Article
Discovery of BBO-11818, a Potent and Selective Noncovalent Inhibitor of (ON) and (OFF) KRAS with Activity against Multiple Oncogenic Mutants.
Cancer discovery - 1 Apr 2026
Stahlhut Carlos, Maciag Anna E, Sullivan Kyle A, Singh Kanchan, Gitego Nadege, Zhang Zuhui, Chan Albert H, Sharma Alok K, Alexander Patrick A, Shu Jin, Yang Yue, Rigby Megan, Ma Roger, Setoodeh Saman, Smith Brian P, Pei Jun, Rabara Dana, Larsen Erik K, Turner David M, Zhang Cathy, Feng Cindy, Feng Siyu, Stice James P, Xu Rui, Lin Ken, Stephen Andrew G, Lightstone Felice C, Ji Chunmei, Wang Keshi, Simanshu Dhirendra K, Nissley Dwight V, Wallace Eli, Wang Bin, Sinkevicius Kerstin W, McCormick Frank, Beltran Pedro J
Abstract excerpt
Although KRASG12C-specific inhibitors have been introduced, no approved targeted therapies exist for other clinically significant KRAS mutants, including KRASG12D and KRASG12V. We discovered BBO-11818, a potent, selective, orally bioavailable noncovalent pan-KRAS inhibitor capable of targeting multiple KRAS mutants in both the inactive GDP-bound (OFF) and active GTP-bound (ON) states. BBO-11818 binds in the...
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