1309444-75-4
1309444-75-4 用途与合成方法
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. |
