| Identification | Back Directory | [Name]
K-756 | [CAS]
130017-40-2 | [Synonyms]
K-756
K-756 >=98% (HPLC)
2(1H)-Quinazolinone, 3-[[1-(6,7-dimethoxy-4-quinazolinyl)-4-piperidinyl]methyl]-3,4-dihydro- | [Molecular Formula]
C24H27N5O3 | [MOL File]
130017-40-2.mol | [Molecular Weight]
433.5 |
| Chemical Properties | Back Directory | [Melting point ]
216-218 °C | [Boiling point ]
680.0±55.0 °C(Predicted) | [density ]
1.261±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:4.55(Max Conc. mg/mL);10.5(Max Conc. mM) | [form ]
Solid | [pka]
14.92±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
K-756 is a a selective Wnt/β-catenin pathway inhibitor. K-756 is also a tankyrase (TNKS) inhibitor. K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. could be a leading compound in the development of anticancer agents. | [Uses]
K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC50s of 31 and 36 nM, respectively. | [in vitro]
K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. Moreover, PARP family enzyme assays showed that K-756 is a selective TNKS inhibitor. K-756 inhibited the cell growth of APC-mutant colorectal cancer COLO 320DM and SW403 cells by inhibiting the Wnt/β-catenin pathway. _x000D_
_x000D_
Reference: Mol Cancer Ther. 2016 Jul;15(7):1525-34. https://pubmed.ncbi.nlm.nih.gov/27196752/ | [in vivo]
An in vivo study showed that the oral administration of K-756 inhibited the Wnt/β-catenin pathway in colon cancer xenografts in mice._x000D_
_x000D_
Reference: Mol Cancer Ther. 2016 Jul;15(7):1525-34. https://pubmed.ncbi.nlm.nih.gov/27196752/ | [target]
K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TMS1 amd TMLS2 with IC50s of 31 and 36 nM, respectively. | [IC 50]
TNKS1: 31 nM (IC50); TNKS2: 36 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Okada-Iwasaki R, et al. The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase. Mol Cancer Ther. 2016 Jul;15(7):1525-34. DOI:10.1158/1535-7163.MCT-15-0938 |
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| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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