ASP3082 | KRAS G12D PROTAC | Probechem Biochemicals

Chemical Structure : ASP3082

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ASP3082 (ASP-3082)

货号: 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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100 mg		Get quote

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生物&药学活性

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).

物理化学性质&存储条件

分子量	1117.32
分子式	C60H65FN12O7S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

参考文献

1. Yoshinari T, et al. Commun Chem. 2025 Aug 23;8(1):254.

ASP3082 (ASP-3082)

生物&药学活性

物理化学性质&存储条件

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ASP3082 (ASP-3082)

生物&药学活性

物理化学性质&存储条件

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