Lapatinib (GW572016): Selectivity & Specificity
Lapatinib (GW572016) is a potent inhibitor of HER2 (10.2 nM), EGFR kinase (0.13 µM), HER2 kinase (0.037 µM), HER2 inhibition (109 nmol/L), EGFR (3 nM), human mPGES-1 (0.8 µM), mouse mPGES-1 (12 µM), β-haematin (5.43 ± 0.03 µM), EGFR/HER1 (10.8 nM), HER4 (367 nM), HER2 enzyme (9.2 nM), ER (>3000 nM), MAPK pathway, PI3K pathway, AKT, Erk1/2, PTTG, PP2A, SRC, FAK, mTORC1, AXL, Casein kinase II, CDKN1B, NFKB, IRS1, IRS4, PIK3CA, PTEN, FGFR, ABCB1, ABCG2, Glycolytic enzymes, HER3, RON, p95HER2. Lapatinib (GW572016) exhibits the greatest inhibitory potency toward EGFR (IC50 = 3 nM).