BBI-2779 (E5832-GRP)

BBI-2779 is a potent, selective, and orally active inhibitor of CHK1 with an IC50 of 0.3 nM. It preferentially kills cancer cells containing extrachromosomal DNA (ecDNA) by inducing replication stress and cell death. In gastric cancer models with FGFR2 gene amplification on ecDNA, BBI-2779 suppresses tumor growth and prevents drug resistance.