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SGX-523

Chemical Structure : SGX-523

CAS No.: 1022150-57-7

SGX-523 (SGX523;SGX 523)

Catalog No.: PC-42835Not For Human Use, Lab Use Only.

SGX-523 (SGX523) is a potent, selective ATP-competitive inhibitor of MET receptor tyrosine kinase with IC50 of 4 nM, does not inhibit RON and a panel of kinases.

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Biological Activity

SGX-523 (SGX523) is a potent, selective ATP-competitive inhibitor of MET receptor tyrosine kinase with IC50 of 4 nM, does not inhibit RON and a panel of kinases.
SGX-523 shows higher affinity for unphosphorylated form of MET (Ki = 2.7 nM) versus the more active phospho-MET (Ki=23 nM).
SGX-523 inhibits MET-mediated signaling, cell proliferation, and cell migration at nanomolar concentrations but has no effect on signaling dependent on other protein kinases.
SGX-523 inhibits MET autophosphorylation with IC50 of 40 nM in GTL16 cells, inhibits MET-dependent tumor growth in vivo.

Physicochemical Properties

M.Wt 359.4077
Formula C18H13N7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 3.6 mg/mL

Chemical Name/SMILES

Quinoline, 6-[[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]-

References

1. Buchanan SG, et al. Mol Cancer Ther. 2009 Dec;8(12):3181-90.

2. Guessous F, et al. Anticancer Agents Med Chem. 2010 Jan;10(1):28-35.

3. Zhang YW, et al. Cancer Res. 2010 Sep 1;70(17):6880-90.

4. Xie Q, et al. Proc Natl Acad Sci U S A. 2012 Jan 10;109(2):570-5.

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