AZD 7648

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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

• Wimberger Simultaneous inhibition of DNA-PK and Polθ improves integration efficiency and precision of genome editing. Nat.Commun. 2023 PMID: 37580318
• Nakamura Inhibition of DNA-PK with AZD7648 sensitizes tumor cells to radiotherapy and induces type I IFN-dependent durable tumor control. Clin.Cancer Res. 2021 PMID: 34011558
• Goldberg 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. 2020 PMID: 31851518
• Fok AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity. Nat.Commun. 2019 PMID: 31699977