中文名称:

CP466722

中文同义词:

ATM激酶抑制剂(CP-466722);1-(6,7-二甲氧基-4-喹唑啉基)-3-(2-吡啶基)-1H-1,2,4-三唑-5-胺;化合物CP466722

英文名称:

CP466722

英文同义词:

CP466722;1-(6,7-Dimethoxy-4-quinazolinyl)-3-(2-pyridinyl)-1H-1,2,4-triazol-5-amine;CP466722;CP 466722;CP-466722;CS-73;CP-466722, >98%;2-(6,7-dimethoxyquinazolin-4-yl)-5-(pyridin-2-yl)-2H-1,2,4-triazol-3-amine;1-(6,7-Dimethoxy-4-quinazolinyl)-3-(2-pyridinyl)-1H-1,2,4-triazol-5-amine CP 466722;2-(6,7-dimethoxyquinazolin-4-yl)-5-pyridin-2-yl-1,2,4-triazol-3-amine

CAS号:

1080622-86-1

分子式:

C17H15N7O2

分子量:

349.35

EINECS号:

808-414-0

相关类别:

DNA损伤;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors

Mol文件:

1080622-86-1.mol

沸点 

642.3±65.0 °C(Predicted)

密度 

1.48

储存条件 

Keep in dark place,Sealed in dry,2-8°C

溶解度 

DMSO: soluble0.5mg/mL, clear (warmed)

形态

powder

酸度系数(pKa)

0.00±0.19(Predicted)

颜色

white to beige

生物活性

CP-466722是一种有效的，可逆的ATM抑制剂，不影响ATR，且抑制PI3K或PIKK家族成员。

体外研究

In vitro, CP-466722 is identified as a potential inhibitor to decrease the activity of purified ATM kinase to phosphorylate GST-p53(1–101) substrate. In addition, CP-466722 also shows the inhibitory activities against abl and src kinases. In HeLa cells, CP-466722 at doses of 6μM, results in the inhibition in ATM-dependent phosphorylation by reversibly inhibiting ionizing radiation (IR)-induced ATM kinase activity. Besides, ATM-dependent p53 induction is also inhibited by CP-466722 in MCF-7 human breast cancer cells and primary and immortalized diploid human fibroblasts. In response to IR, CP-466722 increased proportion of cells with G2/M DNA content and reduces proportion of cells with G1-phase DNA content in HeLa cells. Transient exposure to CP-466722 for a period of 4 hours sensitizes HeLa cells to IR without affecting cell plating nor cell viability.

靶点

ATM 4.1 μM (IC 50 )

ATM 4.1 μM (IC 50 )

危险品标志 

Xn

危险类别码 

22

WGK Germany 

3