Tivantinib is a staurosporine derivative which binds to inactive, dephosphorylated MET receptor tyrosine kinase, in a manner that is not competitive with ATP (Munshi et al.; Eathiraj et al.) It is selective for MET (Ki ≅ 355 nM) in a screen of 230 kinases (Munshi et al.) It also shows cytotoxic activity which is distinct from its inhibition of MET (Basilico et al.; Katayama et al.) It has also been shown to bind directly to the colchicine binding pocket of tubulin, thereby reducing tubulin polymerization (Aoyama et al.)
