2821793-99-9

Setidegrasib (KRAS G12D inhibitor 17, Example 8) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib has antitumor effect. (Blue: E3 ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700))[1].

KRAS(G12D)

[1] Yoshinari, et al. Preparation of quinazoline-linked (4R)-4-hydroxy-L-prolinamide compounds for inducing degradation of G12D-mutation KRAS protein: World Intellectual Property Organization, WO2022173032[P]. 2022-08-18.