| 产品描述： | AZD7648是DNA-PK的有效抑制剂，IC50为0.6 nM，其选择性比对所检测激酶库中其他的396种激酶高100倍以上 |
| 靶点： |
DNA-PK(Cell-free assay):0.6 nM;DNA-PK |
| 体外研究： |
AZD7648 inhibits IR-induced DNA-PK S2056 auto phosphoryalation with an IC50 = 92 nM in A549 non-small cell lung cancer (NSCLC) cells. In A549 cells, AZD7648 (≥1 µM) in combination with 2Gy IR for 48 hours leads to a significant accumulation of cells arrested in the G2/M of the cell cycle, a 4-fold increase in micronuclei formation, and 3-fold induction of γH2AX, pATM S1981 and 53BP1 foci formation compared with IR alone |
| 体内研究： |
AZD7648 is a potent and highly selective DNA-PK inhibitor, with good crystalline solubility, permeability and metabolic stability, good bioavailability and predictable pharmacokinetics in preclinical species, and potent knockdown of pRPA and regressions in murine xenograft models when combining with olaparib or radiation |
| 细胞实验： |
Cell lines: HeLa cells Concentrations: 10 μM Incubation Time: 1 h Method: Cells were treated with indicated concentration of drug for 1 h. |
| 动物实验： |
Animal Models: SCID mice Dosages: 4-100 mg/kg Administration: p.o. |
| 参考文献： |
1. Frederick W. Goldberg, et al. Abstract DDT01-02: Discovery and first structural disclosure of AZD7648: A potent and selective DNA-PK inhibitor. AACR Cancer Res. 2019, 79(13 Suppl):Abstract nr DDT01-02. 2. Jacqueline H. Fok, et al. Abstract 3512: AZD7648, a potent and selective inhibitor of DNA-PK, potentiates the activity of ionising radiation and doxorubicin in vitro and causes tumour regression in xenograft models. AACR Cancer Res. 2019, 79(13 Suppl):Abstract nr 3512. 3. Zhang H, et al. TDP1-independent pathways in the process and repair of TOP1-induced DNA damage. Nat Commun. 2022 Jul 22;13(1):4240. 4. Fok JHL, et al. TDP1-independent pathways in the process and repair of TOP1-induced DNA damage. Nat Commun. 2019 Nov 7;10(1):5065. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-20°C |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.629 ml |
13.144 ml |
26.288 ml |
| 5 mM |
0.526 ml |
2.629 ml |
5.258 ml |
| 10 mM |
0.263 ml |
1.314 ml |
2.629 ml |
| 50 mM |
0.053 ml |
0.263 ml |
0.526 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京