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SGX-523

Catalog No.: 16070912
Cas No.: 1022150-57-7
Purity : 98% by HPLC 

SGX523 is a novel, ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L and is >1,000-fold selective versus the >200-fold selectivity of other protein kinases tested in biochemical assays. Crystallographic study revealed that SGX523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases, suggesting an explanation for the selectivity. SGX523 inhibited MET-mediated signaling, cell proliferation, and cell migration at nanomolar concentrations but had no effect on signaling dependent on other protein kinases, including the closely related RON, even at micromolar concentrations. SGX523 inhibition of MET in vivo was associated with the dose-dependent inhibition of growth of tumor xenografts derived from human glioblastoma and lung and gastric cancers, confirming the dependence of these tumors on MET catalytic activity. Our results show that SGX523 is the most selective inhibitor of MET catalytic activity described to date and is thus a useful tool to investigate the role of MET kinase in cancer without the confounding effects of promiscuous protein kinase inhibition.  

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Chemical Information

NameSGX-523
Iupac Chemical Name6-((6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)thio)quinoline 
SynonymsSGX523; SGX-523 
Molecular FormulaC18H13N7S 
Molecular Weight359.41 
SmileCN1N=CC(=C1)C=1C=CC=2N(N1)C(=NN2)SC=2C=C1C=CC=NC1=CC2
InChiKeyBCZUAADEACICHN-UHFFFAOYSA-N
InChiInChI=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
CAS Number1022150-57-7
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Ordering Information

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FormulationSolid powder 
Purity98% by HPLC 
Storage-20 ºC for 3 years 
SolubilitySoluble in DMSO 
Handling
Shipping ConditionShipped under ambient temperature 
HS Code
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study
Not available

Chemical Structure

16070912 - SGX-523 | CAS 1022150-57-7

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