448106

Met Kinase Inhibitor VI, SGX523

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.

• 別名: Met Kinase Inhibitor VI, SGX523, 6-(6-(1-Methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline, SGX523
• 実験式（ヒル表記法）: C₁₈H₁₃N₇S
• CAS番号: 1022150-57-7
• 分子量: 359.41
• MDL番号: MFCD16660190
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥97% (HPLC)
• フォーム: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: tan
• 溶解性: DMSO: 2.5 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C
• SMILES記法: S(c3[n]4c(nn3)C=CC(=N4)c5c[n](nc5)C)c1cc2c(nccc2)cc1
• InChI: 1S/C18H13N7S/c1-24-11-13(10-20-24)16-6-7-17-21-22-18(25(17)23-16)26-14-4-5-15-12(9-14)3-2-8-19-15/h2-11H,1H3
• InChI Key: BCZUAADEACICHN-UHFFFAOYSA-N

詳細

詳細

A cell-permeable triazolopyridazine compound that acts as a potent, ATP-competitive (K_i = 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.

包装

Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months -20°C.

その他情報

Buchanan, S.G., et al. 2009. Mol. Cancer Ther.8, 3181.
Eder, J.P., et al. 2009. Clin. Cancer Res.15, 2207.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable