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Decernotinib

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产品编号 T2636Cas号 944842-54-0
别名 VX-509, VRT-831509

Decernotinib (VRT-831509) 是一种可口服的JAK3抑制剂,对JAK3、JAK1、JAK2 和 TYK2 的Ki 值分别为 2.5、11、13 和 11 nM。

Decernotinib
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Decernotinib

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纯度: 100%
产品编号 T2636 别名 VX-509, VRT-831509Cas号 944842-54-0

Decernotinib (VRT-831509) 是一种可口服的JAK3抑制剂,对JAK3、JAK1、JAK2 和 TYK2 的Ki 值分别为 2.5、11、13 和 11 nM。

规格价格库存数量
1 mg¥ 298现货
2 mg¥ 428现货
5 mg¥ 690现货
10 mg¥ 1,080现货
25 mg¥ 2,180现货
50 mg¥ 3,320现货
100 mg¥ 4,920现货
500 mg¥ 9,870期货
1 mL x 10 mM (in DMSO)¥ 776现货
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产品介绍

生物活性
产品描述
Decernotinib (VRT-831509)(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
靶点活性
JAK3:2.5 nM(Ki)
体外活性
在HT-2细胞中,Decernotinib抑制了IL-2刺激的HT-2 STAT-5磷酸化、人类T细胞爆发增殖和CD40L/IL-4诱导的B细胞增殖。[1]
体内活性
在大鼠胶原诱导性关节炎模型中,Decernotinib(50 mg/kg, 口服) 显示出剂量依赖性地减少踝部肿胀和爪重,并改善爪部组织病理学评分。在小鼠草酰胺诱导的迟发型超敏反应模型中,Decernotinib(50 mg/kg, 口服) 显著抑制耳部水肿。[1] 在大鼠HvG模型中,Decernotinib(50 mg/kg, 口服) 以剂量依赖的方式抑制腘淋巴结 (PLN) 增生。[2]
激酶实验
Kinase Activity Assays: The effect of VX-509 on JAK3 activity is assessed by measuring the residual kinase activity of the recombinantly expressed JAK3 kinase domain using a radiometric assay. The final concentrations of the components in the assay are as follows: 100 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM dithiothreitol (DTT), 0.01% BSA, 0.25 nM JAK3, 0.25 mg/ml polyE4Y, and 5 μM 33P-γ-ATP (200 μCi/μMol). A 10 mM stock solution of VX-509 is prepared in DMSO, from which additional dilutions are prepared. A substrate mixture (100 mM HEPES, 10 mM MgCl2, 0.5 mg/ml polyE4Y, and 10 μM 33P-γ-ATP) is added and mixed with VX-509 stock solution. The reaction is initiated by the addition of an enzyme mixture [100 mM HEPES (pH 7.5), 10 mM MgCl2, 2 mM DTT, 0.02% BSA, 0.5 nM JAK3]. After 15 minutes, the reaction was quenched with 20% trichloroacetic acid (TCA). The quenched reaction was transferred to the GF/B filter plates and washed three times with 5% TCA. Following the addition of Ultimate Gold scintillant (50 μl), the samples were counted in a Packard TopCount gamma counter (PerkinElmer). In this procedure, the radioactivity trapped is a measure of the residual JAK3 kinase activity. From the activity versus concentration of VX-509 titration curve, the Ki value was determined by fitting the data to an equation for competitive tight binding inhibition kinetics using Prism software.
细胞实验
Frozen purified human B cells atr thawed, washed, and resuspended in complete medium. Cells are plated onto a 96-well plate at a density of 2 × 105 cells/well. VX-509 is added, and plates are incubated for 30 minutes at 37°C, followed by stimulation with a combination of 10 ng/ml IL-4 and 1 μg/ml CD40L. DMSO alone is added to the top two rows, one of which is stimulated with IL-4 or CD40L (negative control) and the other of which served as a proliferation control. The plates are incubated at 37°C for 6 days. On day 6, cells are pulsed with [3H]thymidine for 7 hours and harvested onto filters for radioactive determination using a PerkinElmer-Wallace beta counter (1205 Betaplate Beta Liquid Scintillation Counter). Data are analyzed with Softmax pro software to generate an IC50 value.(Only for Reference)
别名VX-509, VRT-831509
化学信息
分子量392.38
分子式C18H19F3N6O
CAS No.944842-54-0
SmilesCC[C@@](C)(Nc1ccnc(n1)-c1c[nH]c2ncccc12)C(=O)NCC(F)(F)F
密度1.363 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
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 72 mg/mL (183.5 mM)
Ethanol: 16 mg/mL (40.8 mM)
溶液配制表
1mg5mg10mg50mg
1 mM2.5485 mL12.7427 mL25.4855 mL127.4275 mL
5 mM0.5097 mL2.5485 mL5.0971 mL25.4855 mL
10 mM0.2549 mL1.2743 mL2.5485 mL12.7427 mL
20 mM0.1274 mL0.6371 mL1.2743 mL6.3714 mL
1mg5mg10mg50mg
50 mM0.0510 mL0.2549 mL0.5097 mL2.5485 mL
100 mM0.0255 mL0.1274 mL0.2549 mL1.2743 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
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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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