Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TAK-733 是选择性 MEK 抑制剂,IC50为 3.2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 456 | 现货 | ||
2 mg | ¥ 659 | 现货 | ||
5 mg | ¥ 987 | 现货 | ||
10 mg | ¥ 1,930 | 现货 | ||
25 mg | ¥ 3,490 | 现货 | ||
50 mg | ¥ 4,960 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,150 | 现货 |
产品描述 | TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. |
靶点活性 | MEK1:3.2 nM |
体外活性 | TAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells. [1] |
体内活性 | TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. TAK-733 is well tolerated with pharmacokinetics and pharmacodynamics that support once-daily oral dosing in humans. [1] TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg. [2] |
激酶实验 | Fluorescence Polarization Based Assays for XIAP, cIAP1, and cIAP2 BIR3 Proteins: FL-AT-406 (the fluorescently tagged AT-406) is employed to develop a set of new FP assays for determination of the binding affinities of Smac mimetics to XIAP, cIAP-1, and cIAP-2 BIR3 proteins. The Kd value of FL-AT-406 to each IAP protein is determined by titration experiments using a fixed concentration of FL-AT-406 and different concentrations of the protein up to full saturation. Fluorescence polarization values are measured using an Infinite M-1000 plate reader in Microfluor 2 96-well, black, round-bottom plates. To each well, FL-AT-406 (2, 1, and 1 nM for experiments with XIAP BIR3, cIAP-1 BIR3, and cIAP-2 BIR3, respectively) and different concentrations of the protein are added to a final volume of 125 μL in the assay buffer (100 mM potassium phosphate, pH 7.5, 100 μg/mL bovine γ-globulin, 0.02% sodium azide, with 4% DMSO). Plates are mixed and incubated at room temperature for 2-3 hours with gentle shaking. The polarization values in millipolarization units (mP) are measured at an excitation wavelength of 485 nm and an emission wavelength of 530 nm. Equilibrium dissociation constants (Kd) are then calculated by fitting the sigmoidal dose-dependent FP increases as a function of protein concentrations using Graphpad Prism 5.0 software. In competitive binding experiments for XIAP3 BIR3, AT-406 is incubated with 20 nM XIAP BIR3 protein and 2 nM FL-AT-406 in the assay buffer (100 mM potassium phosphate, pH 7.5; 100 μg/mL bovine γ-globulin; 0.02% sodium azide). In competitive binding experiments for cIAP1 BIR3 protein, 3 nM protein and 1 nM FL-AT-406 are used. In competitive binding experiments for cIAP2 BIR3, 5 nM protein and 1 nM FL-AT-406 are used. For each competitive binding experiment, polarization values are measured after 2-3 hours of incubation using an Infinite M-1000 plate reader.The IC50 value, the inhibitor concentration at which 50% of the bound tracer is displaced, is determined from the plot using nonlinear least-squares analysis. Curve fitting is performed using the PRISM software. A Ki value for AT-406 is calculated. |
别名 | TAK733, TAK 733 |
分子量 | 504.23 |
分子式 | C17H15F2IN4O4 |
CAS No. | 1035555-63-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: <1 mg/mL
Ethanol: <1 mg/mL
DMSO: 93 mg/mL (184.4 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9832 mL | 9.9161 mL | 19.8322 mL | 49.5805 mL |
5 mM | 0.3966 mL | 1.9832 mL | 3.9664 mL | 9.9161 mL | |
10 mM | 0.1983 mL | 0.9916 mL | 1.9832 mL | 4.9581 mL | |
20 mM | 0.0992 mL | 0.4958 mL | 0.9916 mL | 2.479 mL | |
50 mM | 0.0397 mL | 0.1983 mL | 0.3966 mL | 0.9916 mL | |
100 mM | 0.0198 mL | 0.0992 mL | 0.1983 mL | 0.4958 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。
TAK-733 1035555-63-5 MAPK MEK TAK733 inhibit Inhibitor MAP2K MAPKK TAK 733 Mitogen-activated protein kinase kinase inhibitor