Cat. No. 4840
Chemical Name: 4-Ethyl-N-[4-[2-(4-morpholinyl)-4-o
Biological ActivityDual PI 3-K and DNA-PK inhibitor (IC50 values are <0.1, 0.5, 4 and 19 nM for PI 3-Kδ, PI 3-Kβ, PI 3-Kα and DNA-PK respectively). Inhibits proliferation of MCF7 cells in vitro and delays growth of MCF7 xenografts in mice. Also enhances CRISPR-Cas9-mediated homology-directed repair (HDR) efficiency ~2 to 4-fold, and decreases nonhomologous end-joining (NHEJ) frequency ~40%; maximum effect seen at 250 nM.
Licensing InformationSold under license from Cancer Research Technology Ltd.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Robert et al (2015) Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 7 93. PMID: 26307031.
Munck et al (2012) Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K. Mol.Cancer Ther. 11 1789. PMID: 22576130.
Dumont et al (2009) Radiosensitising agents for the radiotherapy of cancer: novel molecularly targeted approaches. Expert Opin.Ther.Patents 19 775. PMID: 19456277.
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Keywords: KU 0060648, supplier, KU0060648, antitumor, antitumour, PI, 3-K, phosphoinositide, 3-kinases, inhibits, inhibitors, DNA-PK, DNA-dependent, protein, CRISPR, Cas9, HDR, NHEJ, homology, directed, repair, nonhomologous, end, joining, Tocris Bioscience, DNA-Dependent Protein Kinase Inhibitor products
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