Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SU9516 是一种 CDK2抑制剂,IC50值为 22 nM,对 CDK1 和 CDK4 也有抑制作用,IC50值分别为 40 和 200 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 263 | 现货 | ||
2 mg | ¥ 369 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,860 | 现货 | ||
50 mg | ¥ 2,810 | 现货 | ||
100 mg | ¥ 4,170 | 现货 | ||
500 mg | ¥ 9,070 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 689 | 现货 |
产品描述 | SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also has inhibitory effects on CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively. |
靶点活性 | CDK1:40 nM, CDK4:200 nM, CDK2:22 nM |
体外活性 | SU9516 decreases cdk2-specific phosphorylation of the retinoblastoma protein pRB, increases caspase-3 activation, and alters cell cycle in RKO and SW480 cells. SU9516 also inhibits the cell proliferation, and induces cell apoptosis in both cell lines. [1] SU9516 kills leukemic cells through inhibition of RNA Pol II CTD phosphorylation, oxidative damage and transcriptional down-regulation of Mcl-1. [2] In human T-cell leukemia Jurkat cells, SU9516 significantly enhances sensitivity to methotrexate. [3] In addition, SU9516 also suppresses Aurora-A centrosomal localization and consequent centrosome amplification. [4] |
激酶实验 | CDK kinase assay: Kinase assays are performed in 96-well polypropylene plates. Each reaction contained 2 μg of histone H1 at a final concentration of 10 μM [γ-33P]ATP (0.2 μCi/well; approximately twice the experimentally determined Km), 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100, and 10% glycerol in a 40 μL volume. The reaction is initiated with the addition of 20 μL enzyme (6 ng cdk2/well resulting in a final concentration of 1.6 nM), which is previously diluted 1:50–1:200 in the same buffer, and allowed to proceed for 1 h at room temperature. Reaction is stopped by the addition of 0.01 mL 10% phosphoric acid, and 25 μL of reaction mixture is transferred to P30 phosphocellulose filter mat paper. The filter mat is washed three times with 1.0% phosphoric acid, air dried, and then counted for radioactivity in a liquid scintillation counter. The cdk4 kinase assay for cyclin D1-cdk4 is carried out in a polypropylene 96-well microtiter plate format measuring the incorporation of radioactive phosphate into GST-Rb. Purified cyclin D1-cdk4 is incubated with 1 μg GST-Rb in 20 mM HEPES (pH 7.5) in the presence of 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100, and 10% glycerol. The final cdk4 concentration is 10 ng/well, or 1.6 nM. Kinase reaction is initiated by the addition of ATP at a final concentration of 10 μM ATP (twice the experimentally determined Km) and [γ-33P]ATP (1.0 μCi per well) in a 60-μL volume and allowed to proceed at room temperature for 1 h. Reaction is stopped by the addition of 0.01 ml 10% phosphoric acid, and 25 μL of reaction mixture is transferred to P30 phosphocellulose filter mat paper. The filter mat is treated as for Cdk1/Cdk2 assays. |
细胞实验 | Method: Cells are seeded at 2×103/well of white bottom 96-well plates, treated with INCB018424 from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37 ℃ in an atmosphere containing 5% CO2. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC50 curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad. |
分子量 | 241.25 |
分子式 | C13H11N3O2 |
CAS No. | 377090-84-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 24.1 mg/mL (100 mM)
Ethanol: 4.8 mg/mL (20 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 4.1451 mL | 20.7254 mL | 41.4508 mL | 103.6269 mL |
5 mM | 0.829 mL | 4.1451 mL | 8.2902 mL | 20.7254 mL | |
10 mM | 0.4145 mL | 2.0725 mL | 4.1451 mL | 10.3627 mL | |
20 mM | 0.2073 mL | 1.0363 mL | 2.0725 mL | 5.1813 mL | |
DMSO | 50 mM | 0.0829 mL | 0.4145 mL | 0.829 mL | 2.0725 mL |
100 mM | 0.0415 mL | 0.2073 mL | 0.4145 mL | 1.0363 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。
SU9516 377090-84-1 Apoptosis Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling MAPK p38 MAPK CDK PKC inhibit Cyclin dependent kinase SU-9516 Inhibitor SU 9516 inhibitor