BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. It inhibits the kinase activity of EGFR L858R, T790M, and C797S with IC50 values of 1 nM, while sparing wild-type EGFR. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. It demonstrates excellent intracranial anti-tumor efficacy in a YU-1097 xenograft model, making it suitable for studying non-small cell lung cancer (NSCLC).
- Orally active
- Reversible
- ATP-competitive EGFR inhibitor
- Blood-brain barrier penetration
- Inhibits kinase activity of EGFR L858R, T790M, and C797S with IC50 values of 1 nM
- Spares wild-type EGFR
- Reduces phosphorylation of AKT, ERK, and S6K
- Demonstrates intracranial anti-tumor efficacy in YU-1097 xenograft model
- Useful for the study of non-small cell lung cancer (NSCLC)