BBO-8520 represents a groundbreaking first-in-class covalent inhibitor that uniquely targets both the active (ON) and inactive (OFF) states of KRAS-G12C. Through comprehensive global cysteine proteome analysis, BBO-8520 demonstrates exceptional binding specificity to KRAS-G12C, showcasing a remarkable selectivity of over 100-fold compared to wild-type KRAS and other mutant isoforms. Notably, BBO-8520 exhibits no detectable activity against N-RAS or H-RAS, underscoring its precision in selectively inhibiting KRAS-G12C. This distinctive profile positions BBO-8520 as a promising therapeutic candidate for addressing KRAS-G12C-driven cancers, offering a novel approach to targeting this historically challenging oncogenic mutation.
Cat.No
DC60571
Name
BBO-8520
Chemical Properties
CAS
2893809-51-1
Formula
C35H33F6N7O2S
MW
729.74
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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