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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.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

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

448106
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
1022150-57-7C₁₈H₁₃N₇S

Products

RéférenceConditionnement Qté
448106-5MG Flacon en verre 5 mg
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
Référence GTIN
448106-5MG 04055977204681

Documentation

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

Titre

Fiche de données de sécurité des matériaux (FDS) 

Met Kinase Inhibitor VI, SGX523 - CAS 1022150-57-7 - Calbiochem Certificats d'analyse

TitreNuméro de lot
448106

Références bibliographiques

Aperçu de la référence bibliographique
Buchanan, S.G., et al. 2009. Mol. Cancer Ther. 8, 3181.
Eder, J.P., et al. 2009. Clin. Cancer Res. 15, 2207.
Fiche technique

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.