产品说明
一般描述
A cell-permeable benzamide compound that acts as a non-competitive, highly potent, selective MEK/MAPKK/MKK inhibitor and effectively blocks cellular Erk1/2 phosphorylation (by >90% in serum-starved HeLa after serum-stimulation and 50% in C26 with 25 and 0.33 nM inhibitor, respectively), while exhibiting little or no effect against the activity of Erk1/2 or a panel of 66 other kinases even at concentrations as high as 10 µM in cell-free kinase assays. Shown to be orally available in mice and suppress both the growth of and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumor in vivo. Also available in InSolution
A cell-permeable benzamide compound that acts as a non-competitive, highly potent, selective MEK/MAPKK/MKK inhibitor and effectively blocks cellular Erk1/2 phosphorylation (by >90% in serum-starved HeLa after serum-stimulation and 50% in C26 with 25 and 0.33 nM inhibitor, respectively), while exhibiting little or no effect against the activity of Erk1/2 or a panel of 66 other kinases even at concentrations as high as 10 µM in cell-free kinase assays. Shown to be orally available in mice and suppress both the growth of and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumor in vivo.
包装
5 mg in Plastic ampoule
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Barrett, S.D., et al. 2008. Bioorg. Med. Chem. Lett.18, 6501.
Leyton, J., et al. 2008. Mol. Cancer Ther.7, 3112.
Silva, J., et al. 2008. PLoS Biol.6, 2237.
Ying, Q.L., et al. 2008. Nature453, 519.
Bain, J., et al. 2007. Biochem. J.408, 297.
Solit, D.B., et al. 2006. Nature439, 358.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C16H14F3IN2O4 |
| 分子量 | 482.19 |
| MDL编号 | MFCD08435926 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥95% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | white to off-white |
| 溶解性 | DMSO: 20 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
安全信息
| 象形图 |   |
| 警示用语： | Danger |
| 危险声明 | H301 - H373 - H413 |
| 预防措施声明 | P260 - P264 - P270 - P273 - P301 + P310 - P314 |
| 危险分类 | Acute Tox. 3 Oral - Aquatic Chronic 4 - STOT RE 2 |
| 储存分类代码 | 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
