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网站主页 化工产品目录 生物化工 生化试剂 激动剂抑制剂 迪西替尼 化合物 Decernotinib
  • 化合物 Decernotinib|T2636|TargetMol

化合物 Decernotinib|T2636|TargetMol

Decernotinib
944842-54-0
￥298 1mg 起订
￥428 2mg 起订
￥690 5mg 起订
上海 更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐
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邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 Decernotinib
英文名称：
Decernotinib
CAS号：
944842-54-0
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.45%
产品类别：
抑制剂
货号：
T2636

Product Introduction

Bioactivity

名称Decernotinib
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.
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)
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.
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]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 72 mg/mL (183.5 mM)
Ethanol : 16 mg/mL (40.8 mM)
关键字VX509 | Decernotinib | VRT831509 | inhibit | JAK | Janus kinase | VX 509 | VRT 831509 | Inhibitor
相关产品JAK-IN-10 | Tofacitinib Citrate | Deucravacitinib | Gefitinib | Ruxolitinib | CEP-33779 | Baricitinib | Fedratinib | GSK 3 Inhibitor IX | Ruxolitinib phosphate | Ibrutinib | Delgocitinib
相关库抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 激酶抑制剂库 | 抗衰老化合物库 | 抗肥胖化合物库 | 药物功能重定位化合物库 | 酪氨酸激酶分子库 | 抗癌临床化合物库 | 抗癌药物库
VX-509|||VRT-831509|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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