5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
![5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮 结构式](https://img.chemicalbook.com/CAS/20150408/GIF/327033-36-3.gif)
5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮 性质
| 熔点 | 181-183℃ (methanol ) |
|---|---|
| 密度 | 1.530±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | ≥ 9.4mg/mL，溶于 DMSO |
| 形态 | 白色至类白色固体。 |
| 酸度系数(pKa) | 7.26±0.20(Predicted) |
5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮 用途与合成方法
Pim
TCS-PIM-1-4a (10 μM; 24-48 hours; 6812/2 cells and Jurkat cells) treatment increases the population of cells in the G1 phase from 44.3% to 68.4% and from 56.2% to 67.1% in 6812/2 and Jurkat, respectively. S-phase cells are decreased in 6812/2, whereas only small changes are seen in Jurkat cells consistent with the lesser G1 block.
TCS-PIM-1-4a (5 μM; 6 hours; 6812/2 cells and Jurkat cells) induces cell death by the induction of apoptosis.
TCS-PIM-1-4a (5 μM; 4-8 hours; 6812/2 cells and Jurkat cells) prevents the increase in 4E-BP1 protein levels and inhibits mTOR-directed phosphorylation on Thr37/46.
Cell Cycle Analysis
| Cell Line: | 6812/2 cells and Jurkat cells |
| Concentration: | 10 μM |
| Incubation Time: | 24 hours, 48 hours |
| Result: | Induced cell-cycle arrest. |
Apoptosis Analysis
| Cell Line: | 6812/2 cells and Jurkat cells |
| Concentration: | 5 μM |
| Incubation Time: | 6 hours |
| Result: | Led to an increase in the number of the cells positive for annexin V and negative for PI from 8.25% in the control to 21.85%. |
Western Blot Analysis
| Cell Line: | 6812/2 cells and Jurkat cells |
| Concentration: | 10 μM |
| Incubation Time: | 4 hours, 8 hours |
| Result: | Prevented the increase in 4E-BP1 protein levels and inhibited mTOR-directed phosphorylation on Thr37/46. |
TCS-PIM-1-4a (SMI-4a; 60 mg/kg; oral gavage; twice daily; for 21 days; nu/nu nude mice) treatment causes a significant delay in the tumor growth without any change in the weight, blood counts, or chemistries.
| Animal Model: | 18 Nu/nu nude mice with 6812/2 murine pre–T-LBL cells |
| Dosage: | 60 mg/kg |
| Administration: | Oral gavage; twice daily; for 21 days |
| Result: | Caused a significant delay in the tumor growth. |
