Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PD318088 是非 ATP 竞争性的MEK1/2变构抑制剂,是 PD184352 的结构类似物。它在MEK1 活性位点与 ATP 结合位点相邻的区域与 ATP 同时结合,可用于癌症研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 427 | 现货 | ||
2 mg | ¥ 615 | 现货 | ||
5 mg | ¥ 997 | 现货 | ||
10 mg | ¥ 1,980 | 现货 | ||
25 mg | ¥ 3,370 | 现货 | ||
50 mg | ¥ 4,880 | 现货 | ||
100 mg | ¥ 6,990 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,290 | 现货 |
产品描述 | PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. |
体外活性 | PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure. [1] |
激酶实验 | Enzyme Assays: Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method from Invitrogen. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software. |
分子量 | 561.09 |
分子式 | C16H13BrF3IN2O4 |
CAS No. | 391210-00-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 14 mg/mL (24.95 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 112 mg/mL (199.61 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.7822 mL | 8.9112 mL | 17.8225 mL | 44.5561 mL |
5 mM | 0.3564 mL | 1.7822 mL | 3.5645 mL | 8.9112 mL | |
10 mM | 0.1782 mL | 0.8911 mL | 1.7822 mL | 4.4556 mL | |
20 mM | 0.0891 mL | 0.4456 mL | 0.8911 mL | 2.2278 mL | |
DMSO | 50 mM | 0.0356 mL | 0.1782 mL | 0.3564 mL | 0.8911 mL |
100 mM | 0.0178 mL | 0.0891 mL | 0.1782 mL | 0.4456 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。
PD318088 391210-00-7 MAPK MEK Mitogen-activated protein kinase kinase PD 318088 inhibit PD-318088 MAPKK MAP2K Inhibitor inhibitor