BBO-8520 - CAS 2893809-51-1

BBO-8520 is a first-in-class, direct dual inhibitor of both the active (ON) and inactive (OFF) conformational states of KRASG12C. BBO-8520 binds to the Switch-II/Helix3 pocket of KRASG12C, covalently modifying the target cysteine residue and thereby disabling effector binding in the ON state. BBO-8520 exhibits potent inhibition of KRAS signaling under growth factor-activated conditions, where existing OFF-only inhibitors demonstrate minimal activity. In vivo, BBO-8520 rapidly engages its target and suppresses signaling, resulting in durable tumor regression across multiple models, including those resistant to OFF-only KRASG12C inhibitors.

Kras, Ras

GPCR/G Protein, MAPK

2893809-51-1

0.97879

C35H33F6N7O2S

729.74

N#CC1=C(SC2=C(F)C=CC(=C12)C=3C(F)=C4N=C(N=C(C4=CC3C(F)(F)F)N5CC(N(C(=O)C=C)CC5C)C)OCC67N(CCC6)CC(F)C7)N

-20°C

Ice Packs

Small Compound