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 greater than 10-fold selectivity for HER1/2 compared to HER4, and exhibits less potency against MEK1/5, c-Met, Aurora B, Lck, and CSK, among others. This compound has shown effective antitumor activity and can cross the blood-brain barrier (BBB).
- Potent and selective inhibition
- ATP-competitive
- Orally active
- Antitumor activity
- Blood-brain barrier penetration
- Inhibitory activity against BT-474 cells
- Preclinical efficacy in xenograft models