Catalog No.: PC-21604Not For Human Use, Lab Use Only.
Kobe2602 is a small-molecule Ras inhibitor that display antitumor activity by interfering with Ras·GTP-effector interaction, inhibits the binding of H-Ras⋅GTP to c-Raf-1 RBD with Ki of 149 uM.
Kobe2602 is a small-molecule Ras inhibitor that display antitumor activity by interfering with Ras·GTP-effector interaction, inhibits the binding of H-Ras⋅GTP to c-Raf-1 RBD with Ki of 149 uM. Kobe2602 (20 μM) efficiently inhibited the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-RasG12V. Kobe2602 (20 μM) almost completely inhibited the proliferation of H-rasG12V–transformed NIH 3T3 cells in the presence of 2% FBS (IC50=2 uM). Kobe2602 (80 mg/kg) exhibited antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-rasG12V gene by oral administration.
