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CB-5083

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产品编号 T6796Cas号 1542705-92-9
别名 CB5083, CB 5083

CB-5083 是一种有效的、选择性的、可口服的 p97 AAA ATPase 抑制剂,IC50为 11 nM。

CB-5083
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CB-5083

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纯度: 100%
产品编号 T6796 别名 CB5083, CB 5083Cas号 1542705-92-9

CB-5083 是一种有效的、选择性的、可口服的 p97 AAA ATPase 抑制剂,IC50为 11 nM。

规格价格库存数量
1 mg¥ 361现货
2 mg¥ 528现货
5 mg¥ 913现货
10 mg¥ 1,390现货
25 mg¥ 3,160现货
50 mg¥ 4,630现货
100 mg¥ 6,620现货
500 mg¥ 13,300现货
1 mL x 10 mM (in DMSO)¥ 973现货
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产品介绍

生物活性
产品描述
CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor ( IC50=11 nM).
靶点活性
p97 AAA ATPase:11 nM
体外活性
In A549 cells, CB-5083 causes significant K48 poly-ubiquitinated protein and CHOP accumulation as well as p62 reduction, and kills tumor cells with IC50 of 680 nM. [1]
体内活性
In mice bearing human HCT 116 colon tumor xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumor growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumor xenografts, CB-5083 (100 mg/kg, p.o.) also results in significant tumor growth inhibition. [1]
激酶实验
ATPase assay: Compounds are diluted in DMSO with a 3-fold 10-point serial dilution starting at 10 μM. The assay is done in a 384-well plate with each row as a single dilution series with duplicate of each compound concentration point. In 5 μL total volume, 20 nM p97 hexameric enzyme and 20 μM ATP are added to start the reaction. The plate is sealed and incubated at 37 °C for 15 min after mixing thoroughly in an orbital shaker. Compound dilution, ATP and enzymes addition are conducted with automated liquid handling using the Freedom Evo. ADP Glo reagents 1 and 2 are added according to the manufacturer's protocol. The luminescence is measured by Envision plate reader as the end point of the reaction. The IC50 of each compound is derived by fitting the luminescence values to a four-parameter sigmoidal curve.
细胞实验
A549 and other tumor cell lines are cultured according to ATCC guidelines. Cells are cultured in black or white, clear-bottomed, tissue culture-treated 384-well plates. Cells are treated with 10-point dose titration of the compound in well duplicates. After a 72 h treatment, CellTiter-Glo is added to the white plates to measure cell viability. Luminescence values are fit to a four-parameter sigmoidal curve to determine IC50 concentrations.(Only for Reference)
别名CB5083, CB 5083
化学信息
分子量413.47
分子式C24H23N5O2
CAS No.1542705-92-9
SmilesCc1cc2c(cccc2n1-c1nc2CCOCc2c(NCc2ccccc2)n1)C(N)=O
密度1.37 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: 11 mg/mL (26.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 60 mg/mL (145.11 mM)
溶液配制表
1mg5mg10mg50mg
1 mM2.4186 mL12.0928 mL24.1856 mL120.9278 mL
5 mM0.4837 mL2.4186 mL4.8371 mL24.1856 mL
10 mM0.2419 mL1.2093 mL2.4186 mL12.0928 mL
20 mM0.1209 mL0.6046 mL1.2093 mL6.0464 mL
1mg5mg10mg50mg
50 mM0.0484 mL0.2419 mL0.4837 mL2.4186 mL
100 mM0.0242 mL0.1209 mL0.2419 mL1.2093 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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