Biological Activity
Reversible and selective inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) (IC50 values are 0.28 and 5.3 μM respectively). Displays little affinity for other commonly studied kinases including PI 3-K, ATM and ATR (IC50 values are all > 100 μM). Induces apoptosis in vitro.
Technical Data
| M. Wt | 281.31 |
| Formula | C16H15N3O2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 168425-64-7 |
| PubChem ID | 10039361 |
| InChI Key | BVRDQVRQVGRNHG-UHFFFAOYSA-N |
| Smiles | O=C3N2C=CC1=CC=CC=C1C2=NC(N4CCOCC4)=C3 |
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 | |||
| DMSO | 2.81 | 10 | |
| ethanol | 1.41 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 281.31. 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 | 3.55 mL | 17.77 mL | 35.55 mL |
| 5 mM | 0.71 mL | 3.55 mL | 7.11 mL |
| 10 mM | 0.36 mL | 1.78 mL | 3.55 mL |
| 50 mM | 0.07 mL | 0.36 mL | 0.71 mL |
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References
References are publications that support the products' biological activity.
Griffen et al (2005) Selective benzopyranone and pyrimido[2,1-α]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies and radiosensitization of a human tumor cell line in vitro. J.Med.Chem. 48 569 PMID: 15658870
Ballo et al (2007) Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)oyrimido[2,1-α]isoquinolin-4-one. J.Biol.Chem. 282 24463 PMID: 17562705
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