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网站主页 化工产品目录 生物化工 抑制剂 酪氨酸蛋白激酶/信号转导子和转录活化子抑制剂(JAK/STAT) JAK 抑制剂 AT9283 化合物 AT9283
  • 化合物 AT9283|T3068|TargetMol

化合物 AT9283|T3068|TargetMol

AT9283
896466-04-9
372 1mg 起订
569 2mg 起订
745 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 AT9283
英文名称:
AT9283
CAS号:
896466-04-9
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:
99.98%
产品类别:
抑制剂
货号:
T3068

Product Introduction

Bioactivity

名称AT9283
描述AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
细胞实验HCT 116 cells are cultured in DMEM + 10% FBS + GLUTAMAX I. Black 96-well flat-bottomed (clear) tissue culture treated plates are seeded in 200 μL of medium and incubated for approximately 16 hours at 37°C in a humidified atmosphere of 5% CO2 in air. Cells are treated with test compound at nine different concentrations (spanning 1 nM to 10 μM, plus DMSO vehicle control) and then incubated for 72 hours. Polyploidy morphological observations of the cells are then noted. The concentration of AT9283 required to produce a distinct polyploid phenotype is reported. Cells are seeded at a concentration of 75−100 cells/mL relevant culture media onto 6- or 24-well tissue culture plates and allowed to recover for 16 hours. Test compound (11 concentrations spanning 0.1 nM to 10 μM) or vehicle control (DMSO) is added to duplicate wells to give a final DMSO concentration of 0.1%. Following compound addition, colonies are allowed to grow between 10 and 14 days for optimum discrete colony counting. Colonies are fixed in 2 mL of Carnoys fixative (25% acetic acid, 75% MeOH) and stained in 2 mL of 0.4% w/v crystal violet. The numbers of colonies in each well is counted. IC50 values are calculated by sigmoidal dose-response (variable slope) IC50 curves using Prism Graphpad software. (Only for Reference)
激酶实验Aurora A and Aurora B Kinase Assays: Assays for Aurora A and B are performed in a DELFIA format. Aurora A enzyme is incubated with AT9283 and 3 μM cross-tide substrate (biotin-CGPKGPGRRGRRRTSSFAEG) in 10 mM MOPS, pH 7, 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, and 2.5% DMSO. Aurora B enzyme is incubated with AT9283, 3 μM of the above substrate in 25 mM Tris, pH 8.5, 5 mM MgCl2, 0.1 mg/mL BSA, 0.025% Tween-20, 1 mM DTT, 15 μM ATP, and 2.5% DMSO. Reactions are allowed to proceed for 60 minutes and 45-90 minutes for Aurora A and Aurora B, respectively, before quenching with EDTA. The reaction mixtures are then transferred to a neutravidin-coated plate, and phosphorylated peptide is quantified by means of a phospho-specific antibody and a europium labeled secondary antibody using time-resolved fluorescence (excitation, 337 nm; emission, 620 nm). IC50 values for the control compounds are 92 nM (Aurora A assay) and 17 nM (Aurora B).
体外活性携带HCT116人结肠癌移植瘤的小鼠中,AT9283(15-20 mg/kg)能够抑制肿瘤生长.
体内活性在HCT116细胞中(IC50=30 nM),AT9283抑制Aurora B 激酶活性,产生多倍体表现型,同时抑制集落形成。AT9283还能够显著抑制多种激酶,例如包括Aurora A(IC50=3 nM), Aurora B( IC50=3 nM), JAK3(IC50=1.1 nM), JAK2(IC50=1.2 nM )和 Abl(IC50=4 nM)。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 71 mg/mL (186.1 mM)
Ethanol : 22 mg/mL (57.7 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字AT-9283 | Apoptosis | Cluster of differentiation antigen 135 | Janus kinase | Autophagy | inhibit | Bcr-Abl | Fms like tyrosine kinase 3 | FLT3 | J504568 | AT9283 | Aurora Kinase | AT 9283 | Inhibitor | J 504568 | JAK | CD135
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J-504568|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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