Repotrectinib Increases KRAS-G12C Inhibitor Effectiveness Via Simultaneous Inhibition of SRC, FAK, and JAK2
Published date:
10/09/2020
Excerpt:
Repotrectinib/AMG510 synergistically decreases KRASG12C NSCLC cell viability and induces apoptosis more robustly relative to either single agent treatments or AMG510 combinations with inhibitors that have a subset of repotrectinib activities.
Abstract 1958: Repotrectinib increases effectiveness of KRAS-G12C inhibitors in KRAS-G12C mutant cancer models via simultaneous SRC/FAK/JAK2 inhibition
Published date:
05/15/2020
Excerpt:
Adding repotrectinib to AMG510 improves AMG510 effectiveness on KRAS-G12C mutant cancer cells with notably increased apoptosis...Treatment of H358 cells with AMG510 alone (100 nM) or repotrectinib alone (1 µM) resulted in slight increases in cleaved PARP and caspase-3 proteins, whereas larger increases were observed with the combination.