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AZD-7648 {[allProObj[0].p_purity_real_show]}

货号:A1175994 Ambeed 开学季,买赠积分,赢豪礼

AZD7648 is a highly potent and selective DNA-PK inhibitor with IC50 value of 92nM.

AZD-7648 化学结构 CAS号:2230820-11-6
AZD-7648 化学结构
CAS号:2230820-11-6
AZD-7648 3D分子结构
CAS号:2230820-11-6
AZD-7648 化学结构 CAS号:2230820-11-6
AZD-7648 3D分子结构 CAS号:2230820-11-6
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AZD-7648 纯度/质量文件 产品仅供科研

货号:A1175994 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 DNA-PK 其他靶点 纯度
PI-103 ++

DNA-PK, IC50: 23 nM

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CC-115 +++

DNA-PK, IC50: 0.013 μM

mTOR {[allProObj[0].p_purity_real_show]}
Samotolisib {[allProObj[0].p_purity_real_show]}
NU 7026 +

DNA-PK, IC50: 0.23 μM

PI3K {[allProObj[0].p_purity_real_show]}
PIK-75 HCl ++++

DNA-PK, IC50: 2 nM

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PP121 +

DNA-PK, IC50: 60 nM

VEGFR,PDGFR {[allProObj[0].p_purity_real_show]}
KU-0060648 ++++

DNA-PK, IC50: 5 nM

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KU-57788 +++

DNA-PK, IC50: 14 nM

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LTURM34 ++

DNA-PK, IC50: 0.034 μM

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SF2523 +++

DNA-PK, IC50: 9 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

AZD-7648 生物活性

描述 DNA-dependent kinase (DNA-PK) is a nuclear serine/threonine protein kinase complex that is a key component of the non-homologous end joining (NHEJ) process. DNA-PK plays an important role in the cellular response to DNA damage through the detection and repair of DNA double strand breaks (DSB). AZD7648 is a potent inhibitor of DNA-PK (0.6 nM in biochemical assay, 89 nM in A549 cells). AZD7648 inhibits ionising radiation (IR)-induced DNA-PK S2056 auto phosphoryalation with an IC50 of 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 led 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. In vivo the combination of AZD7648 with IR (5x 2Gy) induced tumour regression in H1299 and A549 NSCLC xenografts in a dose-dependent manner (84 and 11% regression respectively). Similarly, liposomal doxorubicin (2.5 mg/kg weekly) in combination with AZD7648 (37.5 mg/kg bid) induced tumour regressions in the BT474c ER+ breast cancer xenograft model and in a TNBC PDX model (63% and 33% regression respectively).

AZD-7648 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.29mL

5.26mL

2.63mL

AZD-7648 技术信息

CAS号2230820-11-6
分子式C18H20N8O2
分子量 380.404
别名
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 7 mg/mL(18.4 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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