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APExBIO

SGX-523

In stock
Catalog No.
A1196
MET inibitor, highly selective, ATP-competitive
Grouped product items
SizePriceStock 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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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.

Product Citation

Physical Appearance

A solid

Chemical Properties

StorageStore at -20°C
M.Wt359.41
Cas No.1022150-57-7
FormulaC18H13N7S
Solubility≥17.95mg/mL in DMSO
Chemical Name6-[[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl]quinoline
SDFDownload SDF
Canonical SMILESCN1C=C(C=N1)C2=NN3C(=NN=C3SC4=CC5=C(C=C4)N=CC=C5)C=C2
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Kinase experiment [1]:

Kinase assay

Initial rate constants were measured at 21 °C in the presence of 100 mM HEPES (pH 7.5), 0.3 mg/mL poly(Glu-Tyr) peptide substrate, 10 mM MgCl2, 1 mg/mL bovine serum albumin, 5% DMSO, 20 nM MET-KD and various concentrations of ATP and SGX523. Total reaction volumes (20 μL) were quenched with 20 μL Kinase-Glo detection buffer. Luminescence was detected in a plate-reading luminometer and the results were analyzed by nonlinear regression.

Cell experiment [1]:

Cell lines

MDCK cells

Preparation method

The solubility of this compound in DMSO is > 18 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.04, 0.12, 0.36 and 3.0 μM; overnight

Applications

In MDCK canine kidney epithelial cells, SGX-523 prevented HGF-induced cell scattering.

Animal experiment [1]:

Animal models

Nude mice bearing GTL16 gastric cancer cell xenografts

Dosage form

10, 20, 30, 100 mg/kg, b.i.d., or 60 mg/kg, q.d.; p.o.

Applications

At the dose of ﹥ 10 mg /kg twice daily, SGX523 significantly retarded the growth of GTL16 xenografts. In addition, SGX523 substantially inhibited MET kinase activity.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

Biological Activity

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

Quality Control

Chemical structure

SGX-523

Related Biological Data

SGX-523

Related Biological Data

SGX-523

Related Biological Data

SGX-523