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.
Synonym(s):
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
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.
Packaging
Packaged under inert gas
Warning
Toxicity: Regulatory Review (Z)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months -20°C.
Other Notes
Buchanan, S.G., et al. 2009. Mol. Cancer Ther.8, 3181. Eder, J.P., et al. 2009. Clin. Cancer Res.15, 2207.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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Transglutaminase 2 (TG2) is an important mesothelioma cancer cell survival protein. However, the mechanism whereby TG2 maintains mesothelioma cell survival is not well understood. We present studies showing that TG2 drives hepatocyte growth factor (HGF)-dependent MET receptor signaling to maintain
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