXLpcoFvfCCqdX3hckBIW1RvdHHn[4VlKE[[UjDsbYdidmRiYnnu[Ilv\yCmb33hbY4hMDF7MzD0c{A1PzJicnXzbYR2\XNrIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCrboPlZ5Qh[2WubIOgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIHnueIVz[WO2aX;uJJdqfGhiYnnveIlvKGyjYnXscIVlKFOUQz2xJIFnfGW{IEGgbJIh[nliSGTSSkBie3OjeTygSWM2OCB;IECuNFE6KM7:TT6= NFnXT289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG0PFgxPid-MkmxOFg5ODZ:L3G+
HEK293T NU\mc5ZETnWwY4Tpc44h[XO|YYm= MXeyOEBpenN? M4XVVGFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gSnhTKGW6cILld5Nm\CCrbjDISWszQTOWIHPlcIx{KGG|c3Xzd4VlKGG|IFLTSXAheHKxbX;0[ZIh\HKrdnXuJINmdGy3bHHyJJRz[W6|Y4LpdJRqd26jbDDhZ5Rqfmm2eTDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyIE2gNE4xQTVizszNMi=> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF2OEiwOkc,OjlzNEi4NFY9N2F-
HepG2 MYPGeY5kfGmxbjDhd5NigQ>? M1X3c|EhfU1? NHzXd|cyQCCqcoO= NVTjRolFTGWlcnXhd4UhcW5iQ2nQO2EyKGenbnWg[ZhxemW|c3nvckBqdiCqdX3hckBJ\XCJMjDj[YxteyCjdDCxJJVOKGGodHXyJFE5KGi{czDifUBTXC2SQ2K= NFi0PZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{m2N|M4OSd-MUe5OlM{PzF:L3G+
Caco-2 M3;HeWZ2dmO2aX;uJIF{e2G7 M1vpRVEhfU1? M1HjRVYh\GG7cx?= MYTBZ5RqfmG2aX;uJI9nKEmEQVLQJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDDZYNwNTJiY3XscJMh[XRiMTD1UUBi\nSncjC2JIRigXNiYomgVnQuWEOU M2fSNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5OU[zN|cyLz5zN{m2N|M4OTxxYU6=
HepG2 MXzGeY5kfGmxbjDhd5NigQ>? M3S3ZlEhfU1? NIG0W24yQCCqcoO= M{HrV2FkfGm4YYTpc44hd2ZiQmPFVEBo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gTIVxTzJiY3XscJMh[XRiMTD1UUBi\nSncjCxPEBpenNiYomgVnQuWEOU MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzl4M{O3NUc,OTd7NkOzO|E9N2F-
Huh7 NGK1W2RHfW6ldHnvckBie3OjeR?= NGDJeoUyKHWP MlrJNVghcHK| MVjBZ5RqfmG2aX;uJI9nKFOKUDDn[Y5mKGW6cILld5Nqd25iaX6gbJVu[W5iSIXoO{Bk\WyuczDheEAyKHWPIHHmeIVzKDF6IHjyd{BjgSCUVD3QR3I> NE\LS3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{m2N|M4OSd-MUe5OlM{PzF:L3G+
Huh7 NXzjU|NNTnWwY4Tpc44h[XO|YYm= MonyNUB2VQ>? NVK5VXM5OThiaILz M3e0U2FkfGm4YYTpc44hd2ZiQmPFVEBo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gTJVpPyClZXzsd{BifCBzIIXNJIFnfGW{IEG4JIhzeyCkeTDSWE1RS1J? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzl4M{O3NUc,OTd7NkOzO|E9N2F-
HepG2 NX7NS4FXTnWwY4Tpc44h[XO|YYm= NEPCTJQyOCC3TR?= Mn\XTY5lfWO2aX;uJI9nKE[[Uj3t[YRq[XSnZDDTTHAhdVKQQTDlfJBz\XO|aX;uJIlvKHOncoXtMZN1[XK4ZXSgbJVu[W5iSHXwS|Ih[2WubIOgZZQhOTBidV2gcYVie3W{ZXSgZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkheVCFUjDhcoFtgXOrcx?= NHfsfWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{O3Nlg1OCd-MkezO|I5PDB:L3G+
HepG2 M2TqPGZ2dmO2aX;uJIF{e2G7 M1vZc|ExKHWP NWXudoQxOTBibXnudy=> Mle4TY5lfWO2aX;uJI9nKE[[Uj3t[YRq[XSnZDDBb5QueGixc4Doc5J6dGG2aX;uJIF1KFN2N{Ogd4l1\SCrbjDz[ZJ2dS2|dHHyeoVlKGi3bXHuJGhmeEd{IHPlcIx{KGG2IEGwJJVOKG2nYYP1doVlKGGodHXyJFExKG2rboOgZpkhf2W|dHXyckBjdG:2IHHuZYx6e2m| MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzN5Mki0NEc,Ojd|N{K4OFA9N2F-
HepG2 Mnm4SpVv[3Srb36gZZN{[Xl? MX6xNEB2VQ>? NVPRU|ZiOTBibXnudy=> M2rIPGlv\HWldHnvckBw\iCIWGKtcYVlcWG2ZXSgRYt1NXCqb4PwbI9zgWyjdHnvckBqdiC|ZYL1cU1{fGG{dnXkJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIFfTT{0{[mW2YT3wbI9{eGixconsZZRqd25iYYSgNVAhfU1ibXXhd5Vz\WRiYX\0[ZIhOTBibXnud{BjgSC5ZYP0[ZJvKGKub4SgZY5idHm|aYO= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzN5Mki0NEc,Ojd|N{K4OFA9N2F-
HepG2 MVPGeY5kfGmxbjDhd5NigQ>? M37sUVExKHWP NFva[FlC[3SrdnH0bY9vKG:oIF\YVkBqdiCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczD1dJJm\3WuYYTpc44hd2ZiU1jQJI1TVkFiZYjwdoV{e2mxbjDheEAyOCC3TTDifUBTXC2SQ2KgcYV1cG:m NVX4T2FbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwN|E3OThpPkOwNFMyPjF6PD;hQi=>
HepG2 NHfzZXNHfW6ldHnvckBie3OjeR?= M{TQd|ExKHWP Mn7ORYN1cX[jdHnvckBw\iCIWGKgbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNidYDy[Yd2dGG2aX;uJI9nKE[[UjDtVm5CKGW6cILld5Nqd25iYYSgNVAhfU1iYomgVnQuWEOUIH3leIhw\A>? Ml7BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByM{G2NVgoRjNyMEOxOlE5RC:jPh?=
HepG2 M1XXO2Z2dmO2aX;uJIF{e2G7 NU\iepRsOTBidV2= NFnzV|NC[3SrdnH0bY9vKG:oIF\YVkBqdiCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDkc5dvemWpdXzheIlwdiCxZjDTVmVDWC1zYzDtVm5CKGW6cILld5Nqd25iYYSgNVAhfU1iYomgVnQuWEOUIH3leIhw\A>? NEDPfoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzNVYyQCd-M{CwN|E3OTh:L3G+
3T3L1 NIHXcZZHfW6ldHnvckBie3OjeR?= M1HRNlExKHWP M4\DVXJm\HWldHnvckBqdiCuaYDp[EBi[2O3bYXsZZRqd25iaX6gcY92e2ViM2SzUFEh[2WubIOgZZQhOTBidV2gZpkhV2muIGLl[EBQKHO2YXnubY5oNWKjc3XkJIFje2:{YnHuZ4UhdWW2aH;kJJJmdGG2aY\lJJRwKGOxboTyc4w> NVLOXpFNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOFI6PTdpPkOwN|QzQTV5PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PTEN / p-AKT / AKT ; 

