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SGX523 | cMET inhibitor

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Price:
$129.00
Catalog #:
C7523-5
Quantity:


Product Description

SGX523 is an ATP-competitive, triazolopyridazine-based inhibitor of MET at an IC50 of 4 nM. SGX523 has higher affinity for the unphosphorylated form of MET (Ki = 2.7 nM) than the more active phospho-enzyme (Ki = 23 nM). In a broad panel of 213 kinases, SGX523 was extremely selective, with no inhibition >36%, suggesting IC50 values > 1 uM, including the closely-associated RON kinase. [1]

SGX523 inhibits MET phosphorylation and downstream ERK and AKT activation in a dose-dependent manner, and nearly eliminates HGF-induced MET activation at 1 uM. Downstream inhibition of ERK is enhanced in combination with erlotinib, affectding tyrosine phosphorylation of ErbB3 and EGFR. In HGF-induced NCI-H596 cells, SGX523 exhibited cell cycle inhibition by reducing the number of cells in the S phase from 32% to 9%. [2]

SGX523 was discontinued in Phase I trials due to unexpected toxicity (compromised kidney function, increased serum creatinine).


Technical information:

Chemical Formula:   C18H13N7S
CAS #:   1022150-57-7
Molecular Weight:   359.41
Purity:   >98%
Appearance:   Pale Pink
Chemical Name:   6-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline
Solubility:   Up to 5 mM in DMSO
Synonyms:   SGX-523, SGX 523, SGX523

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Buchanan et al., SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol. Cancer Ther. 2009, 8, 3181-3290. Pubmed ID: 19934279
2. Zhang et al., MET kinase inhibitor SGX523 synergizes with epidermal growth factor receptor inhibitor erlotinib in a hepatocyte growth factor-dependent fashion to suppress carcinoma growth. Cancer Res. 2010, 70, 6880-6890. Pubmed ID: 20643778

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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