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BBI-2779

Development stage: Preclinical
Lead developer: Boundless Bio
Modality: Small Molecules
Administration: Oral

Overview

BBI-2779 is a potent, selective, and orally bioavailable inhibitor of CHK1 (checkpoint kinase 1) with biochemical IC50 of 0.5 nM and cellular IC50 of 3 nM (pCHK1-S345 activity in HT29 cells), showing 160-fold selectivity for CHK1 over CHK2. It preferentially kills ecDNA-containing tumor cells and has demonstrated superior biochemical and selective cell growth inhibition compared to other orally bioavailable CHK1 inhibitors. In preclinical studies, BBI-2779 has shown significant anti-tumor activity, particularly when combined with targeted therapies like infigratinib in ecDNA-positive cancer models.

Targets

CHEK1 (Checkpoint kinase 1)

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