H-Ras-cRaf1 interaction inhibitor; inhibits Raf signaling. Selectively attenuates proliferation and induces apoptosis of cancer cells harboring Ras oncogenes. Reduces growth of K-Ras mutant SW480 colon carcinoma cell xenografts in mice. Orally active.
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In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction.
Shima et al.