KU 0060648

Name: KU 0060648
Brand: Tocris Bioscience
SKU: 4840

Tocris Bioscience, part of Bio-Techne | Catalog # 4840

Citations (1)

COA / SDS

Dual DNA-PK and PI 3-K inhibitor

Key Product Details

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)
Molecular Weight:	582.71

View Full Technical Details for KU 0060648

Technical Data
Citations

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
InChi Key	AATCBLYHOUOCTO-UHFFFAOYSA-N
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 for KU 0060648

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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.

Dumont Radiosensitising agents for the radiotherapy of cancer: novel molecularly targeted approaches. Expert Opin.Ther.Patents 2009 PMID: 19456277
Robert Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 2015 PMID: 26307031
Munck Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K. Mol.Cancer Ther. 2012 PMID: 22576130