EPZ015666 (GSK3235025)
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
产品质控
批次：
纯度： >97%
97
EPZ015666 (GSK3235025)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| MDA-MB-468 | Function assay | 48 h | inhibits PRMT5 activity | 30957988 | |
| MDA-MB-453 | Cell viability assay | IC50=1 μM | 30957988 | ||
| HCC1954 | Cell viability assay | IC50=0.8 μM | 30957988 | ||
| HCC38 | Cell viability assay | IC50=2.2 μM | 30957988 | ||
| MDA-MB-468 | Cell viability assay | IC50=2.2 μM | 30957988 | ||
| MCF7 | Cell viability assay | IC50=2.6 μM | 30957988 | ||
| SKBR3 | Cell viability assay | IC50=3.9 μM | 30957988 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [3H]-SAM by Topcount method, IC50=0.022μM | 29628326 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [4H]-SAM by Topcount method, IC50=0.022μM | 29628326 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [5H]-SAM by Topcount method, IC50=0.022μM | 30366617 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [6H]-SAM by Topcount method, IC50=0.022μM | 30366617 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [7H]-SAM by Topcount method, IC50=0.047μM | 30366617 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [8H]-SAM by Topcount method, IC50=0.047μM | 30366617 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [9H]-SAM by Topcount method, IC50=0.047μM | 30605830 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [10H]-SAM by Topcount method, IC50=0.047μM | 30605830 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [11H]-SAM by Topcount method, IC50=0.047μM | 30605830 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [12H]-SAM by Topcount method, IC50=0.047μM | 30605830 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [13H]-SAM by Topcount method, IC50=0.096μM | 29870258 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [14H]-SAM by Topcount method, GI50=0.106μM | 30605830 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [15H]-SAM by Topcount method, GI50=0.106μM | 30605830 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [16H]-SAM by Topcount method, GI50=0.212μM | 30605830 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [17H]-SAM by Topcount method, GI50=0.212μM | 30605830 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [18H]-SAM by Topcount method, IC50=0.45μM | 29870258 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [19H]-SAM by Topcount method, IC50=0.96μM | 30366617 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [20H]-SAM by Topcount method, IC50=1.1μM | 30366617 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [21H]-SAM by Topcount method, IC50=1.8μM | 30366617 | ||
| Sf9 | Function assay | Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 insect cells using biotinylated histone peptide as substrate in presence of [22H]-SAM by Topcount method, IC50=2.6μM | 30366617 | ||
| 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，Ki 为 5 nM，选择性比其它 PMTs 高 20,000多倍。 | ||
|---|---|---|---|
| 靶点 |
|
| 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] |
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|---|---|---|---|---|
| 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 | -- |
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| 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. | |
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) | |||
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体外溶解度 |
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 (67.8 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 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 | |||||
实验计算
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
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。
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