DNA-PK抑制剂III是一种细胞可渗透的芳基吗啉类化合物，是一种有效的、选择性的DNA-PK (IC|50|= 120 nM)和PI 3-激酶催化亚单位p110β (IC|50|= 135 nM)的ATP竞争性抑制剂。抑制DNA-PK介导的细胞DNA DSB(双链断裂)修复(EC|50|= 68μM)并增强DSB诱导的抗肿瘤活性|体外|，同时在不存在DSB的情况下不显示细胞毒性作用(高达50μM)。也仅在高得多的浓度下抑制PI 3K p110α、p110γ和p110δ(IC50分别为1.4 μM, 880 nM, and 1.0 μM),并且对包括Cdk2、Src、PKA、PKC、Chk1、CK1、ATM和FKBP12在内的其他几种激酶没有作用，甚至在高达100 μM的浓度下也是如此。 DNA-PK Inhibitor III is a cell-permeable aryl-morpholino compound that is potent, selective, and an ATP-competitive inhibitor of DNA-PK (IC|50|= 120 nM) and PI 3-Kinase catalytic subunit p110β (IC|50|= 135 nM). Inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC|50|= 68 μM) and enhances DSB-induced antitumor activity|in vitro|, while exhibiting no cytotoxic effects (up to 50 μM) in the absence of DSBs. Also inhibits PI 3K p110α, p110γ, and p110δ only at much higher concentrations (IC50= 1.4 μM, 880 nM, and 1.0 μM, respectively) and exhibits no effect against a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 μM.
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DNA-PK Inhibitor III
Dangerous GoodsCAS number：404009-40-1 molecular formula：C12H15NO3
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | Q27077089 | 1-(2-HYDROXY-4-MORPHOLINOPHENYL)ETHANONE | 1-[2-hydroxy-4-(morpholin-4-yl)phenyl]ethan-1-one | A914137 | BCP08943 | BDBM50398036 | s5314 | DTXSID40431950 | WS-01628 | CCG-206744 | BDBM50306886 | DNA-PK Inhibitor III - CAS 404009-40-1 | DTXSID4 | ||
| CAS number | 404009-40-1 | molecular formula | C12H15NO3 |
| molecular weight | 221.26 g/mol | Exact mass | - |
| PSA | 49.800 Ų | logp | 1.800 |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P304+P340: 如误吸入：将人转移
WGK Germany：
3
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