中文名 | TCS PIM-1 1 |
英文名 | TCS PIM-1 1 |
别名 | 化合物TCS PIM-1 1 PIM-1激酶抑制剂(TCS PIM-1 1) 3-氰基-4-苯基-6-(3-溴-6-羟基苯基)-2(1H)-吡啶酮 6-(5-溴-2-羟基苯)-2-氧代-4-苯基-1,2-二氢吡啶-3-腈 |
英文别名 | CS-1482 TCS PIM-1 SC 204330 TCS PIM-1 1 TCS PIM 1-1 3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone 6-(5-Bromo-2-hydroxyphenyl)-1,2-dihydro-2-oxo-4-phenyl-3-pyridinecarbonitrile |
CAS | 491871-58-0 |
化学式 | C18H11BrN2O2 |
分子量 | 367.2 |
密度 | 1.63±0.1 g/cm3(Predicted) |
沸点 | 592.6±50.0 °C(Predicted) |
溶解度 | DMSO: ≥ 52 mg/mL |
酸度系数 | 6.93±0.10(Predicted) |
存储条件 | Store at +4°C |
体外研究 | TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.723 ml | 13.617 ml | 27.233 ml |
5 mM | 0.545 ml | 2.723 ml | 5.447 ml |
10 mM | 0.272 ml | 1.362 ml | 2.723 ml |
5 mM | 0.054 ml | 0.272 ml | 0.545 ml |
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