SGX-523

SGX-523 is a highly selective, orally bioavailable small molecule inhibitor of the MET receptor tyrosine kinase (also known as hepatocyte growth factor receptor or HGFR). It acts as an ATP-competitive inhibitor with nanomolar potency (IC50 = 4 nM for MET), showing over 1,000-fold selectivity versus other kinases. By binding to c-Met and preventing activation by its ligand HGF, it disrupts downstream signaling pathways involved in tumor cell proliferation, survival, invasion, metastasis and angiogenesis. Preclinical studies demonstrated antitumor activity in xenograft models of glioblastoma and lung/gastric cancers dependent on MET signaling. However, clinical development was discontinued due to unexpected nephrotoxicity observed in Phase I trials[1][2][5][8][9].

Other names

1022150-57-7WH8SQN09KJWH-8SQN09KJWH 8SQN09KJCHEBI:906246-(6-(1-methyl-1H-pyrazol-4-yl)-(1,2,4)triazolo(4,3-b)pyridazin-3-ylsulfanyl)quinoline