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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 & Dephosphorylation applications.

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Synonyme: 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
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
1022150-57-7C₁₈H₁₃N₇S

Preis & Verfügbarkeit

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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
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      448106-5MG 04055977204681

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

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

      TitelChargennummer
      448106

      Literatur

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

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision24-October-2011 RFH
      Synonyms6-(6-(1-Methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline, SGX523
      DescriptionA 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.
      FormTan powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1022150-57-7
      Chemical formulaC₁₈H₁₃N₇S
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (2.5 mg/ml)
      Storage Protect from light
      -20°C
      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.
      Toxicity Regulatory Review
      ReferencesBuchanan, S.G., et al. 2009. Mol. Cancer Ther. 8, 3181.
      Eder, J.P., et al. 2009. Clin. Cancer Res. 15, 2207.