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EPZ015666 (GSK3235025)

Catalog No.S7748

For research use only.

EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with K_i 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 17 publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Related Compound Libraries

Biological Activity

Description

EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with K_i 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	NGHXd3lHfW6ldHnvckBie3OjeR?=	NIG4Z5M1QCCq	NGrnb5FqdmirYnn0d{BRWk2WNTDhZ5Rqfmm2eR?=	NEXrTZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEm1O\|k5QCd-M{C5OVc6QDh:L3G+
HCC1954	NXm0d2tPS2WubDD2bYFjcWyrdImgZZN{[Xl?		NGjEb\|VKSzVyPUCuPEDPxE1?	NEH5NpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEm1O\|k5QCd-M{C5OVc6QDh:L3G+
MDA-MB-453	MlPiR4VtdCC4aXHibYxqfHliYYPzZZk>		NEPYXYdKSzVyPUGg{txO	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl3N{m4PEc,OzB7NUe5PFg9N2F-
HCC38	NVXqfXh{S2WubDD2bYFjcWyrdImgZZN{[Xl?		NITkR2RKSzVyPUKuNkDPxE1?	MljrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NUe5PFgoRjNyOUW3PVg5RC:jPh?=
MDA-MB-468	MnPSR4VtdCC4aXHibYxqfHliYYPzZZk>		MoXwTWM2OD1{LkKg{txO	NHXncFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEm1O\|k5QCd-M{C5OVc6QDh:L3G+
MCF7	MkPaR4VtdCC4aXHibYxqfHliYYPzZZk>		M4DDRmlEPTB;Mj62JO69VQ>?	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl3N{m4PEc,OzB7NUe5PFg9N2F-
SKBR3	NUD1Z4x1S2WubDD2bYFjcWyrdImgZZN{[Xl?		MX3JR\|UxRTNwOTFOwG0>	NUK0XHk4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OVc6QDhpPkOwPVU4QTh6PD;hQi=>
Sf9	NFnlTVlHfW6ldHnvckBie3OjeR?=		NXLrXYQ4UW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm\|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcO0ifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xOjMQvF2=	NYPRR3F6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2Nlg{OjZpPkK5OlI5OzJ4PD;hQi=>
Sf9	MUfGeY5kfGmxbjDhd5NigQ>?		MnfoTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbOGheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MD6wNlLPxE1?	MnzEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4MkizNlYoRjJ7NkK4N\|I3RC:jPh?=
Sf9	NXi2UIhzTnWwY4Tpc44h[XO\|YYm=		NXu3R4NiUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm\|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcPUifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xOjMQvF2=	NHHMWWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEO2OlYyPyd-M{CzOlY3OTd:L3G+
Sf9	M2fMc2Z2dmO2aX;uJIF{e2G7		MUnJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGu2TH0uW0GPIHL5JHRweGOxdX70JI1mfGixZDygTWM2OD1yLkCyNu69VQ>?	M1ewS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[2OlE4Lz5\|MEO2OlYyPzxxYU6=
Sf9	Ml7kSpVv[3Srb36gZZN{[Xl?		NY\BVpY4UW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm\|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcP0ifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xPDgQvF2=	M2PEdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[2OlE4Lz5\|MEO2OlYyPzxxYU6=
Sf9	MorZSpVv[3Srb36gZZN{[Xl?		NXXsTZRDUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm\|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcQEifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xPDgQvF2=	NXzlR\|dLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlY3OTdpPkOwN\|Y3PjF5PD;hQi=>
Sf9	M3\YeWZ2dmO2aX;uJIF{e2G7		MoiwTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbPWheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MD6wOFfPxE1?	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODZyNUizNEc,OzB4MEW4N\|A9N2F-
Sf9	NEDIeVJHfW6ldHnvckBie3OjeR?=		MlXwTY5pcWKrdHnvckBw\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	NFTYVoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|ME[wOVg{OCd-M{C2NFU5OzB:L3G+
Sf9	MmrTSpVv[3Srb36gZZN{[Xl?		NGqzTJVKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHsyOUifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xPDgQvF2=	MmiwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4MEW4N\|AoRjNyNkC1PFMxRC:jPh?=
Sf9	MVzGeY5kfGmxbjDhd5NigQ>?		Mn3GTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbNVJJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUCuNFQ4\|ryP	M2HoclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNkC1PFMxLz5\|ME[wOVg{ODxxYU6=
