8-(4-氨基苯基)-2-(4-吗啉基)-4H-1-苯并吡喃-4-酮
| 中文名称 | 8-(4-氨基苯基)-2-(4-吗啉基)-4H-1-苯并吡喃-4-酮 |
|---|---|
| 中文同义词 | 8-(4-氨基苯基)-2-(4-吗啉基)-4H-1-苯并吡喃-4-酮;化合物 T16528 |
| 英文名称 | PI 828 |
| 英文同义词 | PI 828;2-(4-Morpholinyl)-8-(4-aminopheny)l-4H-1-benzopyran-4-one;8-(4-Aminophenyl)-2-(4-morpholinyl)-4H-1-benzopyran-4-one;8-(4-aminophenyl)-2-morpholin-4-ylchromen-4-one;LY 294002, 4-NH - CAS 942289-87-4 - Calbiochem;LY 294002, 4′-NH2;PI 828,PI828;4H-1-Benzopyran-4-one, 8-(4-aminophenyl)-2-(4-morpholinyl)- |
| CAS号 | 942289-87-4 |
| 分子式 | C19H18N2O3 |
| 分子量 | 322.36 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 942289-87-4.mol |
| 结构式 |  |
8-(4-氨基苯基)-2-(4-吗啉基)-4H-1-苯并吡喃-4-酮 性质
| 沸点 | 534.2±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.316±0.06 g/cm3(Predicted) |
| 储存条件 | Store at +4°C |
| 溶解度 | DMF：25mg/mL； DMSO：25mg/mL；乙醇：微溶 |
| 酸度系数(pKa) | 4.14±0.10(Predicted) |
| 形态 | 类白色固体 |
PI-828 是一种双重 PI3K 和 casein kinase 2 (CK2) 抑制剂，抑制 p110α，CK2 和 CK2α2，IC50 分别为 173 nM，149 nM 和 1127 nM。
|
p110α 173 nM (IC 50 ) |
CK2 149 nM (IC 50 ) |
CK2α2 1.127 μM (IC 50 ) |
PI-828 (0.01-100 μM) exhibits cytotoxic effect on the 4T1 breast cancer cells and 4306 ovarian cancer cells.
PI-828 (0.78-3.12 µM; 48 hours) decreases caspase 3 activation; higher concentrations of PI-828 (6.25-12.5 μM) alone causes apoptosis.
Cell Viability Assay
| Cell Line: | 4T1 breast cancer cells and 4306 ovarian cancer cells |
| Concentration: | 0.01, 0.1, 1, 10 and 100 μM |
| Incubation Time: | |
| Result: | Exhibited cytotoxic effect. |
Apoptosis Analysis
| Cell Line: | Human embryonic carcinoma NCCIT cells |
| Concentration: | 0.78, 1.56, 3.12, 6.25, 12.5 μM |
| Incubation Time: | 48 hours |
| Result: | Concentrations of ranging from 0.78 to 3.12 µM decreased caspase 3 activation; higher concentrations caused apoptosis. |