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说明： Potent and selective DNA-PK inhibitor; enhances CRISPR-mediated HDR efficiency
化学名： 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
纯度： ≥98% (HPLC)
生物活性 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.
技术数据 for AZD 7648
| 分子量 | 380.41 |
| 公式 | C18H20N8O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for AZD 7648
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 7.61 | 20 |
制备储备液 for AZD 7648
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for AZD 7648
参考文献 for AZD 7648
参考文献是支持产品生物活性的出版物。
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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关键词: AZD 7648, AZD 7648 supplier, AZD7648, potent, selective, DNA-dependent, protein, kinases, inhibitors, inhibits, DNA-PK, orally, bioavailable, HDR, homology-directed, repair, CRISPR, cas9, Protein, Kinase, Reagents, 7825, Tocris Bioscience
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该领域的文献
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
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- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.