Sf9	NVe4OGV3TnWwY4Tpc44h[XO\|YYm=		NIHJfFBKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHsyO0ifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NE4xQTcQvF2=	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh5MEK1PEc,Ojl6N{CyOVg9N2F-
Sf9	MVTGeY5kfGmxbjDhd5NigQ>?		NILOUG5KdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHsyPEifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEeLNUC9NE4yODcQvF2=	NYCyTFdIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C2NFU5OzBpPkOwOlA2QDNyPD;hQi=>
Sf9	M3;sTGZ2dmO2aX;uJIF{e2G7		M3TDdWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gSmxCTy22YXfn[YQhWFKPVEWv[pVtdCCuZX7neIghemWlb33ibY5idnRiaIXtZY4hUGm\|Nj30ZYdo\WRiTVXQOVAh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiYnnveIlvgWyjdHXkJIhqe3SxbnWgdIVxfGmmZTDhd{B{fWK\|dILheIUhcW5icILld4Vv[2Vib3[gX\|E2UF1vU1HNJIJ6KFSxcHPveY51KG2ndHjv[EwhT0l3ME2wMlExPs7:TR?=	M{LzVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNkC1PFMxLz5\|ME[wOVg{ODxxYU6=
Sf9	MX3GeY5kfGmxbjDhd5NigQ>?		NX;tTo5GUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm\|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcOT[KXT3TRW0h[nliVH;wZ492dnRibXX0bI9lNCCJSUWwQVAvOjF{zszN	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODZyNUizNEc,OzB4MEW4N\|A9N2F-
Sf9	NWr1cI1HTnWwY4Tpc44h[XO\|YYm=		NXnFWIVVUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm\|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcOTeKXT3TRW0h[nliVH;wZ492dnRibXX0bI9lNCCJSUWwQVAvOjF{zszN	M3jVcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNkC1PFMxLz5\|ME[wOVg{ODxxYU6=
Sf9	M{n2TGZ2dmO2aX;uJIF{e2G7		MVfJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuxPGheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MD60Oe69VQ>?	NYe2OFc2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm4O\|AzPThpPkK5PFcxOjV6PD;hQi=>
Sf9	NXvxb5ZWTnWwY4Tpc44h[XO\|YYm=		MYfJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuxPWheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MD65Ou69VQ>?	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4Nk[xO{c,OzB\|Nk[2NVc9N2F-
Sf9	M1vGNGZ2dmO2aX;uJIF{e2G7		MmDyTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbNlBJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUGuNe69VQ>?	NHvHZ\|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEO2OlYyPyd-M{CzOlY3OTd:L3G+
Sf9	NUnxfYFnTnWwY4Tpc44h[XO\|YYm=		MWPJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuyNWheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MT64{txO	NXnNW2pNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlY3OTdpPkOwN\|Y3PjF5PD;hQi=>
Sf9	NWjsTYZlTnWwY4Tpc44h[XO\|YYm=		NV2ySVUxUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm\|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcOjKKXT3TRW0h[nliVH;wZ492dnRibXX0bI9lNCCLQ{WwQVIvPs7:TR?=	M3;hT\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[2OlE4Lz5\|MEO2OlYyPzxxYU6=

Click to View More Cell Line Experimental Data

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: -- (Only for Reference)
Animal Research: ^[1]	Animal Models: MCL (Z-138, and Maver-1) xenograft models Dosages: 200 mg/kg BID Administration: p.o. (Only for Reference)

References	[1] Penebre et al. Epizyme, Inc.

References

[1] Penebre et al. Epizyme, Inc.

Solubility (25°C)

In vitro	DMSO	60 mg/mL warmed (156.47 mM)
	Water	Insoluble
	Ethanol	'48 mg/mL warmed
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. Click to purchase: PEG300	5mg/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	383.44
Formula	C₂₀H₂₅N₅O₃
CAS No.	1616391-65-1
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1CN(CC2=CC=CC=C21)CC(CNC(=O)C3=CC(=NC=N3)NC4COC4)O

Download EPZ015666 (GSK3235025) SDF

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:μL Number of animals:

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
=	×	×

Dilution Calculator Molecular Weight Calculator

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 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.

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