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Dacinostat

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产品编号 T2454Cas号 404951-53-7
别名 达西司特, NVP-LAQ824, LAQ824

Dacinostat (NVP-LAQ824) 是一种新型 HDAC 抑制剂,IC50 为 32 nM,是 p21 启动子的激活剂。它也可抑制HDAC1的活性,IC50值为 9 nM,主要用于癌症研究。

Dacinostat

Dacinostat

Rating icon 很棒
纯度: 95.28%
产品编号 T2454 别名 达西司特, NVP-LAQ824, LAQ824Cas号 404951-53-7

Dacinostat (NVP-LAQ824) 是一种新型 HDAC 抑制剂,IC50 为 32 nM,是 p21 启动子的激活剂。它也可抑制HDAC1的活性,IC50值为 9 nM,主要用于癌症研究。

规格价格库存数量
1 mg
¥ 477
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2 mg
¥ 691
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5 mg
¥ 1,110
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10 mg
¥ 1,730
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25 mg
¥ 2,930
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50 mg
¥ 4,330
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100 mg
¥ 6,180
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500 mg
¥ 12,600
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1 mL x 10 mM (in DMSO)
¥ 1,330
现货
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产品介绍

生物活性
产品描述
LAQ824 (Dacinostat (NVP-LAQ824)) is a novel HDAC inhibitor with IC50 of 32 nM and is an activator of the p21 promoter.
靶点活性
HDAC:32 nM
体外活性
100 mg/kg LAQ824剂量依赖性抑制携带HCT116和人结肠癌移植瘤的裸鼠肿瘤生长,且无细胞毒性.
体内活性
LAQ824诱导A549细胞中p21蛋白的剂量依赖性增加和Rb肿瘤抑制因子的低磷酸化状态的增加。LAQ824在IL-10基因启动子水平诱导染色质改变,导致增强的转录抑制因子HDAC11和PU.1的募集并抑制BALB/c鼠巨噬细胞中IL-10的产生。此外,LAQ824通过激活p21启动子,也激活编码p21细胞周期抑制剂的基因表达,最大启动子活性AC50为50%时,浓度为0.30 μM。 LAQ824抑制H1299(一种非小细胞肺癌细胞系)和HCT116(一种结肠癌细胞系)的细胞生长,IC50分别为0.15 μM和0.01 μM,LAQ824的抗增殖作用对肿瘤细胞系具有选择性,同时仅在正常成纤维细胞中诱导生长停滞。
激酶实验
In Vitro Histone Deacetylase Assay: HDAC enzymes are partially purified from H1299 cell lysate by ion exchange chromatography using the Q Sepharose Fast Flow column. Enzyme complexes are collected from 500 mg of total cell lysate by immunoprecipitation with cdk2 polyclonal antibody or cdk1/cdc2 monoclonal antibody. Immunoprecipitates are resuspended in kinase buffer (50 mM Hepes, pH 8, 10 mM MgCl2, 2.5 mM EDTA, 1 mM dithiothreitol, 20 mM ATP, 10 mM β-glycerophosphate, 0.1 mM NaVO4, 1 mM sodium fluoride, 50 mM ATP, 10 μCi of [γ-32P]ATP) along with 1 μg of pRb recombinant protein substrate (cdk2) or 10 mL of H1 histone mixture containing 20 μg of substrate (cdc2). Phosphorylated Rb and H1 histone are resolved by electrophoresis and quantitated using a PhosphorImager.
细胞实验
Cell proliferation is measured using an adaptation of published procedures (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium assay). The cells are seeded in 12-well dishes and cultured in RPMI 1640 containing 10% FBS. The cells are cultured in the presence of various concentrations of TSA (up to 1,000 ng/mL). To examine the growth inhibition by TSA, viable cell numbers are determined by trypan blue dye exclusion, counted in a Nesbauer-type hemocytometer for 0 hour, 24 hours, and 48 hours. The same amount of ethanol is added to the RPMI 1640 medium as the control experiment. All experiments are performed in duplicate and repeated 3 times The average background value (treatment with medium alone) is subtracted from each experimental well; triplicate values are averaged for each compound dilution. The following formulas are used to calculate the percentage of growth: If XT0, %Growth=(X-T0)/(GC-T0)*100. where T0 is the average value of T0 ? background, GC is the average value of untreated cells (in triplicate) ? background, and X is the average value of compound-treated cells (in triplicate)-background. The "% Growth" is plotted against compound concentration and used to calculate the IC50 using the linear regression techniques between data points to predict the concentration of compounds at 50% inhibition.(Only for Reference)
别名达西司特, NVP-LAQ824, LAQ824
化学信息
分子量379.45
分子式C22H25N3O3
CAS No.404951-53-7
SmilesOCCN(CCc1c[nH]c2ccccc12)Cc1ccc(\C=C\C(=O)NO)cc1
密度1.29g/cm3
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: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 40 mg/mL (105.42 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.6354 mL13.1770 mL26.3539 mL131.7697 mL
5 mM0.5271 mL2.6354 mL5.2708 mL26.3539 mL
10 mM0.2635 mL1.3177 mL2.6354 mL13.1770 mL
20 mM0.1318 mL0.6588 mL1.3177 mL6.5885 mL
50 mM0.0527 mL0.2635 mL0.5271 mL2.6354 mL
100 mM0.0264 mL0.1318 mL0.2635 mL1.3177 mL

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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

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