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,327033-36-3,结构式](https://www.chemicalbook.com/CAS/20150408/GIF/327033-36-3.gif)
- CAS号:327033-36-3
- 英文名:SMI-4a
- 中文名:5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
- CBNumber:CB12650480
- 分子式:C11H6F3NO2S
- 分子量:273.23
- MOL File:327033-36-3.mol
- 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 in DMSO
- 形态 :White to off-white solid.
- 酸度系数(pKa) :7.26±0.20(Predicted)
5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮性质、用途与生产工艺
- 生物活性 TCS-PIM-1-4a (SMI-4a) 是一种泛-Pim 激酶抑制剂，可通过激活 AMPK 来阻断 mTORC1 的活性。TCS-PIM-1-4a 可杀死多种髓样和淋巴样细胞系 (IC50 值为 0.8 μM 至 40 μM)。
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靶点
Pim
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体外研究
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. -
体内研究
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.
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