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EPZ004777

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产品编号 T3081Cas号 1338466-77-5

EPZ004777 是一种选择性 DOT1L 抑制剂,IC50为 0.4 nM。

EPZ004777

EPZ004777

Rating icon 很棒
纯度: 99.32%
产品编号 T3081Cas号 1338466-77-5

EPZ004777 是一种选择性 DOT1L 抑制剂,IC50为 0.4 nM。

规格价格库存数量
1 mg¥ 348现货
5 mg¥ 828现货
10 mg¥ 1,330现货
25 mg¥ 2,660现货
50 mg¥ 4,160现货
100 mg¥ 5,920现货
1 mL x 10 mM (in DMSO)¥ 986现货
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"EPZ004777"的相关化合物库

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纯度:99.32%
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TargetMol 的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。

产品介绍

生物活性
产品描述
EPZ004777 is a potent and selective DOT1L inhibitor with an IC50 of 0.4 nM.
靶点活性
DOT1L:0.4 nM
体外活性
EPZ004777对MLL白血病小鼠移植瘤模型产生有效的抗肿瘤功效,且平均寿命显著延长.
体内活性
在抑制DOT1L后,EPZ004777选择性抑制MLL重排细胞系和MLL-AF9转化的鼠造血细胞的增殖。EPZ004777也诱导MLL基因重排的细胞系分化和凋亡。 EPZ004777选择性抑制细胞H3K79甲基化,并抑制关键MLL融合靶基因的表达。EPZ004777选择性抑制MLL-AF10和CALM-AF10转化的小鼠造血细胞增殖。EPZ004777 抑制DOT1L后,导致MLL-AF6转化的小鼠造血细胞的增殖明显降低,MLL-AF6靶基因表达降低和细胞周期停滞。
激酶实验
Determination of Inhibitor IC50 Values: EPZ004777 is serially diluted 3-fold in DMSO for a total of ten concentrations, beginning at 1 mM. A 1 μL aliquot of each inhibitor dilution is plated in a 384-well microtiter plate. The 100% inhibition control consisted of 2.5 mM ?nal concentration of the product inhibitor S-adenosyl-L-homocysteine, (SAH). Compound is incubated for 30 min with 40 ml per well of 0.25 nM DOT1L(1-416) in assay buffer (20 mM TRIS [pH 8.0] 10 mM NaCl, 0.002% Tween 20, 0.005% Bovine Skin Gelatin, 100 mM KCl, and 0.5 mM DTT). 10 ml per well of substrate mix comprising assay buffer with 200 nM 3H-SAM (American Radiolabeled Chemicals: 80 Ci/mmol), 600 nM unlabeled SAM, and 20 nM nucleosomes are added to initiate the reaction (both substrates are present in the ?nal reaction mixture at their respective KM values). Reactions are incubated for 120 min and quenched with 10 ml per well of 800 mM SAM. Incorporation of radioactivity into nucleosome substrate is measured in a ?ashplate. IC50 values for enzymes in the histone methyltransferase panel are determined under similar balanced assay conditions with both SAM and protein/peptide substrate present at concentrations equal to their respective KM values.
细胞实验
For assessment of cell proliferation and viability in human cell lines, exponentially growing cells are plated, in triplicate, in 96-well plates in a ?nal volume of 150 ml. Cells are incubated in the presence of 3 μM (proliferation curve), or increasing concentrations (IC50 determination) of EPZ004777 up to 50 μM. Viable cell number is determined every 3–4 days for up to 18 days using the Guava Viacount assay and analyzed on a Guava EasyCyte Plus instrument according to the manufacturer’s protocol. On days of cell counts, growth media and EPZ004777 are replaced and cells split back to a density of 5×104 cells/well. Total cell number is expressed as split-adjusted viable cells per well. For each cell line, IC50 values are determined from concentration-dependence curves at each time point using Graphpad Prism software. Experiments to determine IC50 values continues until IC50 values stabilized (day 18 for THP-1 cells, day 14 for all other cell lines). For assessment of the effect of EPZ004777 treatment on transformed murine hematopoietic progenitors, cells from two independent transductions for each virus are plated in 24-well plates at a density of 0.5–1×105 cell/well in 1 ml media in 24-well plates and exposed to increasing concentrations of EPZ004777 up to 30 mM. Cells are counted and replated at equal cell numbers in fresh media with fresh compound every 3–4 days. For MTT assays, cells from serial replatings are harvested on day 10 and plated, in triplicate at 2×104 cells/well in 100 ml media with the appropriate concentration of EPZ004777. Cells are incubated for 2.5 days, the exposed to 10 ml MTT reagent for 3 hr, and lysed over night in 100 ml MTT- solubilization buffer (both from Cell Proliferation Kit I [MTT]). (Only for Reference)
化学信息
分子量539.67
分子式C28H41N7O4
CAS No.1338466-77-5
SmilesOC=O.CC(C)N(CCCNC(=O)Nc1ccc(cc1)C(C)(C)C)C[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1ccc2c(N)ncnc12
密度1.33 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 54 mg/mL (100 mM)
DMSO: 54 mg/mL (100 mM)
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.8530 mL9.2649 mL18.5298 mL92.6492 mL
5 mM0.3706 mL1.8530 mL3.7060 mL18.5298 mL
10 mM0.1853 mL0.9265 mL1.8530 mL9.2649 mL
20 mM0.0926 mL0.4632 mL0.9265 mL4.6325 mL
50 mM0.0371 mL0.1853 mL0.3706 mL1.8530 mL
100 mM0.0185 mL0.0926 mL0.1853 mL0.9265 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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