The invention discloses a targeted
protein degradation c-Met degradation agent as well as a preparation method and application thereof. The invention provides a c-Met degradation agent based on a targeted
protein degradation PROTAC strategy, a preparation method thereof and application of the c-Met degradation agent in the treatment of non-
small cell lung cancer, gastric
cancer and other cancers.The compound has a remarkable c-Met degradation effect and a remarkable
cell proliferation inhibition effect, has the potential of serving as an anti-tumor
drug to treat tumors, shows remarkable proliferation inhibition activity in an EBC1
drug-
resistant cell strain constructed by lentiviral
transfection, is obviously superior to a
small molecule inhibitor LXM262. and obviously improves the
cell selectivity. The compound has significant advantages in overcoming tumor c-Met acquired
drug resistance, especially the
compound S27 only provides good activity for c-Met dependent EBC-1
lung cancer cells, it is indicated that the
compound S27 has good
cell selectivity while the original
small molecule inhibitor is multi-target, and the compound also has an inhibition effect on a c-Met non-dependent cell line.