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 exhibits more than 10-fold selectivity for HER1/2 over HER4 and is less potent against MEK1/5, c-Met, Aurora B, Lck, and CSK. This compound demonstrates effective antitumor activity and can cross the blood-brain barrier (BBB).
- Potent, selective, ATP-competitive, and orally active HER2 and EGFR (HER1) inhibitor
- IC50 values: HER2: 17 nM; EGFR: 23 nM
- Exhibits more than 10-fold selectivity for HER1/2 over HER4
- Less potent against MEK1/5, c-Met, Aurora B, Lck, and CSK
- Demonstrates effective antitumor activity
- Can cross the blood-brain barrier (BBB)