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SGX-523MET inibitor, highly selective, ATP-competitive

SGX-523

Catalog No. A1196
Size Price Stock Qty
10mM (in 1mL DMSO) $130.00 In stock
Evaluation Sample $28.00 In stock
5mg $120.00 In stock
25mg $320.00 In stock
100mg $780.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Shi P, Oh YT, et al. "Met gene amplification and protein hyperactivation is a mechanism of resistance to both first and third generation EGFR inhibitors in lung cancer treatment." Cancer Lett. 2016 Jul 19;380(2):494-504. PMID:27450722

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Chemical structure

SGX-523

Related Biological Data

SGX-523

Related Biological Data

SGX-523

Related Biological Data

SGX-523

Biological Activity

Description SGX-523 is a selective inhibitor of Met with IC50 of 4 nM.
Targets Met          
IC50 4 nM          

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Chemical Properties

Cas No. 1022150-57-7 SDF Download SDF
Chemical Name 6-[[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl]quinoline
Canonical SMILES CN1C=C(C=N1)C2=NN3C(=NN=C3SC4=CC5=C(C=C4)N=CC=C5)C=C2
Formula C18H13N7S M.Wt 359.41
Solubility >18mg/mL in DMSO Storage Store at -20°C
General tips No
Shipping Condition No

Background

SGX-523 is a novel, potent, ATP-competitive, and highly-selective Hepatocyte growth factor receptor (MET) inhibitor with IC50 value of 4 nM [1].

SGX523 inhibits MET autophosphorylation in gastric cancer cell line GTL16 and human lung carcinoma cell line A549, with IC50 of 40 nM and 12 nM, respectively [1]. Additionally, tumor regression was observed in gastic cancer cell line GTL16 and human GBM cell line U87MG derived mouse xenograft models that are treated with SGX-523 by oral gavage [1].

SGX523 has been shown to inhibit the phosphorylateion of MEK, MAPK, AKT in brain cancer cell lines including U87, U373, DAOY, as well as glioma stem cells 1228. The inhibition of MEK in brain cancer cells and stem cells led to cell proliferation, G1/S cell cycle progression, cell migration, and cell invasion [2].

References:
[1] Buchanan SG1, Hendle J, Lee PS, Smith CR, Bounaud PY, Jessen KA, Tang CM, Huser NH, Felce JD, Froning KJ, Peterman MC, Aubol BE, Gessert SF,Sauder JM, Schwinn KD, Russell M, Rooney IA, Adams J, Leon BC, Do TH, Blaney JM, Sprengeler PA, Thompson DA, Smyth L, Pelletier LA, Atwell S, Holme K,Wasserman SR, Emtage S, Burley SK, Reich SH. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther. 2009 Dec;8(12):3181-90.
[2] Guessous F1, Zhang Y, diPierro C, Marcinkiewicz L, Sarkaria J, Schiff D, Buchanan S, Abounader R.An orally bioavailable c-Met kinase inhibitor potently inhibits brain tumor malignancy and growth. Anticancer Agents Med Chem. 2010 Jan;10(1):28-35.