BGG463

BGG463 (NVP-BGG463) was generated by a rational 'hybrid design' approach. Like Imatinib, BGG463 disrupts the assembly of the hydrophobic spine, a characteristic feature of the active state of several kinases, thereby locking the kinase in an inactive 'DFG-out' conformation. BGG463 can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 µM, 0.09 µM and 0.590 µM, respectively.