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Submit ReviewAZD 7762 hydrochloride
说明： Potent and selective ATP-competitive inhibitor of Chk1 and Chk2; also enhances CRISPR-Cpf1-mediated genome editing
化学名： 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-thiophenecarboxamide hydrochloride
纯度： ≥98% (HPLC)
生物活性 for AZD 7762 hydrochloride
AZD 7762 hydrochloride is a potent and selective ATP-competitive inhibitor of Chk1 and Chk2 (IC50 vales are 5 nM for both kinases); displays at least >10 fold selectivity over a panel of 164 kinases. Potentiates cytotoxicity of DNA-damaging agents. Active in vivo. Also improves efficiency of CRISPR-Cpf1-mediated genome editing in hPSC lines (2.7-fold at 1 μM).
许可信息
Sold for research purposes under agreement from AstraZeneca
化合物库 for AZD 7762 hydrochloride
AZD 7762 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for AZD 7762 hydrochloride
| 分子量 | 398.88 |
| 公式 | C17H19FN4O2S.HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1246094-78-9 |
| PubChem ID | 56972142 |
| InChI Key | WFZBLOIXZRZEDG-YDALLXLXSA-N |
| Smiles | FC1=CC=CC(C2=CC(NC(N)=O)=C(C(N[C@@H]3CNCCC3)=O)S2)=C1.Cl |
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 7762 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 39.89 | 100 | |
| DMSO | 39.89 | 100 |
制备储备液 for AZD 7762 hydrochloride
以下数据基于产品分子量 398.88。 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 |
|---|---|---|---|
| 1 mM | 2.51 mL | 12.54 mL | 25.07 mL |
| 5 mM | 0.5 mL | 2.51 mL | 5.01 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.51 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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产品说明书 for AZD 7762 hydrochloride
参考文献 for AZD 7762 hydrochloride
参考文献是支持产品生物活性的出版物。
Zabludoff et al (2008) AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Mol. Cancer Ther. 7 2955 PMID: 18790776
Morgan et al (2010) Mechanism of radiosensitization by the Chk1/2 inhibitor AZD7762 involves abrogation of the G2 checkpoint and inhibition of homologous recombinational DNA repair. Cancer Res. 70 4972 PMID: 20501833
Ma et al (2018) Small molecules promote CRISPR-Cpf1-mediated genome editing in human pluripotent stem cells. Nat Commun. 9 1303 PMID: 29610531
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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.