TAK-285 is a potent, selective, ATP-competitive, and orally active inhibitor of HER2 and EGFR (HER1), with IC50 values of 17 nM and 23 nM, respectively. It demonstrates over 10-fold selectivity for HER1/2 compared to HER4, and is less potent against MEK1/5, c-Met, Aurora B, Lck, and CSK. This compound exhibits effective antitumor activity and can cross the blood-brain barrier (BBB).
- Potent and selective HER2 and EGFR (HER1) inhibitor.
- ATP-competitive.
- Orally active.
- High selectivity for HER1/2 over HER4.
- Effective antitumor activity against HER2-overexpressing human breast cancer cells.
- Capable of crossing the blood-brain barrier (BBB).