Home Others PROTAC chemical Setidegrasib (ASP3082)

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Setidegrasib (ASP3082) PROTAC chemical

Cat.No.E4757

Setidegrasib (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. This compound shows significant antitumor efficacy across multiple murine xenograft models and serves as a research tool for investigating KRAS(G12D)-driven solid tumors. (Blue: VHL ligand ; Black: linker ; Pink: G12D-targeting moiety ).
Setidegrasib (ASP3082) PROTAC chemical Chemical Structure

Chemical Structure

Molecular Weight: 1117.30

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Chemical Information, Storage & Stability

Molecular Weight 1117.30 Formula

C60H65FN12O7S

 Storage (From the date of receipt)
CAS No. 2821793-99-9 Download SDF Storage of Stock Solutions

Synonyms ASP-3082; KRAS G12D inhibitor 17 Smiles CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)C)N4C=C(N=N4)C5=CC=C(C=C5)COC6=[C@]([C@]7=C(C(F)=CC8=C7C=NN8)C)C(C9CC9)=CC%10=C6N=C(N=C%10N%11C[C@@H]%12C[C@H]%11CN%12)OC%13CCOCC%13)=O)O)=O)CO

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Mechanism of Action

In vivo
Setidegrasib (ASP3082) exhibits dose-dependent anti-tumor activity in PK-59, LXFA 1125 NSCLC PDX, AsPC-1 (pancreatic) and GP2d (colorectal) KRAS(G12D)-mutated xenograft models of Balb/c nu/nu nude mice at doses of 0.3–30 mg/kg (i.v., once/twice weekly, 14–22 days).
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