JCN037 (JCN 037, JGK037) is novel potent, brain-penetrant, noncovalent EGFR inhibitor with IC50 of 2.49 nM.
JCN037 demonstrated both nanomolar potency against both mutant EGFRvIII and wtEGFR in cellular assays (IC50=3.85 and 4.48 nM, respectively) and greater than 2:1 brain to plasma levels.
JCN037 shows high inhibitory activity against EGFRvIII mutant patient derived GBM cells, HK301 and GBM39, which is more potent than Erlotinib and Lapatinib.
JCN037 displays superior efficacy in an EGFR-driven orthotopic glioblastoma xenograft model.
