1080622-86-1
中文名稱
CP466722
英文名稱
CP466722
CAS
1080622-86-1
分子式
C17H15N7O2
分子量
349.35
MOL 文件
1080622-86-1.mol
更新日期
2024/11/15 18:20:27
1080622-86-1 結(jié)構(gòu)式
基本信息
中文別名
化合物CP466722ATM激酶抑制劑(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
英文別名
CS-73CP466722
CP-466722, >98%
CP-466722
CP466722
CP466722 USP/EP/BP
CP466722 >=98% (HPLC)
CP466722
CP 466722
CP-466722
2-(6,7-dimethoxyquinazolin-4-yl)-5-pyridin-2-yl-1,2,4-triazol-3-amine
1-(6,7-Dimethoxy-4-quinazolinyl)-3-(2-pyridinyl)-1H-1,2,4-triazol-5-amine
1-(6,7-Dimethoxyquinazolin-4-yl)-3-(pyridin-2-yl)-1H-1,2,4-triazol-5-amine
所屬類別
生物化工：ATM/ATR 抑制劑物理化學(xué)性質(zhì)
沸點642.3±65.0 °C(Predicted)
密度1.48
儲存條件2-8°C
溶解度DMSO：可溶，0.5mg/mL，澄清（加熱）
酸度系數(shù)(pKa)0.00±0.19(Predicted)
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
CP-466722是一種有效的，可逆的ATM抑制劑，不影響ATR，且抑制PI3K或PIKK家族成員。體外研究
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.靶點
|
ATM 4.1 μM (IC 50 ) |