KU57788(NU7441) Chemical Properties

Melting point:

220-221 °C

Boiling point:

646.9±55.0 °C(Predicted)

Density 

1.376±0.06 g/cm3(Predicted)

storage temp. 

Store at +4°C

solubility 

Soluble in DMSO (up to 10 mg/ml with warming).

form 

solid

pka

0.51±0.20(Predicted)

color 

Off-white to beige

Stability:

Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

KU57788(NU7441) Usage And Synthesis

Description

DNA-dependent protein kinase (DNA-PK) catalyzes nonhomologous end-joining, which is required to repair lethal DNA double-strand breaks. Because cells that are defective in DNA double-strand break repair are highly sensitive to ionizing radiation and topoisomerase II poisons, modulating DNA-PK is one strategy to defer cancer cell resistance to radiation or chemotherapeutic treatments. NU 7441 is a selective DNA-PK inhibitor with an IC₅₀ value of 14 nM. It inhibits other members of the PI3K-related kinase family, including mTOR, PI3K, ataxia telangiectasia mutated (ATM), and ataxia telangiectasia and Rad3 related (ATR) with IC₅₀ values of 1.7, 5, >100, and >100 μM, respectively. NU 7441 has been shown to increase the cytotoxicity of ionizing radiation and etoposide in human colon cancer cell lines in vitro and to potentiate the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.

Uses

A potent and selective DNA-PK inhibitor with an IC50 of 14 nM.

Uses

A potent novel DNA-dependent protein kinase inhibitor models of human cancer. Antitumor agent.

Definition

ChEBI: 8-(4-dibenzothiophenyl)-2-(4-morpholinyl)-1-benzopyran-4-one is a member of dibenzothiophenes.

storage

Store at +4°C

References

1) Leahy?et al.?(2004),?Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries; Bioorg. Med. Chem. Lett.,?14?6083 2) Hardcastle?et al.?(2005),?Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach: J. Med. Chem.,?48?7829 3) Zhao?et al.?(2006),?Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441: Cancer Res.?66?5354 4) Ciszewski?et al.?(2014),?DNA-PK inhibition by NU7441 sensitizes breast cancer cells to ionizing radiation and doxorubicin: Breast Cancer Res. Treat.,?143?83 5) Yang?et al.?(2016),?NU7441 Enhances the Radiosensitivity of Liver Cancer Cells: Cell Physiol. Biochem.,?38?1897 6) Geng?et al.?(2019),?DNA-PKcs inhibitor increases the sensitivity of gastric cancer cells to radiotherapy: Oncol. Rep.,?42?561

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