SBI-0206965 是一种高度选择性自吞噬激酶ULK1抑制剂,IC50为108 nM,选择性比作用于ULK2高7倍。SBI-0206965 可抑制人胶质母细胞瘤和肺癌细胞中的自噬而增强凋亡。 Information SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells. Targets ULK1 (Cell-free assay); ULK2 (Cell-free assay) 108 nM; 711 nM In vitro In HEK293T transfected with WT or KI Myc-tagged ULK1 and WT Vps34, SBI-0206965 inhibits Ser249 phosphorylation of overexpressed Vps34 and Beclin1 Ser15 phosphorylation. SBI-0206965 suppresses autophagy induced by mTOR inhibition in A549 cells, and prevents ULK1-dependent cell survival in WT MEFs. In addition, SBI-0206965 also synergizes with mTOR inhibition to induce cancer cell death.
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SBI-0206965
Dangerous GoodsCAS number:1884220-36-3 molecular formula:C21H21BrN4O5
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | SBI-0206965 | 1884220-36-3 | Sbi0206965 | 2-((5-Bromo-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)oxy)-N-methylbenzamide | 2-[5-bromo-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]oxy-N-methylbenzamide | 2-({5-bromo-2-[(3,4,5-trimethoxyphenyl)amino]pyrimi | ||
| CAS number | 1884220-36-3 | molecular formula | C21H21BrN4O5 |
| molecular weight | 489.32 g/mol | Exact mass | - |
| PSA | 104.000 Ų | logp | 4.128 |
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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
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