PubMed: 25187826     


Protein expression levels of PTEN, phosphorylated and total Akt in LNcaP cells treated with a vehicle control (DMSO), CDCA or GW4064. 

p-EGFR / EGFR / p-ERK / ERK / p-Src / Src ; 

PubMed: 23119029     


A. Time-course and dose-response for GW4064-induced inhibition of EGFR (Tyr845) phosphorylation. B. Time-course and dose-response for GW4064-induced inhibition of ERK1/2 phosphorylation. C. Time-course and dose-response for GW4064-induced inhibition of Src (Tyr 416) phosphorylation. Phosphorylation of EGFR (Tyr845), ERK1/2 and Src (Tyr 416) was determined by immunoblotting with anti-phospho-EGFR (Tyr845), anti-phospho-ERK1/2 and anti-phospho-Src (Tyr 416) antibody, respectively. For time-course experiments, SNU-C4 cells were treated with 1 µM GW4064 for the indicated times at 37°C. For dose-response experiments, cells were treated with the indicated concentrations of GW4064 for 20 min at 37°C. Immunoblotting for total EGFR, ERK2 or Src was used as a loading control. Immunoblots are representative of at least 3 separate experiments. Numbers between immunoblots represent densitometry. Experimental/control ratios were calculated after normalizing each test band to the respective EGFR, ERK2 or Src band.

SOCS3 / p21 / p-STAT3 / STAT3 ; 

PubMed: 26416445     


HepG2 cells and Huh7 cells were treated with GW4064 (2 μM) or vehicle DMSO for 24 h. The protein levels of SOCS3, p21, total STAT3 (t-SATA3) and phosphoraylated STAT3 (p-STAT3) were assayed by Western blot, taking GAPDH as a loading control

25187826 23119029 26416445
Growth inhibition assay
Cell proliferation ; 

PubMed: 25187826     


LNcaP cells were treated with CDCA (5 μM), GW4064 (2 μM) or vehicle control (DMSO) and cell proliferation ability was measured using BrdU assays. A450 absorption was assayed following treatment for 24 h. 

25187826
In vivo Pharmacokinetic analysis in rats shows that GW 4064 possesses an oral bioavailability of 10% with a t1/2 = 3.5 h. Fisher rats are dosed with GW 4064 by oral gavage. After 7 days, a dose-dependent lowering of serum triglycerides is observed in the rats receiving GW 4064, with an ED50 = 20 mg/kg. [2]

Protocol

Animal Research:

[2]

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  • Animal Models: Fisher rats
  • Dosages: 0-100 mg/kg
  • Administration: Orally, b.i.d.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (184.21 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.
11 mg/mL

* 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 542.84
Formula

C28H22Cl3NO4

CAS No. 278779-30-9
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)C1=C(C(=NO1)C2=C(C=CC=C2Cl)Cl)COC3=CC(=C(C=C3)C=CC4=CC(=CC=C4)C(=O)O)Cl

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

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