EPZ015666 (GSK3235025)

Catalog No.S7748

For research use only.

EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.

EPZ015666 (GSK3235025) Chemical Structure

CAS No. 1616391-65-1

Selleck's EPZ015666 (GSK3235025) has been cited by 18 publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
Targets
PRMT5 [1]
(Cell-free assay)
5 nM(Ki)
In vitro

EPZ015666 shows potent cellular activity that blocks symmetric dimethylation of SmD3 and inhibit proliferation of MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) with IC50 of 96-904 nM. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-468 NIDpSYtHfW6ldHnvckBie3OjeR?= MUm0PEBp Mly2bY5pcWKrdIOgVHJOXDViYXP0bZZqfHl? NHr0SlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm1O|k5QCd-M{C5OVc6QDh:L3G+
HCC1954 MlrlR4VtdCC4aXHibYxqfHliYYPzZZk> MXzJR|UxRTBwODFOwG0> NFy5eIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm1O|k5QCd-M{C5OVc6QDh:L3G+
MDA-MB-453 NY\qUpI2S2WubDD2bYFjcWyrdImgZZN{[Xl? M{S0fWlEPTB;MTFOwG0> MljrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NUe5PFgoRjNyOUW3PVg5RC:jPh?=
HCC38 NEH1O3ZE\WyuII\pZYJqdGm2eTDhd5NigQ>? MVnJR|UxRTJwMjFOwG0> M1noZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUW3PVg5Lz5|MEm1O|k5QDxxYU6=
MDA-MB-468 M4f5WGNmdGxidnnhZoltcXS7IHHzd4F6 Ml74TWM2OD1{LkKg{txO M{Dn[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUW3PVg5Lz5|MEm1O|k5QDxxYU6=
MCF7 NU\aRmpWS2WubDD2bYFjcWyrdImgZZN{[Xl? NYDle45pUUN3ME2yMlYh|ryP Ml33QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NUe5PFgoRjNyOUW3PVg5RC:jPh?=
SKBR3 MV7D[YxtKH[rYXLpcIl1gSCjc4PhfS=> M17mbmlEPTB;Mz65JO69VQ>? NHLLdII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm1O|k5QCd-M{C5OVc6QDh:L3G+
Sf9 NF3wZ2lHfW6ldHnvckBie3OjeR?= NUTzZlJmUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcO0ifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xOjMQvF2= NXvEVmtzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2Nlg{OjZpPkK5OlI5OzJ4PD;hQi=>
Sf9 NEHhc4FHfW6ldHnvckBie3OjeR?= M3XOfGlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gSmxCTy22YXfn[YQhWFKPVEWv[pVtdCCuZX7neIghemWlb33ibY5idnRiaIXtZY4hUGm|Nj30ZYdo\WRiTVXQOVAh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiYnnveIlvgWyjdHXkJIhqe3SxbnWgdIVxfGmmZTDhd{B{fWK|dILheIUhcW5icILld4Vv[2Vib3[gX|RJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUCuNFIz|ryP MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ{OEOyOkc,Ojl4MkizNlY9N2F-
Sf9 MYrGeY5kfGmxbjDhd5NigQ>? M3u3RWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gSmxCTy22YXfn[YQhWFKPVEWv[pVtdCCuZX7neIghemWlb33ibY5idnRiaIXtZY4hUGm|Nj30ZYdo\WRiTVXQOVAh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiYnnveIlvgWyjdHXkJIhqe3SxbnWgdIVxfGmmZTDhd{B{fWK|dILheIUhcW5icILld4Vv[2Vib3[gX|VJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUCuNFIz|ryP NFHIPVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO2OlYyPyd-M{CzOlY3OTd:L3G+
Sf9 Mk\oSpVv[3Srb36gZZN{[Xl? NFHIWGxKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHs3UF1vU1HNJIJ6KFSxcHPveY51KG2ndHjv[EwhUUN3ME2wMlAzOs7:TR?= M4LMOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[2OlE4Lz5|MEO2OlYyPzxxYU6=
Sf9 NHy0VHdHfW6ldHnvckBie3OjeR?= M1nSeWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gSmxCTy22YXfn[YQhWFKPVEWv[pVtdCCuZX7neIghemWlb33ibY5idnRiaIXtZY4hUGm|Nj30ZYdo\WRiTVXQOVAh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiYnnveIlvgWyjdHXkJIhqe3SxbnWgdIVxfGmmZTDhd{B{fWK|dILheIUhcW5icILld4Vv[2Vib3[gX|dJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUCuNFQ4|ryP MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4Nk[xO{c,OzB|Nk[2NVc9N2F-
Sf9 NV20eopqTnWwY4Tpc44h[XO|YYm= NXzmeo9qUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcQEifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xPDgQvF2= NXfiSHI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlY3OTdpPkOwN|Y3PjF5PD;hQi=>
Sf9 NULGUmpbTnWwY4Tpc44h[XO|YYm= Mme5TY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbPWheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MD6wOFfPxE1? NYO5U3FTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C2NFU5OzBpPkOwOlA2QDNyPD;hQi=>
Sf9 MliySpVv[3Srb36gZZN{[Xl? MoC1TY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbNVBJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUCuNFQ4|ryP M{PJbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNkC1PFMxLz5|ME[wOVg{ODxxYU6=
Sf9 NEi4V|RHfW6ldHnvckBie3OjeR?= NYXn[YxIUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcOTGKXT3TRW0h[nliVH;wZ492dnRibXX0bI9lNCCLQ{WwQVAvODR5zszN MlrRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4MEW4N|AoRjNyNkC1PFMxRC:jPh?=
