Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MBQ-167 是一种 Rac/Cdc42 的双重抑制剂,在 MDA-MB-231 细胞中,Rac 1/2/3 和 Cdc42 的 IC50 分别为 103 nM 和 78 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 279 | 现货 | ||
2 mg | ¥ 393 | 现货 | ||
5 mg | ¥ 659 | 现货 | ||
10 mg | ¥ 987 | 现货 | ||
25 mg | ¥ 1,970 | 现货 | ||
50 mg | ¥ 2,930 | 现货 | ||
100 mg | ¥ 4,260 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 768 | 现货 |
产品描述 | MBQ-167 is a dual inhibitor of Rac/Cdc42 (IC50s: 103 nM for Rac 1/2/3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively). |
靶点活性 | CDC42:78 nM, Ras1/2/3:103 nM |
体外活性 | MBQ-167 causes this phenotype in multiple mesenchymal cancer cell types including GFP-HER2-BM, MDA-MB-468, and Hs578t human breast cancer cells, as well as Mia-PaCa-2 pancreatic cancer cells, SKOV3 ovarian cancer cells, AGS and NCI-N87 gastric cancer cells, and SH-SY5Y neuroblastoma cells. MBQ-167 (≥100 nM) causes a loss of polarity in metastatic breast cancer cells. MBQ-167(500 nM; 24 h)treatment, results in ~95% cell rounding and detachment from the substratum in metastatic MDA-MB-231 cells. At earlier times (6h), MBQ-167(250 or 500 nM)treatment, induce an inhibition in Rac activity in the attached cell population, while the detached population demonstrates a ~40-50% inhibition. The attached population of MDA-MB-231 cells demonstrate a ~25% decrease in Rac activation while the detached cells are more responsive with a ~75% decrease following treatment with 250 nM MBQ-167 for 24 h . |
体内活性 | MBQ-167 treated mice display similar doubling times for both treatments (10 and 11 days). MBQ-167-treated mice show a statistically significant reduction in tumor growth. At sacrifice, 1.0 mg/kg BW of MBQ-167 causes a ~80% reduction in tumor growth, and the 10 mg/kg BW MBQ-167 treatment results in a ~95% reduction in tumor growth. Since EHop-016 only exerts ~40% reduction of tumor growth at 10 mg/kg BW, MBQ-167 is 10X more effective than EHop-016 . |
分子量 | 338.41 |
分子式 | C22H18N4 |
CAS No. | 2097938-73-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 0.1 mg/mL (insoluble)
DMSO: 155 mg/mL (458.02 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.955 mL | 14.775 mL | 29.55 mL | 73.8749 mL |
5 mM | 0.591 mL | 2.955 mL | 5.91 mL | 14.775 mL | |
10 mM | 0.2955 mL | 1.4775 mL | 2.955 mL | 7.3875 mL | |
20 mM | 0.1477 mL | 0.7387 mL | 1.4775 mL | 3.6937 mL | |
50 mM | 0.0591 mL | 0.2955 mL | 0.591 mL | 1.4775 mL | |
100 mM | 0.0295 mL | 0.1477 mL | 0.2955 mL | 0.7387 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。
MBQ-167 2097938-73-1 Cell Cycle/Checkpoint GPCR/G Protein MAPK CDK Ras Cyclin dependent kinase Inhibitor inhibit MBQ167 MBQ 167 inhibitor