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Biological Activity:
Potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases.
* The HCl salt of KU-0060648 has excellent aqueous solubility.
References:
C Cano et al. Development of potent inhibitors of the DNA-dependent protein kinase (DNA-PK). RSC 2009 meeting abstract O6.
C Cano et al. Development of potent water-soluble inhibitors of the DNA-dependent protein kinase (DNA-PK). NARI cancer conference 2010 [online]
J Bardos et al. Radio- and chemosensitization through inhibition of DNA-PK by KU-0060648. Mol. Cancer Ther. 2009, 8(12 Suppl), A116. [online]
F Dumont et al. Radiosensitising agents for the radiotherapy of cancer: novel molecularly targeted approaches. Expert Opin. Ther. Pat. 2009, 19(6), 775-799. [online]
Chemical Name: 2-(4-Ethylpiperazin-1-yl)-N-(4-(2-morpholino-4-oxo-4H-chromen-8-yl)dibenzo[b,d]thiophen-1-yl)acetamide trihydrochloride
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