您的位置：首页 > 产品中心 > 1022150-57-7， Met Kinase Inhibitor VI, SGX523-CAS 1022150-57-7-Calbiochem
Met Kinase Inhibitor VI, SGX523-CAS 1022150-57-7-Calbiochem
| 产品编号： | 4084106 |
| 规格： | The Met Kinase Inhibitor VI, SGX523, also referenced under CAS 1022150-57-7, controls the biological activity of Met Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. |
| CAS NO： | 1022150-57-7 |
| 包装规格： | 5 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
1022150-57-7
Met Kinase Inhibitor VI, SGX523-CAS 1022150-57-7-Calbiochem
6-(6-(1-Methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline, SGX523
基本信息
| Empirical Formula【经验(实验)分子式】 | C18H13N7S |
| Molecular weight | 359.41 |
| General description【一般描述】 | A cell-permeable triazolopyridazine compound that acts as a potent, ATP-competitive (Ki = 2.7 & 23 nM using non-phosphorylated and phosphorylated MET kinase domain, respectively), and highly selective inhibitor against the tyrosine kinase activity of the HGF (hepatocyte growth factor) receptor c-MET (IC50 = 4 nM), while exhibiting little or no activity toward a panel of more than 210 other kinases, including the closely related RTK RON. Shown to inhibit the constitutive (IC50 = 40 nM in GTL16 cells) as well as HGF-stimulated (IC50 = 12 nM in A549 cells) MET autophosphorylation/activation in cultures in vitro and effectively suppress MET-dependent tumor growths in mice in vivo (twice daily oral dosings at 30 mg/kg). X-ray crystallography reveals that SGX523 locks MET in a "DFG-in" conformation with the triazolopyridazine moiety interacting with the hydrophobic side chains of Met1229 and Tyr1248, while Tyr1248 mutations are found to render MET insensitive to SGX523 inhibition both in cell-free and cell-based assays. |
| Warning【警告】 | Toxicity: Regulatory Review (Z) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months -20°C. |
| Other Notes【其他说明】 | Buchanan, S.G., et al. 2009. Mol. Cancer Ther.8, 3181. Eder, J.P., et al. 2009. Clin. Cancer Res.15, 2207. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥97% (HPLC) |
| form【形式】 | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | tan |
| solubility【溶解性】 | DMSO: 2.5 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | −20℃ |
| packaging【包装】 | 5 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 2 |
