Chemical Structure : ASP3082
CAS No.:
2821793-99-9
ASP3082
(ASP-3082)
Catalog No.: PC-25407Not For Human Use, Lab Use Only.
ASP3082 is a potent, selective KRAS G12D PROTAC degrader with DC50 of 38 nM, effectively induces KRAS(G12D) protein degradation with remarkable selectivity.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
ASP3082 is a potent, selective KRAS G12D PROTAC degrader with DC50 of 38 nM, effectively induces KRAS(G12D) protein degradation with remarkable selectivity.
ASP3082 effectively induced KRAS(G12D) degradation with remarkable selectivity over other KRAS variants and more than 9000 non-KRAS proteins.
ASP3082 significantly inhibits ERK phosphorylation with IC50 of 14 nM and cell proliferation with IC50 of 19 nM in pancreatic cancer cells (AsPC-1) harboring the KRAS(G12D) mutation.
ASP3082 induces selective degradation of KRAS(G12D) via VHL-mediated proteasomal degradation and inhibits KRAS signaling pathway.
ASP3082 (10 and 30 mg/kg, i.v.) demonstrates anti-tumor effect in vivo and achieves tumor regression in subcutaneous cell-line derived xenograft (CDX) mouse models using KRAS(G12D)-mutated pancreatic cancer PK-59 cells.
ASP3082 does not inhibit tumor growth in the KRAS(WT) xenograft models (A375 and HT-29).
Physicochemical Properties
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M.Wt
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1117.32
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Formula
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C60H65FN12O7S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(2S,4R)-1-((S)-2-(4-(4-((((R)-4-((1S,4S)-2,5-diazabicyclo[2.2.1]heptan-2-yl)-6-cyclopropyl-7-(6-fluoro-5-methyl-1H-indazol-4-yl)-2-((tetrahydro-2H-pyran-4-yl)oxy)quinazolin-8-yl)oxy)methyl)phenyl)-1H-1,2,3-triazol-1-yl)-3-methylbutanoyl)-4-hydroxy-N-((R)-2-hydroxy-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
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References
1. Yoshinari T, et al. Commun Chem. 2025 Aug 23;8(1):254.
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