Stemcell, 73432, SU11274

SU11274 is a selective, ATP-competitive inhibitor of MET receptor tyrosine kinase (IC₅₀ = 20 nM; Sattler et al.). It shows good selectivity towards MET versus other receptor tyrosine kinases with IC₅₀ values of 1.3 μM and 9.7 μM for kinase insert domain receptor (KDR) and fibroblast growth factor receptor-1 (FGFR1), respectively (Sattler et al.). It retains activity for certain MET mutants, for example H1112Y and M1268T (Berthou et al.).

CANCER RESEARCH

· Induces apoptosis and cell cycle arrest in TPR-MET-transformed mouse pre-B (Ba/F3) cells (Sattler et al.).

· Inhibits cell viability and motility of human head and neck squamous cell carcinoma cell lines in vitro (Seiwert et al.).

· Inhibits cell viability of c-MET-expressing human non-small cell lung carcinoma cell lines in vitro (Ma et al.).