Description
Information(Rac)-JBJ-04-125-02 (JBJ-04-125-02 racemate) is a mutant-selective allosteric inhibitor ofEpidermal growth factor receptor (EGFR)with potential anticancer activity.TargetsEGFRIn vitroJBJ-04-125-02 can inhibit cell proliferation in vitro. Osimertinib, an ATP-competitive covalent EGFR inhibitor, uniquely and significantly enhances the binding of JBJ-04-125-02 for mutant EGFR. The combination of osimertinib and JBJ-04-125-02 results in an increase in apoptosis, a more effective inhibition of cellular growth in vitro compared to either single agent alone.In vivoJBJ-04-125-02 can inhibit EGFR L858R/T790M/C797S signaling in vivo. The combination of osimertinib and JBJ-04-125-02 results in an increase in apoptosis, and an increased efficacy in vivo compared to either single agent alone.Cell Research(from reference)Cell lines：Ba/F3, H1975, H3255GR, H3255DR cells Concentrations：0.1 nM, 1 nM, 10 nM, 0.1 µM, 1 µM Incubation Time：72 hours