Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ZM 447439是一种极光激酶 (aurora) 抑制剂,对aurora A 和B 的IC50值分别为110和130 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 317 | 现货 | ||
10 mg | ¥ 579 | 现货 | ||
25 mg | ¥ 1,220 | 现货 | ||
50 mg | ¥ 2,179 | 现货 | ||
100 mg | ¥ 3,775 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 375 | 现货 |
产品描述 | ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc. |
靶点活性 | Aurora A:110 nM, Aurora B:130 nM |
体外活性 | In vitro, ZM-447439 selectively inhibits recombinant human Aurora A and B with IC50 values of 110 and 130 nM, respectively, while other protein kinases of diverse structural types including the mitotic kinases CDK1 and PLK1 are inhibited with IC50 values >10 μM. [1] Aurora kinase inhibitor, ZM-447439 time- and dose-dependently inhibits the growth of all three cell lines with IC50 values of 3 μM (BON), 0.9 μM (QGP-1) and 3 μM (MIP-101) after 72 hours of continuous exposure. In addition, ZM-447439 potently induces cell apoptosis by promoting DNA fragmentation and caspase 3 and 7 activation, and arrests GEP-NET cells in the G0 /G1and G2/M phase of the cell cycle. [2] In mouse embryo, inhibition of Aurora kinase activity by ZM-447439 results in abnormalities during mitosis by regulating the phosphorylation of histone H3 serine 10 (H3S10Ph) from G2 to metaphase with different perturbations in each embryonic cycle. [3] A recent study shows that ZM-447439 exhibits growth inhibitory and proapoptotic effect on cervical cancer SiHa cells, and enhances the chemosensitivity to cisplatin. [4] |
激酶实验 | In vitro kinase assays : Recombinant Aurora A and B are expressed as NH2-terminal His6-tagged fusion proteins using a baculovirus expression system. Aurora A is purified by affinity chromatography using Ni-NTA agarose, and Aurora B is purified by ion exchange chromatography using CM Sepharose Fast Flow. 1 ng purified recombinant enzyme is added to a reaction cocktail containing 25 mM Tris-HCl, pH 7.5, 12.5 mM KCl, 2.5 mM NaF, 0.6 mM DTT, 6.25 mM MnCl2, 10 μM peptide substrate, 10 μM for Aurora A or 5 μM ATP for Aurora B, and 0.2 μCi γ-[33P]ATP (specific activity ≥2,500 Ci/mmol), and is then incubated at RT for 60 minutes. Reactions are stopped by addition of 20% phosphoric acid, and the products are captured on P30 nitrocellulose filters and assayed for incorporation of 33P with a BetaplateTM counter. No enzyme and no compound control values are used to determine the concentration of ZM447439, which gave 50% inhibition of enzyme activity. Further details are available on request from Nicholas Keen. |
细胞实验 | Cell number is evaluated by crystal violet staining. In brief, cells in 96-well plates are fixed with 1% glutaraldehyde. Then cells are stained with 0.1% crystal violet. The unbound dye is removed by washing with water. Bound crystal violet is solubilized with 0.2% Triton X-100. Light extinction which increases linearly with the cell number is analyzed at 570 nm using an ELISA reader.(Only for Reference) |
分子量 | 513.59 |
分子式 | C29H31N5O4 |
CAS No. | 331771-20-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 51.4 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9471 mL | 9.7354 mL | 19.4708 mL | 48.677 mL |
5 mM | 0.3894 mL | 1.9471 mL | 3.8942 mL | 9.7354 mL | |
10 mM | 0.1947 mL | 0.9735 mL | 1.9471 mL | 4.8677 mL | |
20 mM | 0.0974 mL | 0.4868 mL | 0.9735 mL | 2.4338 mL | |
50 mM | 0.0389 mL | 0.1947 mL | 0.3894 mL | 0.9735 mL | |
100 mM | 0.0195 mL | 0.0974 mL | 0.1947 mL | 0.4868 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。
ZM-447439 331771-20-1 Angiogenesis Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic MAPK Tyrosine Kinase/Adaptors MEK Src Aurora Kinase Inhibitor ZM 447439 inhibit ZM447439 inhibitor