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K-756

Chemical Structure : K-756

CAS No.: 130017-40-2

K-756 (K756)

Catalog No.: PC-23199Not For Human Use, Lab Use Only.

K-756 is a small molecule inhibitor of the Wnt/β-catenin pathway with IC50 of 110 nM in Wnt/β-catenin reporter assay, and selective tankyrase (TNKS) inhibitor with IC50 of 31 and 36 nM for TNKS1 and TNKS2, stabilizes Axin1/2 by inhibiting TNKS1/2.

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

Biological Activity

K-756 is a small molecule inhibitor of the Wnt/β-catenin pathway with IC50 of 110 nM in Wnt/β-catenin reporter assay, and selective tankyrase (TNKS) inhibitor with IC50 of 31 and 36 nM for TNKS1 and TNKS2, stabilizes Axin1/2 by inhibiting TNKS1/2.
K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity.
K-756 inhibited the cell growth of APC-mutant colorectal cancer COLO 320DM and SW403 cells by inhibiting the Wnt/β-catenin pathway.
K-756 inhibited the Wnt/β-catenin pathway in colon cancer xenografts in mice.
When K-756 was combined with an EGFR inhibitor (gefitinib), it showed a strong synergistic effect.

Physicochemical Properties

M.Wt 433.51
Formula C24H27N5O3
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

3-((1-(6,7-Dimethoxyquinazolin-4-yl)piperidin-4-yl)methyl)-3,4-dihydroquinazolin-2(1H)-one

References

1. Okada-Iwasaki R, et al. Mol Cancer Ther. 2016 Jul;15(7):1525-34.

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