MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy ( EGFR WT IC 50 =281 nM, c-MET IC 50 =205 nM, B-RAF WT IC 50 =112 nM, and CDK4/6 IC 50 =95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF ( EGFR T790M IC 50 =69 nM and B-RAF V600E IC 50 =83 nM).