942289-87-4
中文名稱
8-(4-氨基苯基)-2-(4-嗎啉基)-4H-1-苯并吡喃-4-酮
英文名稱
PI 828
CAS
942289-87-4
分子式
C19H18N2O3
分子量
322.36
MOL 文件
942289-87-4.mol
更新日期
2024/12/16 15:20:12
942289-87-4 結構式
基本信息
中文別名
8-(4-氨基苯基)-2-(4-嗎啉基)-4H-1-苯并吡喃-4-酮 英文別名
PI 828LY 294002, 4′-NH2
LY 294002, 4-NH - CAS 942289-87-4 - Calbiochem
8-(4-aminophenyl)-2-morpholin-4-ylchromen-4-one
8-(4-Aminophenyl)-2-(4-morpholinyl)-4H-1-benzopyran-4-one
2-(4-Morpholinyl)-8-(4-aminopheny)l-4H-1-benzopyran-4-one
物理化學性質
沸點534.2±50.0 °C(Predicted)
密度1.316±0.06 g/cm3(Predicted)
儲存條件Store at +4°C
溶解度DMF: 25 mg/ml; DMSO: 25 mg/ml; Ethanol: slightly soluble
酸度系數(shù)(pKa)4.14±0.10(Predicted)
形態(tài)類白色固體
顏色White to yellow
常見問題列表
生物活性
PI-828 是一種雙重 PI3K 和 casein kinase 2 (CK2) 抑制劑，抑制 p110α，CK2 和 CK2α2，IC50 分別為 173 nM，149 nM 和 1127 nM。靶點
|
p110α 173 nM (IC 50 ) |
CK2 149 nM (IC 50 ) |
CK2α2 1.127 μM (IC 50 ) |
體外研究
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. |