Sf9 M4WzcWZ2dmO2aX;uJIF{e2G7 NH;Qe4NKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHsyOkifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xPDgQvF2= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODZyNUizNEc,OzB4MEW4N|A9N2F-
Sf9 MlWzSpVv[3Srb36gZZN{[Xl? NEnDbYdKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHsyO0ifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xQTcQvF2= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh5MEK1PEc,Ojl6N{CyOVg9N2F-
Sf9 NI\WU2hHfW6ldHnvckBie3OjeR?= MoTCTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbNVRJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBIUTVyPUCuNVA3|ryP M2rxVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNkC1PFMxLz5|ME[wOVg{ODxxYU6=
Sf9 M2G3eWZ2dmO2aX;uJIF{e2G7 MYfJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6|ZXP0JINmdGy|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuxOWheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGdKPTB;MD6xNFbPxE1? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODZyNUizNEc,OzB4MEW4N|A9N2F-
Sf9 NFv2VYJHfW6ldHnvckBie3OjeR?= NWXDcFc{UW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcOT[KXT3TRW0h[nliVH;wZ492dnRibXX0bI9lNCCJSUWwQVAvOjF{zszN NEjWV2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|ME[wOVg{OCd-M{C2NFU5OzB:L3G+
Sf9 NILSc5hHfW6ldHnvckBie3OjeR?= NF:1b2tKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHsyP0ifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEeLNUC9NE4zOTMQvF2= M3HTOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNkC1PFMxLz5|ME[wOVg{ODxxYU6=
Sf9 NXfwRXlRTnWwY4Tpc44h[XO|YYm= M4XHWWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gSmxCTy22YXfn[YQhWFKPVEWv[pVtdCCuZX7neIghemWlb33ibY5idnRiaIXtZY4hUGm|Nj30ZYdo\WRiTVXQOVAh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiYnnveIlvgWyjdHXkJIhqe3SxbnWgdIVxfGmmZTDhd{B{fWK|dILheIUhcW5icILld4Vv[2Vib3[gX|E5UF1vU1HNJIJ6KFSxcHPveY51KG2ndHjv[EwhUUN3ME2wMlQ2|ryP MoX4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl6N{CyOVgoRjJ7OEewNlU5RC:jPh?=
Sf9 MYHGeY5kfGmxbjDhd5NigQ>? MlPsTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbNVlJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUCuPVbPxE1? M3;vcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[2OlE4Lz5|MEO2OlYyPzxxYU6=
Sf9 MV\GeY5kfGmxbjDhd5NigQ>? MUjJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6|ZXP0JINmdGy|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuyNGheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MT6x{txO NYjPR5VFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlY3OTdpPkOwN|Y3PjF5PD;hQi=>
Sf9 MmfySpVv[3Srb36gZZN{[Xl? NF:1NIVKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHszOUifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NU45|ryP M2PESVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[2OlE4Lz5|MEO2OlYyPzxxYU6=
Sf9 NWO4eGt5TnWwY4Tpc44h[XO|YYm= MX;Jcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6|ZXP0JINmdGy|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuyNmheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;Mj62{txO NX\rWGtDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlY3OTdpPkOwN|Y3PjF5PD;hQi=>
Assay
Methods Test Index PMID
Western blot PRMT5 / H3R8me2s ; H4R3me2s 30957988 28945229
Immunofluorescence IKKβ 29158558
Growth inhibition assay Cell viability 30957988
In vivo EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models. [1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1)
  • Concentrations: 5 μM
  • Incubation Time: 12 days
  • Method:

    --

Animal Research:

[1]

  • Animal Models: MCL (Z-138, and Maver-1) xenograft models
  • Dosages: 200 mg/kg BID
  • Administration: p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 383.44
Formula

C20H25N5O3

CAS No. 1616391-65-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CC2=CC=CC=C21)CC(CNC(=O)C3=CC(=NC=N3)NC4COC4)O

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

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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

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

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Frequently Asked Questions

Question 1:
I want to use this compound for injection, how to reconstitute it?

Answer:
S7748, EPZ015666 is a clear solution in 2% DMSO+30% PEG300+68% water and it can be used for tail vein injection.

Tags: buy EPZ015666 (GSK3235025) | EPZ015666 (GSK3235025) supplier | purchase EPZ015666 (GSK3235025) | EPZ015666 (GSK3235025) cost | EPZ015666 (GSK3235025) manufacturer | order EPZ015666 (GSK3235025) | EPZ015666 (GSK3235025) distributor