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网站主页 化工产品目录 生物化工 抑制剂 细胞周期(Cell Cycle) CDK 抑制剂 4-[(2,6-二氯苄基)氨基]-N-4-哌啶1H-吡唑-3-羧胺 化合物 AT7519
  • 化合物 AT7519|T6205|TargetMol

化合物 AT7519|T6205|TargetMol

AT7519
844442-38-2
￥285 1mg 起订
￥662 5mg 起订
￥1120 10mg 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 AT7519
英文名称：
AT7519
CAS号：
844442-38-2
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：
99.65%
产品类别：
抑制剂
货号：
T6205

Product Introduction

Bioactivity

名称AT7519
描述AT7519 is a CDK1/2/4/6/9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.
细胞实验Cells are incubated with different concentrations of AT7519 for 24 or 48 hours at 37 °C. Cell viability is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrasodium bromide (MTT) dye absorbance. DNA synthesis is measured by tritiated thymidine uptake (3H-TdR). Apoptosis is assessed by using Annexin V/PI staining. The percentage of cells undergoing apoptosis is defined as the sum of early apoptosis (Annexin V-positive cells) and late apoptosis (Annexin V-positive and PI-positive cells(Only for Reference)
激酶实验In vitro Kinase Assays: Kinase assays for CDK1, CDK2 and GSK3-β are all carried out in a radiometric filter binding format. Assays for CDK5 are in DELFIA format and for CDKs 4 and 6 in ELISA format. For CDKs 1 and 2, the relevant CDK and 0.12 μg/mL Histone H1 are incubated in 20 mM MOPS, pH 7.2, 25 mM β-glycerophosphate, 5 mM EDTA, 15 mM MgCl2, 1 mM sodium orthovanadate, 1 mM DTT, 0.1 mg/mL BSA, 45 μM ATP (0.78 Ci/mmol) and different concentrations of AT7519 for 2 or 4 hours respectively. For GSK3-β, the relevant enzyme and 5 μM glycogen synthase peptide 2 along with 10 mM MOPS pH 7.0, 0.1 mg/mL BSA, 0.001% Brij-35, 0.5% glycerol, 0.2 mM EDTA, 10 mM MgCl2, 0.01% β-mercaptoethanol, 15 μM ATP (2.31 Ci/mmol) and different concentrations of AT7519 are incubated for 3 hours. Assay reactions are stopped by adding an excess of orthophosphoric acid and filtered using Millipore MAPH filter plates. The plates are then washed, scintillant added and radioactivity measured by scintillation counting on a Packard TopCount. For CDK5, CDK5/p35 and 1 μM of a biotinylated Histone H1 peptide (Biotin-PKTPKKAKKL) are incubated in 25 mM Tris-HCl, pH 7.5, 2.5 mM MgCl2, 0.025% Brij-35, 0.1 mg/mL BSA, 1 mM DTT, 15 μM ATP and different concentrations of AT7519 for 30 minutes. Assay reactions are stopped using EDTA, transferred to Neutravidin-coated plates and phosphorylated peptide quantified by means of a rabbit phospho-cdk1 substrate polyclonal antibody and DELFIA europium-labelled anti-rabbit IgG secondary antibody using time-resolved fluorescence at λex=335 nM, λem=620 nM. For CDK 4 and 6 assays, plates are coated with GST- pRb769-921 and blocked with Superblock. CDK4 or 6 is incubated with 15 mM MgCl2, 50 mM HEPES, pH 7.4, 1 mM DTT, 1 mM EGTA, pH 8.0, 0.02% Triton X-100, 2.5% DMSO and different concentrations of AT7519; the reaction is initiated by addition of ATP. After 30 minutes, reactions are stopped by the addition of 0.5 M EDTA pH 8.0.Plates are then washed and incubated for one hour with the primary antibody (anti- p-Rb Serine 780) diluted in Superblock followed by secondary antibody (alkaline phosphatase linked anti-rabbit) for a further hour. Plates are developed using the Attophos system and fluorescence read on a Spectramax Gemini plate reader at excitation 450 nm and emission 580 nm. In all cases, IC50 values are calculated from replicate curves, using GraphPad Prism software.
体外活性AT7519是一种与ATP竞争的CDK抑制剂，对CDK1的Ki值为38 nM，除了对GSK3β（IC50 = 89 nM）有活性外，对所有非CDK激酶均无活性。AT7519在多种人类肿瘤细胞系中显示出强大的抗增殖活性，IC50值从MCF-7的40 nM到SW620的940 nM不等，这与CDK1和CDK2的抑制作用一致。[1] AT7519在48小时内对多发性骨髓瘤（MM）细胞系产生剂量依赖性的细胞毒性，IC50值从0.5到2 μM不等，对MM.1S（0.5 μM）和U266（0.5 μM）细胞系最为敏感，而对MM.1R（>2 μM）最为耐药。它不对外周血单核细胞（PBMNC）产生细胞毒性。AT7519部分克服了IL6和IGF-1提供的增殖优势以及骨髓基质细胞（BMSCs）的保护效果。AT7519快速促进RNA pol II CTD在丝氨酸2和丝氨酸5位点的去磷酸化，并导致转录抑制，这部分地促成了AT7519对MM细胞诱导的细胞毒性。通过下调GSK-3β的磷酸化，AT7519激活GSK-3β，这也促成了AT7519诱导的凋亡，这一过程与转录抑制无关。[2]
体内活性每日两次给药AT7519（9.1 mg/kg）能够促使HCT116与HT29结肠癌异种移植模型中的早期和晚期s.c.肿瘤退化。[1] AT7519治疗（15 mg/kg）抑制了人类MM异种移植小鼠模型中的肿瘤生长，并与caspase 3活化增加相关，延长了小鼠的中位总生存时间。[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)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 16.67 mg/mL (43.6 mM)
关键字AT 7519 | inhibit | Apoptosis | CDK | AT-7519 | Inhibitor | AT7519M | AT7519 | Cyclin dependent kinase
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相关库神经保护化合物库 | 抑制剂库 | 抗癌活性化合物库 | 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 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库
AT7519|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

化合物 AT7519相关厂家报价

  • AT7519
  • AT7519
  • 南京百鑫德诺生物科技有限公司
  • 2024-09-26
  • 询价
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