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ADT-1004

Chemical Structure : ADT-1004

CAS No.: 1945941-72-9

ADT-1004 (ADT1004)

Catalog No.: PC-23212Not For Human Use, Lab Use Only.

ADT-1004 is an orally bioavailable prodrug of ADT-007, potent, selective pan-RAS inhibitor, selectively inhibits PDAC cells with mutant KRAS, does not impact the growth of tumors from RAS WT PDAC cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ADT-1004 is an orally bioavailable prodrug of ADT-007, potent, selective pan-RAS inhibitor, selectively inhibits PDAC cells with mutant KRAS, does not impact the growth of tumors from RAS WT PDAC cells.
ADT-1004 is designed to improve the water solubility and metabolic stability of ADT-007.
ADT-1004 inhibited ERK phosphorylation in PDAC tumors.
ADT-1004 blocked tumor growth and ERK phosphorylation in PDX PDAC models with KRAS G12D , KRAS G12V , KRAS G12C , or KRAS G13Q mutations.
ADT-1004 treatment increased CD4 + and CD8 + T cells in the TME consistent with exhaustion and increased MHCII + M1 macrophage and dendritic cells
ADT-1004 demonstrated superior efficacy over sotorasib and adagrasib in tumor models involving human PDAC cells resistant to these KRAS G12C inhibitors.

Physicochemical Properties

M.Wt 589.66
Formula C33H36FN3O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(Z)-4-((5-fluoro-3-(2-((furan-2-ylmethyl)amino)-2-oxoethyl)-2-methyl-1H-inden-1-ylidene)methyl)-2,6-dimethoxyphenyl (1-methylpiperidin-4-yl)carbamate

References

1. Reddy Bandi DS, et al. bioRxiv [Preprint]. 2024 Oct 8:2024.10.04.616725.

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