Setidegrasib (ASP3082)

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Setidegrasib (KRAS G12D inhibitor 17, ASP3082) is a PROTAC-based KRAS degrader (DC50 = 37 nM) that specifically targets G12D-mutated KRAS protein for degradation. It demonstrates potent inhibition of p-ERK, p-AKT, and p-S6 signaling pathways in AsPC-1 cells. The compound shows significant antitumor efficacy across multiple murine xenograft models. Setidegrasib serves as a research tool for investigating KRAS (G12D) -driven solid tumors. (Blue: VHL ligand ; Black: linker ; Pink: G12D-targeting moiety) .