EPZ015666 (GSK3235025)

目录号:S7748

仅限科研使用

EPZ015666 (GSK3235025)是一种有效的,选择性且口服生物有效的 PRMT5 抑制剂,Ki 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 购买数量
RMB 1602.26 现货
RMB 4906.16 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的EPZ015666 (GSK3235025)发表文献18篇:

质量管理及产品安全说明书

Histone Methyltransferase抑制剂选择性比较

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,Ki 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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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HCC1954 NFfJXldE\WyuII\pZYJqdGm2eTDhd5NigQ>? NXLLXYp3UUN3ME2wMlgh|ryP MlnNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NUe5PFgoRjNyOUW3PVg5RC:jPh?=
MDA-MB-453 MoTtR4VtdCC4aXHibYxqfHliYYPzZZk> NWTycGNlUUN3ME2xJO69VQ>? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl3N{m4PEc,OzB7NUe5PFg9N2F-
HCC38 NFvm[FRE\WyuII\pZYJqdGm2eTDhd5NigQ>? NVq4XVdMUUN3ME2yMlIh|ryP MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl3N{m4PEc,OzB7NUe5PFg9N2F-
MDA-MB-468 NFTWS5ZE\WyuII\pZYJqdGm2eTDhd5NigQ>? MmfRTWM2OD1{LkKg{txO NI\KNog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm1O|k5QCd-M{C5OVc6QDh:L3G+
MCF7 NIjVZXpE\WyuII\pZYJqdGm2eTDhd5NigQ>? M3fWVmlEPTB;Mj62JO69VQ>? NELZVWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm1O|k5QCd-M{C5OVc6QDh:L3G+
SKBR3 MVzD[YxtKH[rYXLpcIl1gSCjc4PhfS=> M4jjeGlEPTB;Mz65JO69VQ>? NET4fYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEm1O|k5QCd-M{C5OVc6QDh:L3G+
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Sf9 M{PsfGZ2dmO2aX;uJIF{e2G7 NUHiVVR4UW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBHVEGJLYTh[4dm\CCSUl3UOU9nfWyuIHzlcod1cCC{ZXPvcYJqdmGwdDDoeY1idiCKaYO2MZRi\2enZDDNSXA2OCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDibY91cW67bHH0[YQhcGm|dH;u[UBx\XC2aXTlJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBcOjCKXT3TRW0h[nliVH;wZ492dnRibXX0bI9lNCCLQ{WwQVEvOc7:TR?= NFHKfIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO2OlYyPyd-M{CzOlY3OTd:L3G+
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Sf9 MmG2SpVv[3Srb36gZZN{[Xl? Mn\rTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDGUGFINXSjZ3fl[EBRWk2WNT;meYxtKGynbnf0bEBz\WOxbXLpcoFvfCCqdX3hckBJcXN4LYTh[4dm\CCPRWC1NEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCkaX;0bY56dGG2ZXSgbIl{fG:wZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDbNlJJZS2VQV2gZpkhXG:yY3;1cpQhdWW2aH;kMEBKSzVyPUKuOu69VQ>? NIGzR2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO2OlYyPyd-M{CzOlY3OTd:L3G+
Assay
Methods Test Index PMID
Western blot PRMT5 / H3R8me2s H4R3me2s 30957988 28945229
Immunofluorescence IKKβ 29158558
Growth inhibition assay Cell viability 30957988
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

  • Cell lines: MCL细胞系(Z-138,Granta-519,Maver-1,Mino,和 Jeko-1)
  • Concentrations: 5 μM
  • Incubation Time: 12天
  • Method:

    --

动物实验:

[1]

  • Animal Models: MCL (Z-138,和 Maver-1) 异种移植模型
  • Dosages: 200 mg/kg BID
  • Administration: p.o.

溶解度(25°C)

体外

体内

从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+ddH2O

5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 383.44
化学式

C20H25N5O3

CAS号 1616391-65-1
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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,: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: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: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。

摩尔浓度计算器

质量 浓度 体积 分子量

技术支持

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操作手册

如果有其他问题,请给我们留言。

* 必填项

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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.

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