D6808 is a highly selective and potent macrocyclic c-Met inhibitor with IC50 of 2.9 nM.
D6808 potently inhibited c-Met kinase and MET-amplified Hs746T gastric cancer cells with IC50 values of 2.9 and 0.7 nM, respectively.
D6808 also strongly suppressed Ba/F3-Tpr-Met cells harboring resistance-relevant mutations (F1200L/M1250T/H1094Y/F1200I/L1195V) with IC50 values of 4.2, 3.2, 1.0, 39.0, and 33.4 nM, respectively.
D6808 exhibited extraordinary target specificity in a Kinome profiling against 373 wild-type kinases.
