(Rac)-JBJ-04-125-02 is a potent, mutant-selective, allosteric inhibitor of EGFR T790M/L858R with IC50 of 0.26 nM.
JBJ-04-125-02 displays excellent selectivity against a panel of 468 kinases using the KINOMEscan approach (S-Score (35)=0.02).
JBJ-04-125-02 increases apoptosis and efficacy in vitro and in vivo compared with either single agent alone when combined with osimertinib.
