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AT9283

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产品编号 T3068Cas号 896466-04-9
别名 J-504568

AT9283 (J-504568) 是一种多靶点激酶抑制剂,抑制多种实体瘤在体内外的生长和存活,有效抑制Aurora A/B,JAK2/3,Abl (T315I),和Flt3,IC50值范围为 1-30 nM。

AT9283

AT9283

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纯度: 99.98%
产品编号 T3068 别名 J-504568Cas号 896466-04-9

AT9283 (J-504568) 是一种多靶点激酶抑制剂,抑制多种实体瘤在体内外的生长和存活,有效抑制Aurora A/B,JAK2/3,Abl (T315I),和Flt3,IC50值范围为 1-30 nM。

规格价格库存数量
1 mg¥ 372现货
2 mg¥ 569现货
5 mg¥ 745现货
10 mg¥ 1,350现货
25 mg¥ 2,490现货
50 mg¥ 3,630现货
100 mg¥ 5,220现货
1 mL x 10 mM (in DMSO)¥ 818现货
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产品介绍

生物活性
产品描述
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).
靶点活性
JAK2:1.2 nM, JAK3:1.1 nM
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)。
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).
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)
别名J-504568
化学信息
分子量381.43
分子式C19H23N7O2
CAS No.896466-04-9
SmilesO=C(NC1CC1)Nc1c[nH]nc1-c1nc2cc(CN3CCOCC3)ccc2[nH]1
密度1.45 g/cm3
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
DMSO: 71 mg/mL (186.1 mM)
Ethanol: 22 mg/mL (57.7 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.6217 mL13.1086 mL26.2171 mL131.0857 mL
5 mM0.5243 mL2.6217 mL5.2434 mL26.2171 mL
10 mM0.2622 mL1.3109 mL2.6217 mL13.1086 mL
20 mM0.1311 mL0.6554 mL1.3109 mL6.5543 mL
50 mM0.0524 mL0.2622 mL0.5243 mL2.6217 mL
DMSO
1mg5mg10mg50mg
100 mM0.0262 mL0.1311 mL0.2622 mL1.3109 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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