Kobe0065 is a small-molecule Ras inhibitor, competitively inhibits the binding of H-Ras⋅GTP to c-Raf-1 RBD with Ki of 46 uM.
Kobe0065 effectively inhibit both anchorage-dependent and -independent growth and induce apoptosis of H-rasG12V–transformed NIH 3T3 cells (IC50=0.5 uM).
Kobe0065 exhibit antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-rasG12V gene by oral administration.
