| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Setidegrasib (10 mg/kg, i.v.) shows antitumor effect in human G12D mutant KRAS-positive pancreatic cancer strain PK-59 tumor-bearing mice[1].
| [IC 50]
KRAS(G12D) | [References]
[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. |
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