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EPZ015666 (GSK3235025)
EPZ015666 (GSK3235025)是一種有效的，選擇性且口服生物有效的 PRMT5 抑制劑，Ki 為 5 nM，選擇性比其它 PMTs 高 20,000多倍。
EPZ015666 (GSK3235025) Chemical Structure
CAS: 1616391-65-1
產(chǎn)品質(zhì)控
批次：
純度： >97%
97
EPZ015666 (GSK3235025)相關(guān)產(chǎn)品
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | EPZ015666 (GSK3235025)是一種有效的，選擇性且口服生物有效的 PRMT5 抑制劑，Ki 為 5 nM，選擇性比其它 PMTs 高 20,000多倍。 | ||
|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | EPZ015666(GSK3235025)表現(xiàn)出有效的細胞活性，阻斷SmD3的對稱二甲基化，并抑制MCL細胞系(Z-138，Granta-519，Maver-1，Mino，和 Jeko-1)的增殖，IC50 為96-904 nM。[1] |
|||
|---|---|---|---|---|
| 細胞實驗 | 細胞系 | MCL細胞系(Z-138，Granta-519，Maver-1，Mino，和 Jeko-1) | ||
| 濃度 | 5 μM | |||
| 孵育時間 | 12天 | |||
| 方法 | -- |
|||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | H4R3me2s PRMT5 / H3R8me2s |
|
28945229 | |
| Immunofluorescence | IKKβ |
|
29158558 | |
| Growth inhibition assay | Cell viability |
|
30957988 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | EPZ015666 (200 mg/kg, p.o.)在MCL異種移植動物模型中表現(xiàn)出強的抗腫瘤活性。[1] |
|
|---|---|---|
| 動物實驗 | Animal Models | MCL (Z-138，和 Maver-1) 異種移植模型 |
| Dosages | 200 mg/kg BID | |
| Administration | p.o. | |
化學(xué)信息&溶解度
| 分子量 | 383.44 | 分子式 | C20H25N5O3 |
| CAS號 | 1616391-65-1 | SDF | Download EPZ015666 (GSK3235025) SDF |
| Smiles | C1CN(CC2=CC=CC=C21)CC(CNC(=O)C3=CC(=NC=N3)NC4COC4)O | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 77 mg/mL ( (200.81 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 26 mg/mL (67.8 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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