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Description: Potent and selective DNA-PK inhibitor; enhances CRISPR-mediated HDR efficiency
Chemical Name: 7,9-Dihydro-7-methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-8H-purin-8-one
Purity: ≥98% (HPLC)
Biological Activity for AZD 7648
AZD 7648 is a potent (IC50 = 0.6 nM in an enzyme assay) and selective DNA-PK inhibitor. It is selective for DNA-PK over a range of kinases including PI3Kα, PI3Kδ, PI3Kγ, ATM, ATR and mTOR. In combination with radiotherapy, it leads to tumor regression in fully immuno-competent mice models. It also enhances the activity of PARP inhibitor Olaparib (Cat. No. 7579). AZD 7648 is orally bioavailable. AZD 7648 also enhances CRISPR-mediated HDR efficiency.
Technical Data for AZD 7648
| M. Wt | 380.41 |
| Formula | C18H20N8O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2230820-11-6 |
| PubChem ID | 135151360 |
| InChI Key | XISVSTPEXYIKJL-UHFFFAOYSA-N |
| Smiles | O=C1N(C)C2=CN=C(NC3=CN4N=CN=C4C=C3C)N=C2N1C5CCOCC5 |
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 AZD 7648
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.61 | 20 |
Preparing Stock Solutions for AZD 7648
The following data is based on the product molecular weight 380.41. 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 |
|---|---|---|---|
| 0.2 mM | 13.14 mL | 65.72 mL | 131.44 mL |
| 1 mM | 2.63 mL | 13.14 mL | 26.29 mL |
| 2 mM | 1.31 mL | 6.57 mL | 13.14 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.63 mL |
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Product Datasheets for AZD 7648
References for AZD 7648
References are publications that support the biological activity of the product.
Fok et al (2019) AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity. Nat.Commun. 10 5065 PMID: 31699977
Nakamura et al (2021) Inhibition of DNA-PK with AZD7648 sensitizes tumor cells to radiotherapy and induces type I IFN-dependent durable tumor control. Clin.Cancer Res. 27 4353 PMID: 34011558
Goldberg et al (2020) The discovery of 7-methyl-2-[(7-methyl[1,2,4]triazolo[1,5- a]pyridin-6-yl)amino]-9-(tetrahydro-2 H-pyran-4-yl)-7,9-dihydro-8 H-purin-8-one (AZD7648), a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor. J.Med.Chem. 63 3461 PMID: 31851518
Wimberger et al (2023) Simultaneous inhibition of DNA-PK and Polθ improves integration efficiency and precision of genome editing. Nat.Commun. 14 4761 PMID: 37580318
If you know of a relevant reference for AZD 7648, please let us know.
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Citations for AZD 7648
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Cell Cycle and DNA Damage Research Product Guide
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