EPZ015666 (GSK3235025)

目录号：S7748 Purity: 97%

EPZ015666 (GSK3235025)是一种有效的，选择性且口服生物有效的 PRMT5 抑制剂，K_i 为 5 nM，选择性比其它 PMTs 高 20,000多倍。

EPZ015666 (GSK3235025) Chemical Structure

CAS: 1616391-65-1

规格	价格	库存
10mM (1mL in DMSO)	RMB 1875.51	现货
5mg	RMB 1602.26	现货
25mg	RMB 4906.16	现货
100mg	RMB 7944.3	现货
1g	RMB 16134.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

客户使用Selleck的EPZ015666 (GSK3235025)发表文献24篇：

产品质控

批次：纯度： >97%

Histone Methyltransferase抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	孵育时间	活性描述	文献信息
MDA-MB-468	NVnPUmx3TnWwY4Tpc44h[XO\|YYm=	MWi0PEBp	MUXpcohq[mm2czDQVm1VPSCjY4Tpeol1gQ>?	M4fJRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUW3PVg5Lz5\|MEm1O\|k5QDxxYU6=
HCC1954	NFj6bolE\WyuII\pZYJqdGm2eTDhd5NigQ>?		M3\1PWlEPTB;MD64JO69VQ>?	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl3N{m4PEc,OzB7NUe5PFg9N2F-
MDA-MB-453	MXPD[YxtKH[rYXLpcIl1gSCjc4PhfS=>		NUTueIR2UUN3ME2xJO69VQ>?	NXTCUXAxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5OVc6QDhpPkOwPVU4QTh6PD;hQi=>
HCC38	Mn;NR4VtdCC4aXHibYxqfHliYYPzZZk>		NVHBV4xOUUN3ME2yMlIh\|ryP	Mn;lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NUe5PFgoRjNyOUW3PVg5RC:jPh?=
MDA-MB-468	NF\DXpBE\WyuII\pZYJqdGm2eTDhd5NigQ>?		MVTJR\|UxRTJwMjFOwG0>	M330WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUW3PVg5Lz5\|MEm1O\|k5QDxxYU6=
MCF7	MoPyR4VtdCC4aXHibYxqfHliYYPzZZk>		NIPHT3ZKSzVyPUKuOkDPxE1?	MkC0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NUe5PFgoRjNyOUW3PVg5RC:jPh?=
SKBR3	NWn4Um1xS2WubDD2bYFjcWyrdImgZZN{[Xl?		NXi0Z284UUN3ME2zMlkh\|ryP	M{fCRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUW3PVg5Lz5\|MEm1O\|k5QDxxYU6=
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Sf9	MkDTSpVv[3Srb36gZZN{[Xl?		NGrpb2pKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHs5UF1vU1HNJIJ6KFSxcHPveY51KG2ndHjv[EwhUUN3ME2wMlA1P87:TR?=	M4rYRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[2OlE4Lz5\|MEO2OlYyPzxxYU6=
Sf9	M1zUVWZ2dmO2aX;uJIF{e2G7		MmnsTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbPWheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;MD6wOFfPxE1?	NIjaOIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|ME[wOVg{OCd-M{C2NFU5OzB:L3G+
Sf9	M4TMOWZ2dmO2aX;uJIF{e2G7		NXLSV2xTUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm\|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcOTCKXT3TRW0h[nliVH;wZ492dnRibXX0bI9lNCCLQ{WwQVAvODR5zszN	NVHISFh4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C2NFU5OzBpPkOwOlA2QDNyPD;hQi=>
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Sf9	M1:xZmZ2dmO2aX;uJIF{e2G7		M4DwT2lvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhcHWvYX6gSmxCTy22YXfn[YQhWFKPVEWv[pVtdCCuZX7neIghemWlb33ibY5idnRiaIXtZY4hUGm\|Nj30ZYdo\WRiTVXQOVAh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiYnnveIlvgWyjdHXkJIhqe3SxbnWgdIVxfGmmZTDhd{B{fWK\|dILheIUhcW5icILld4Vv[2Vib3[gX\|E5UF1vU1HNJIJ6KFSxcHPveY51KG2ndHjv[EwhUUN3ME2wMlQ2\|ryP	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh5MEK1PEc,Ojl6N{CyOVg9N2F-
Sf9	M{PYVmZ2dmO2aX;uJIF{e2G7		Mon2TY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbNVlJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUCuPVbPxE1?	NHzrdYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEO2OlYyPyd-M{CzOlY3OTd:L3G+
Sf9	MmnxSpVv[3Srb36gZZN{[Xl?		NGTtbmVKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHszOEifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NU4y\|ryP	MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4Nk[xO{c,OzB\|Nk[2NVc9N2F-
Sf9	NXT4PXRVTnWwY4Tpc44h[XO\|YYm=		NEDjWFRKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGZNSUdvdHHn[4VlKFCUTWS1M4Z2dGxibHXu[5RpKHKnY3;tZolv[W62IHj1cYFvKEirc{[teIFo\2WmIF3FVFUxKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIHLpc5RqdnmuYYTl[EBpcXO2b37lJJBmeHSrZHWgZZMhe3Wkc4TyZZRmKGmwIIDy[ZNmdmOnIH;mJHszOUifLWPBUUBjgSCWb4Djc5VvfCCvZYToc4QtKEmFNUC9NU45\|ryP	NXm0TVhkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOlY3OTdpPkOwN\|Y3PjF5PD;hQi=>
Sf9	NWq0OoxnTnWwY4Tpc44h[XO\|YYm=		MWHJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JIh2dWGwIF\MRWcufGGpZ3XkJHBTVVR3L3\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KGi3bXHuJGhqezZvdHHn[4VlKE2HUEWwJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IIXzbY5oKGKrb4Tpcplt[XSnZDDobZN1d26nIIDldJRq\GViYYOgd5Vje3S{YYTlJIlvKHC{ZYPlcoNmKG:oIGuyNmheNVODTTDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTB;Mj62{txO	Mn7zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB\|Nk[2NVcoRjNyM{[2OlE4RC:jPh?=
点击查看更多细胞系数据

