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SGX-523

Catalog No.: 16070912
Cas No.: 1022150-57-7
Purity : 98% by HPLC 
16070912 - SGX-523 | CAS 1022150-57-7

Catalog number : 16070912

CAS number : 1022150-57-7

Molecular Formula : C18H13N7S 

Molecular Weight : 359.41 

Iupac Chemical Name : 6-((6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)thio)quinoline 

Smile : CN1N=CC(=C1)C=1C=CC=2N(N1)C(=NN2)SC=2C=C1C=CC=NC1=CC2

InChiKey : BCZUAADEACICHN-UHFFFAOYSA-N

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SynonymsSGX523; SGX-523 
Molecular FormulaC18H13N7S 
Molecular Weight359.41 
AppearanceSolid powder 
Purity98% by HPLC 
SolubilitySoluble in DMSO 
Storage-20 ºC for 3 years 
Shipping ConditionShipped under ambient temperature 
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
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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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