SGX-523 Inhibitor CAS No. 1022150-57-7

Cat. No.	Name	Size	Price
KI1266	SGX-523	5 mg	$272
	SGX-523	10 mg	$432
	SGX-523	25 mg	$720
	SGX-523	50 mg	$1232

Chemical Characteristic

Product Name	SGX-523
CAS No.	1022150-57-7
Molecular Weight	359.41
Formula	C₁₈H₁₃N₇S
Chemical Name	6-[[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl]quinoline
Smiles	n1cccc2cc(ccc12)Sc1n2c(ccc(n2)c2cnn(c2)C)nn1
Chemical Structure

Biological activities

SGX-523 is a potent and selective Met inhibitor with an IC50 of 4 nM. SGX-523 potently inhibits unphosphorylated form of Met [MET-KD (0P)] and phosphorylated form of Met [MET-KD (3P)] with Ki values of 2.7 and 23 nM, respectively. SGX-523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases.^[1] In human brain tumors, SGX-523 inhibits c-Met, AKT and MAPK phosphorylation, cell proliferation, cell cycle progression, migration and invasion in different human glioblastoma cell lines, glioblastoma primary cells, glioblastoma stem cells and medulloblastoma cell lines. In addition, oral administration of SGX-523 (50 mg/kg) to mice bearing intracranial human glioma xenografts leads to inhibition of tumor growth in vivo.^[2] In vivo, SGX-523 (60 mg/kg) partially inhibits the HGF-dependent growth of lung, breast, and pancreatic tumors.^[3] In human GTL16 gastric tumor model, SGX-523 significantly retards the growth of tumors when administered orally at doses of ??0 mg/kg twice daily. Furthermore, in U87MG- and H441-derived xenografts model, SGX-523 (30 mg/kg) also potently inhibits tumor growth.^[1]

Protocols

In vivo: SGX-523 is dissolved in 0.5% (w/v) Methocel A4M Premium plus 0.05% Tween 80 in distilled water.^[3]

References

[1] Buchanan SG, 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(12): 3181-3190. [2] Guessous F, et al. An orally bioavailable c-Met kinase inhibitor potently inhibits brain tumor malignancy and growth. Anticancer Agents Med Chem. 2010, 10(1): 28-35. [3] Zhang YW, 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(17): 6880-6890.

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