MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. The receptor has normal roles in morphogenesis, migration, apoptosis, and angiogenesis.{23657} Dysregulation of c-Met occurs in many types of cancer.{23657} Tivantinib is a staurosporine (Item No. 81590) derivative that binds to dephosphorylated c-Met kinase, yet its mechanism of action is not known.{27930} Tivantinib has been tested in clinical studies for its ability to selectively inhibit c-Met.{27930} However, it can promote mitotic arrest and apoptosis of various human tumor cell lines (EC50s ranging from 60-600 nM) through mechanisms independent of its ability to bind c-Met.{27930} Tivantinib has been reported to bind directly to the colchicine binding site of tubulin, reducing tubulin polymerization in cells and in mouse xenograft tumors in vivo.{27931}
产品描述
A staurosporine derivative that binds to dephosphorylated c-Met kinase and to the colchicine binding site of tubulin; promotes mitotic arrest and apoptosis of various human tumor cell lines (EC50s ranging from 60-600 nM)
