KU 0060648

Pricing Availability   Qty
Description: Dual DNA-PK and PI 3-K inhibitor
Chemical Name: 4-Ethyl-N-[4-[2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-8-yl]-1-dibenzothienyl]-1-piperazineacetamide
Purity: ≥97% (HPLC)
Literature (2)

Biological Activity for KU 0060648

KU 0060648 is a dual 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 Information

Sold under license from Cancer Research Technology Ltd.

Technical Data for KU 0060648

M. Wt 582.71
Formula C33H34N4O4S
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 881375-00-4
PubChem ID 11964036
Smiles O=C1C3=C(C(C4=CC=C(NC(CN7CCN(CC)CC7)=O)C5=C4SC6=C5C=CC=C6)=CC=C3)OC(N2CCOCC2)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for KU 0060648

Solvent Max Conc. mg/mL Max Conc. mM
2eq.HCl 58.27 100

Preparing Stock Solutions for KU 0060648

The following data is based on the product molecular weight 582.71. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.72 mL 8.58 mL 17.16 mL
5 mM 0.34 mL 1.72 mL 3.43 mL
10 mM 0.17 mL 0.86 mL 1.72 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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References for KU 0060648

References are publications that support the biological activity of the product.

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

Robert et al (2015) Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 7 93 PMID: 26307031

If you know of a relevant reference for KU 0060648, please let us know.

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Literature in this Area

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Cell Cycle and DNA Damage Research Product Guide

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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.