TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR (HER1) inhibitor with IC 50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B , Lck , CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
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