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G007-LK

Chemical Structure : G007-LK

CAS No.: 1380672-07-0

G007-LK (G007 LK;G007LK)

Catalog No.: PC-43035Not For Human Use, Lab Use Only.

G007-LK is a potent, specific, metabolically stable TNKS1/2 inhibitor with IC50 of 46 nM and 25 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

G007-LK is a potent, specific, metabolically stable TNKS1/2 inhibitor with IC50 of 46 nM and 25 nM, respectively.
G007-LK reduces Wnt/β-catenin signaling by preventing poly(ADP-ribosyl)ation-dependent AXIN degradation, thereby promoting β-catenin destabilization.
G007-LK effectively blocks ligand-driven Wnt/β-catenin signaling in cell culture and displays approximately 50% inhibition of APC mutation-driven signaling in most CRC cell lines, inhibits the g of mouse intestinal organoids cultured ex vivo with IC50 of 80 nM.
G007-LK inhibits in vivo tumor growth in a subset of APC-mutant CRC xenograft models.

Physicochemical Properties

M.Wt 529.9576
Formula C25H16ClN7O3S
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

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

Benzonitrile, 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-

References

1. Voronkov A, et al. J Med Chem. 2013 Apr 11;56(7):3012-23.

2. Lau T, et al. Cancer Res. 2013 May 15;73(10):3132-44.

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