SGX-523 MedChemExpress (MCE)

Product Name	6-((6-(1-methyl-1h-pyrazol-4-yl)-1,2,4-triazolo(4,3-b)pyridazin-3-yl)thio)quinoline
Synonyms	SGX523 SGX-523 SGX 523 SGX 523(SGX-523) 6-((6-(1-methyl-1h-pyrazol-4-yl)-1,2,4-triazolo(4,3-b)pyridazin-3-yl)thio)quinoline 6-[[6-(1-Methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]quinoline Synonyms SGX523 SGX-523 SGX 523 SGX 523(SGX-523) 6-((6-(1-methyl-1h-pyrazol-4-yl)-1,2,4-triazolo(4,3-b)pyridazin-3-yl)thio)quinoline 6-[[6-(1-Methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]quinoline 6-[[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl]quinoline Quinoline,6-[[6-(1-Methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]- 6-[[6-(1-Methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]quinoline SGX 523
CAS	1022150-57-7
EINECS
Chemical Formula	C18H13N7S
Molecular Weight	359.41
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg;50 mg
Price	Get quote
Descriptions	SGX-523 SGX-523 MedChemExpress (MCE) HY-12019 1022150-57-7 99.23% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions SGX-523 SGX-523 MedChemExpress (MCE) HY-12019 1022150-57-7 99.23% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. SGX523 is a exquisitely selective and ATP-competitive MET inhibitor. SGX523 potently inhibits MET with an IC50 of 4 nM and is >1,000-fold selective versus other protein kinases. Antitumor activity. SGX523 shows ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD(0P), Ki=2.7 nM] versus the more active phospho-enzyme [MET-KD(3P), Ki=23 nM][1]. SGX523 inhibits the growth of gastric and lung cancer cell lines with amplification of the MET gene but has no effect, even at high micromolar concentration, on cell lines with normal MET gene copy number. TheIC50s of 0.02, 0.113, and 0.035 μM for NSCLC H1993, gastric cncer MKN45, and gastric cancer Hs746T cells, respectively[1]. The IC50 value for the inhibition of MET autophosphorylation is 0.040 μM in GTL16 cells[1]. SGX523 (0.5, 1.5, 4.6, 13.7, 41, 123, 370, 1100, 3300, 10000 nM 1 hour) inhibits MET autophosphorylation without affecting total MET or extracellular signal-regulated kinase protein levels in HGF-stimulated A549 cells[1]. SGX523 exhibits antitumor activity in vivo. SGX523 inhibits MET-dependent tumor growth[2]. \| \| \| \| \| \| \| \| \| \| [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. [Content Brief]
Last Update	2025-04-01 14:45:47

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