(Rac)-JBJ-04-125-02 (C09-1029-383)

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. Specification: 10mM in DMSO Molecular Formula: C29H26FN5O3S Molecular Weight: 543.61 PubChem CID: 132020316 Isomeric SMILES: C1CN(CCN1)C2=CC=C(C=C2)C3=CC4=C(CN(C4=O)C(C5=C(C=CC(=C5)F)O)C(=O)NC6=NC=CS6)C=C3