1309444-75-4
| 中文名称 | 1309444-75-4 |
|---|---|
| 中文同义词 | 化合物 T11739;化合物 K145;K145 ,E1123 |
| 英文名称 | K145 |
| 英文同义词 | K145;3-(2-Aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione;2,4-Thiazolidinedione, 3-(2-aminoethyl)-5-[3-(4-butoxyphenyl)propylidene]-;K145 ，K145 HCl salt;K145,K-145;Sphingosine Kinase-2 Inhibitor, K145;K145 ，E1123 |
| CAS号 | 1309444-75-4 |
| 分子式 | C18H24N2O3S |
| 分子量 | 348.46 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1309444-75-4.mol |
| 结构式 |  |
1309444-75-4 性质
| 沸点 | 501.017±60.00 °C(Press: 760.00 Torr)(predicted) |
|---|---|
| 密度 | 1.238±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 8.314±0.10(predicted) |
| 颜色 | off-white |
IC50: 4.3 µM (SphK2)
Ki: 6.4 µM (SphK2)
K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner.
K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells.
K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt.
Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels.
Cell Viability Assay
| Cell Line: | U937 cells |
| Concentration: | 0 µM, 4 µM, 6 µM, 8 µM, 10 µM |
| Incubation Time: | 24 hours, 48 hours, 72 hours |
| Result: | Significantly inhibited the growth of U937 cells in a concentration-dependent manner. |
Apoptosis Analysis
| Cell Line: | U937 cells |
| Concentration: | 10 µM |
| Incubation Time: | 24 hours |
| Result: | Significantly induced apoptosis in U937 cells. |
Western Blot Analysis
| Cell Line: | U937 cells |
| Concentration: | 4 µM, 8 µM |
| Incubation Time: | 3 hours |
| Result: | Phosphorylated ERK and Akt were decreased. |
K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice.
| Animal Model: | BALB/c-nu mice injected with U937 cells |
| Dosage: | 50 mg/kg |
| Administration: | Oral gavage; daily; for 15 days |
| Result: | Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed. |
安全信息
| WGK Germany | WGK 3 |
|---|---|
| 存储类别 | 11 - 可燃固体 |