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(+)-JQ-1

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产品编号 T2110Cas号 1268524-70-4
别名 JQ1

(+)-JQ-1 (JQ1) 是一种 BET 溴结构域抑制剂,抑制 BRD4(1/2) (IC50=77/33 nM),具有特异性和可逆性。(+)-JQ-1 可以诱导细胞自噬,抑制细胞增殖。

(+)-JQ-1

(+)-JQ-1

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纯度: 99.97%
产品编号 T2110 别名 JQ1Cas号 1268524-70-4

(+)-JQ-1 (JQ1) 是一种 BET 溴结构域抑制剂,抑制 BRD4(1/2) (IC50=77/33 nM),具有特异性和可逆性。(+)-JQ-1 可以诱导细胞自噬,抑制细胞增殖。

规格价格库存数量
1 mg¥ 253现货
2 mg¥ 357现货
5 mg¥ 588现货
10 mg¥ 863现货
25 mg¥ 1,360现货
50 mg¥ 1,860现货
100 mg¥ 2,950现货
200 mg¥ 3,580现货
500 mg¥ 4,850现货
1 mL x 10 mM (in DMSO)¥ 657现货
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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
(+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1/2) (IC50=77/33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.
靶点活性
BRD4(1):77 nM(cell free), BRD4(2):33 nM(cell free)
体外活性
方法:BRD4-NUT 依赖性细胞系 NMC 797 用 (+)-JQ-1 (250 nM) 处理 48 h,使用 Flow Cytometry 检测细胞周期情况。
结果:(+)-JQ-1 诱导 G1 细胞周期停滞。[1]
方法:人多发性骨髓瘤细胞 KMS11、LR5、OPM1 和 INA-6 用 (+)-JQ-1 (500 nM) 处理 24 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:(+)-JQ-1 抑制扩增的 Myc 依赖性 MM 细胞系中对 c-Myc 蛋白表达。[2]
体内活性
方法:为检测体内抗肿瘤活性,将 (+)-JQ-1 (50 mg/kg,5% DMSO in 5% dextrose) 腹腔注射给携带 NMC 异种移植瘤的 NCr nude 小鼠,每天一次,持续十八天。
结果:(+)-JQ-1 治疗后,观察到明显的肿瘤消退和总生存率的提高。[1]
方法:为检测体内抗肿瘤活性,将 (+)-JQ-1 (50 mg/kg) 腹腔注射给携带人胃癌肿瘤 HGC27 的 nude 小鼠,每天一次,持续两周。
结果:(+)-JQ-1 阻止胃癌肿瘤生长并抑制肿瘤转移。[3]
细胞实验
Cells were plated at 5,000 cells per well of 96-well plates containing titrations of the compounds as indicated. After incubation, the cells were washed once with PBS and resuspended in 175 μL of ice-cold 70% ethanol and fixed for a minimum of 16 h at 4 °C. The cells were pelleted and washed 1× with PBS and stained for 30 min at room temperature (RT) with 120 μL of staining solution [propidium iodide (20 μg/mL), RNase A (25 μg/mL), 0.1% Triton X-100 in PBS]. Cell number and cell cycle data were obtained by using a flow cytometer using the Express Pro module. DNA content histograms were analyzed by using ModFit LT 3.2 Software. To calculate the number of viable cells in each well, the concentration of events measured using the Guava was multiplied by the volume of cells in the well, then by the fraction of cells in G1+S+G2/M. GI50 values for each cell line were calculated as the concentration of compound giving a 50% reduction in cell number relative to the DMSO control [4].
动物实验
(Harlan) inoculated s.c. with 3 × 10^6 cells per mouse resuspended in 10% Matrigel. Two weeks later (average tumor volume 150 mm3), mice were assigned into two groups: 15 mice were treated with vehicle control (5:95 DMSO:10% 2-Hydroxypropyl-β-cyclodextrin), and 15 mice were treated with 30 mg/kg (+)-JQ1 by i.p. injection twice a day for 28 d. Body weight and tumor volume were measured daily. Tumor volume was calculated from caliper measurements by using the following formula: W × H × L × 0.52. Mice were killed when tumor volume reached 2,000 mm3, when body weight decreased >20% of initial weight, or when the mice were in poor health as established in the IACUC protocol. Survival was plotted and analyzed in GraphPad Prism software, and statistical significance was calculated by using log-rank (Mantel-Cox) and Gehan–Breslow–Wilcoxon tests. MV4-11 xenografts were established in nude mice injected with 10 × 10^6 cells per mouse. JQ1 was dosed i.p. and formulated as described above. Mice were divided into 4 groups of 10 animals: vehicle control once a day; 50 mg/kg (+)-JQ1 once a day; 30 mg/kg (+)-JQ1 twice a day; and cytarabine 100 mg/kg daily (5 d on, 2 d off). Treatment of mice with cytarabine at 100 mg/kg resulted in significant weight loss at day 8 and, therefore, the dose needed to be decreased to 75 mg/kg [4].
别名JQ1
化学信息
分子量456.99
分子式C23H25ClN4O2S
CAS No.1268524-70-4
SmilesCC=1C2=C(N3C([C@H](CC(OC(C)(C)C)=O)N=C2C4=CC=C(Cl)C=C4)=NN=C3C)SC1C
密度1.33 g/cm3
储存&溶解度
存储keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.94 mg/mL (6.43 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
Ethanol: 45.7 mg/mL (100 mM)
DMSO: 45 mg/mL (98.47 mM), Sonication is recommended.
溶液配制表
1mg5mg10mg50mg
1 mM2.1882 mL10.9412 mL21.8823 mL109.4116 mL
5 mM0.4376 mL2.1882 mL4.3765 mL21.8823 mL
1mg5mg10mg50mg
10 mM0.2188 mL1.0941 mL2.1882 mL10.9412 mL
20 mM0.1094 mL0.5471 mL1.0941 mL5.4706 mL
50 mM0.0438 mL0.2188 mL0.4376 mL2.1882 mL
1mg5mg10mg50mg
100 mM0.0219 mL0.1094 mL0.2188 mL1.0941 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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