Biological Activity
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
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 2eq.HCl | 58.27 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 582.71. Batch specific molecular weights may vary from batch to batch due to solvent 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
References are publications that support the products' biological activity.
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
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, DNA-dependent, Protein, Kinase, Tocris Bioscience
