生化/生理作用
Potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor in vitro and in vivo.
NU7441 is a potent and selective DNA-dependent protein kinase inhibitor (DNA-PK IC50 = 14 nM; IC50 = 1.7 μM/mTOR, 5 μM/PI3Kα, >100 μM/ATM & ATR) that effectively sensitizes cancer cells to the cytotoxic effects of both ionizing radiation and the topoisomerase II inhibitor etoposide in cultures (0.5 μM; SW620 & LoVo cells) and in vivo (10 mg/kg via daily i.p. in mice with human colon cancer SW620 xenografts).
NU7441 is a potent and selective DNA-dependent protein kinase inhibitor (DNA-PK IC50 = 14 nM; IC50 = 1.7 μM/mTOR, 5 μM/PI3Kα, >100 μM/ATM & ATR) that effectively sensitizes cancer cells to the cytotoxic effects of both ionizing radiation and the topoisomerase II inhibitor etoposide in cultures (0.5 μM; SW620 & LoVo cells) and in vivo (10 mg/kg via daily i.p. in mice with human colon cancer SW620 xenografts).
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Sensitization of breast carcinoma cells to ionizing radiation by small molecule inhibitors of DNA-dependent protein kinase and ataxia telangiectsia mutated
Biochemical Pharmacology, 71(1-2), 13-20 (2005)
Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441
Cancer research, 66(10), 5354-5362 (2006)
Justin J J Leahy et al.
Bioorganic & medicinal chemistry letters, 14(24), 6083-6087 (2004-11-18)
A solution-phase multiple-parallel synthesis approach was employed for the preparation of 6-, 7- and 8-aryl-substituted chromenone libraries, which were screened as inhibitors of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). These studies resulted in the identification of 8-dibenzothiophen-4-yl-2-morpholin-4-yl-chromen-4-one (NU7441)
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