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merck millipore,默克密理博,448106,Met Kinase Inhibitor VI, SGX523 - CAS 1022150-57-7 - Calbiochem
产品名称：Met Kinase Inhibitor VI, SGX523 - CAS 1022150-57-7 - Calbiochem
产品型号：448106
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 & Depho More>>
merck millipore,默克密理博,448106,Met Kinase Inhibitor VI, SGX523 - CAS 1022150-57-7 - Calbiochem
- 产品介绍
重要规格表
经验配方 CAS号 C₁₈H₁₃N₇S 1022150-57-7 描述 概述 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. 产品目录编号 448106 品牌系列 Calbiochem®
同义词 6-(6-(1-Methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline, SGX523 参考 参考 Buchanan, S.G., et al. 2009. Mol. Cancer Ther. 8, 3181.
Eder, J.P., et al. 2009. Clin. Cancer Res. 15, 2207.产品信息 CAS号 1022150-57-7 形式 Tan powder Hill配方 C₁₈H₁₃N₇S 化学配方 C₁₈H₁₃N₇S Molar Mass 359.4 结构配方图像 生物信息 纯度 ≥97% by HPLC 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Shipped with Blue Ice or with Dry Ice
毒性 Regulatory Review
储存 -20°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
上一件merck millipore产品：merck millipore,默克密理博,6510-OP,OmniPur Polyethylene Glycol 8,000 - CAS 25322-68-3 - Calbiochem
下一件merck millipore产品：merck millipore,默克密理博,05-406,Anti-JAK3 Antibody, clone B32-32
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