Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD8330 (ARRY-704) 是非竞争性的 MEK1/MEK2抑制剂,IC50为 7 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 415 | 现货 | ||
2 mg | ¥ 597 | 现货 | ||
5 mg | ¥ 889 | 现货 | ||
10 mg | ¥ 1,550 | 现货 | ||
25 mg | ¥ 2,620 | 现货 | ||
50 mg | ¥ 3,890 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 927 | 现货 |
产品描述 | AZD8330 (ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1. |
靶点活性 | MEK1/2:7 nM |
体外活性 | AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 200 other kinases including at concentrations up to 10 μM. AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK 1/2 inhibitor sensitive cell lines. [1] |
体内活性 | In a Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model a single, 1.25 mg/kg oral dose of AZD8330 inhibits ERK phosphorylation by > 90% for between 4 and 8 hours. Doses as low as 0.4 mg/kg once daily are sufficient for > 80% tumor growth inhibition in the Calu-6 nude rat xenograft model. In the Calu-6 model, AZD8330 inhibits tumor growth in a dose-dependent fashion, at 0.3 mg/kg and 1.0 mg/kg once daily. [1] |
激酶实验 | MEK1 enzymatic assays: NH2-terminal hexahistidine tagged, constitutively active MEK1 (S218D, S222D ΔR4F) is expressed in baculovirus-infected Hi5 insect cells and purified by immobilized metal affinity chromatography, ion exchange, and gel filtration. The activity of MEK1 is assessed by measuring the incorporation of [γ- 33P]phosphate from [γ-33P]ATP onto ERK2. The assay is carried out in a 96-well polypropylene plate with an incubation mixture (100 μL) composed of 25 mM HEPES (pH 7.4), 10 mM MgCl2, 5 mM β-glycerolphosphate, 100 μM sodium orthovanadate, 5 mM DTT, 5 nM MEK1, 1 μM ERK2, and 0 to 80 nM AZD8330 (final concentration of 1% DMSO). The reactions are initiated by the addition of 10 μM ATP (with 0.5 μC k[γ-33P]ATP/well) and incubated at room temperature for 45 min. An equal volume of 25% trichloracetic acid is added to stop the reaction and precipitate the proteins. Precipitated proteins are trapped onto glass fiber B filter plates, excess labeled ATP is washed off with 0.5% phosphoric acid, and radioactivity is counted in a liquid scintillation counter. ATP dependence is determined by varying the amount of ATP in the reaction mixture. The data are globally fitted. |
细胞实验 | Malme-3M melanoma cells are plated in 96-wells and treated with various concentrations of AZD8330 for 1 hour at 37 °C. The cells are fixed, permeabilized, and incubated with an anti-phospho-ERK antibody and an anti-ERK 1/2 antibody. Plates are washed and fluorescently-labeled secondary antibodies are added. Plates are analyzed on a LICOR fluorescence imager. The pERK signal is normalized to the total ERK signa (Only for Reference) |
别名 | ARRY-424704, ARRY-704 |
分子量 | 461.23 |
分子式 | C16H17FIN3O4 |
CAS No. | 869357-68-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 85 mg/mL (184.3 mM)
DMSO: 85 mg/mL (184.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.1681 mL | 10.8406 mL | 21.6812 mL | 54.2029 mL |
5 mM | 0.4336 mL | 2.1681 mL | 4.3362 mL | 10.8406 mL | |
10 mM | 0.2168 mL | 1.0841 mL | 2.1681 mL | 5.4203 mL | |
20 mM | 0.1084 mL | 0.542 mL | 1.0841 mL | 2.7101 mL | |
50 mM | 0.0434 mL | 0.2168 mL | 0.4336 mL | 1.0841 mL | |
100 mM | 0.0217 mL | 0.1084 mL | 0.2168 mL | 0.542 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。
AZD8330 869357-68-6 MAPK ERK MEK ARRY 704 AZD 8330 ARRY-424704 ARRY-704 MAPKK Inhibitor Mitogen-activated protein kinase kinase ARRY 424704 inhibit MAP2K ARRY704 AZD-8330 ARRY424704 inhibitor