Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 396 | 现货 | ||
2 mg | ¥ 569 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,350 | 现货 | ||
25 mg | ¥ 2,490 | 现货 | ||
50 mg | ¥ 3,720 | 现货 | ||
100 mg | ¥ 5,350 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
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 |
分子量 | 381.43 |
分子式 | C19H23N7O2 |
CAS No. | 896466-04-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 71 mg/mL (186.1 mM)
Ethanol: 22 mg/mL(57.7 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.6217 mL | 13.1086 mL | 26.2171 mL | 65.5428 mL |
5 mM | 0.5243 mL | 2.6217 mL | 5.2434 mL | 13.1086 mL | |
10 mM | 0.2622 mL | 1.3109 mL | 2.6217 mL | 6.5543 mL | |
20 mM | 0.1311 mL | 0.6554 mL | 1.3109 mL | 3.2771 mL | |
50 mM | 0.0524 mL | 0.2622 mL | 0.5243 mL | 1.3109 mL | |
DMSO | 100 mM | 0.0262 mL | 0.1311 mL | 0.2622 mL | 0.6554 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AT9283 896466-04-9 Angiogenesis Apoptosis Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors FLT Aurora Kinase JAK Bcr-Abl AT-9283 Cluster of differentiation antigen 135 J-504568 Janus kinase inhibit Fms like tyrosine kinase 3 FLT3 J504568 AT 9283 Inhibitor J 504568 CD135 inhibitor