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448106 Met Kinase Inhibitor VI, SGX523 - CAS 1022150-57-7 - Calbiochem

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 & D

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Synonymes: 6-(6-(1-Methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline, SGX523

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448106
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Tableau de caractéristiques principal

CAS #Empirical Formula
1022150-57-7C₁₈H₁₃N₇S

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448106-5MG
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      Description
      OverviewA 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.
      Catalogue Number448106
      Brand Family Calbiochem®
      Synonyms6-(6-(1-Methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline, SGX523
      References
      ReferencesBuchanan, S.G., et al. 2009. Mol. Cancer Ther. 8, 3181.
      Eder, J.P., et al. 2009. Clin. Cancer Res. 15, 2207.
      Product Information
      CAS number1022150-57-7
      FormTan powder
      Hill FormulaC₁₈H₁₃N₇S
      Chemical formulaC₁₈H₁₃N₇S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Purity≥97% by HPLC
      Storage and Shipping Information
      Ship Code Shipped with Blue Ice or with Dry Ice
      Toxicity Regulatory Review
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Référence GTIN
      448106-5MG 04055977204681