生物活性

产品描述

EPZ015666 (GSK3235025)是一种有效的，选择性且口服生物有效的 PRMT5 抑制剂，K_i 为 5 nM，选择性比其它 PMTs 高 20,000多倍。

靶点

PRMT5 ^[1]
(Cell-free assay)

5 nM(Ki)

体外研究(In Vitro)
体外研究活性	EPZ015666(GSK3235025)表现出有效的细胞活性，阻断SmD3的对称二甲基化，并抑制MCL细胞系(Z-138，Granta-519，Maver-1，Mino，和 Jeko-1)的增殖，IC50 为96-904 nM。^[1]
细胞实验	细胞系	MCL细胞系(Z-138，Granta-519，Maver-1，Mino，和 Jeko-1)
	浓度	5 μM
	孵育时间	12天
	方法	--
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	H4R3me2s PRMT5 / H3R8me2s		28945229
	Immunofluorescence	IKKβ		29158558
	Growth inhibition assay	Cell viability		30957988

体内研究(In Vivo)
体内研究活性	EPZ015666 (200 mg/kg, p.o.)在MCL异种移植动物模型中表现出强的抗肿瘤活性。^[1]
动物实验	Animal Models	MCL (Z-138，和 Maver-1) 异种移植模型
	Dosages	200 mg/kg BID
	Administration	p.o.

参考文献
[1] Chan-Penebre E, et, al. Nat Chem Biol. 2015 Jun;11(6):432-7.

参考文献

[1] Chan-Penebre E, et, al. Nat Chem Biol. 2015 Jun;11(6):432-7.

化学信息&溶解度

分子量	383.44	分子式	C₂₀H₂₅N₅O₃
CAS号	1616391-65-1	SDF	Download EPZ015666 (GSK3235025) SDF
Smiles	C1CN(CC2=CC=CC=C21)CC(CNC(=O)C3=CC(=NC=N3)NC4COC4)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 77 mg/mL ( 200.81 mM； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 26 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

点击购买： PEG300 PEG400 Tween 80 Castor Oil CMC Na Corn Oil

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

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常见问题及建议解决方法

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

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

Histone Methyltransferase相关信号通路图

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase信号通路图

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):