5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
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- CAS号:
- 327033-36-3
- 英文名:
- SMI-4a
- 英文别名:
- SMI-4q;CS-627;SMI-4a ≥95%(NMR);2 Kinase Inhibitor V;5-(3-(Trifluoromethyl)benzylidene)thiazolidine-2,4-dione;5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione;2,4-Thiazolidinedione, 5-[[3-(trifluoromethyl)phenyl]methylene]-;SMI-4a5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione
- 中文名:
- 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
- 中文别名:
- 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
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5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮化学性质
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熔点:
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181-183℃ (methanol )
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密度:
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1.530±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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≥ 9.4mg/mL in DMSO
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形态:
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White to off-white solid.
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酸度系数(pKa):
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7.26±0.20(Predicted)
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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
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)。
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
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Cell Line:
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6812/2 cells and Jurkat cells
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Concentration:
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10 μM
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Incubation Time:
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24 hours, 48 hours
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Result:
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Induced cell-cycle arrest.
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Apoptosis Analysis
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Cell Line:
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6812/2 cells and Jurkat cells
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Concentration:
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5 μM
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Incubation Time:
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6 hours
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Result:
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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%.
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Western Blot Analysis
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Cell Line:
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6812/2 cells and Jurkat cells
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Concentration:
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10 μM
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Incubation Time:
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4 hours, 8 hours
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Result:
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Prevented the increase in 4E-BP1 protein levels and inhibited mTOR-directed phosphorylation on Thr37/46.
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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.
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Animal Model:
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18 Nu/nu nude mice with 6812/2 murine pre–T-LBL cells
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Dosage:
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60 mg/kg
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Administration:
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Oral gavage; twice daily; for 21 days
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Result:
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Caused a significant delay in the tumor growth.
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5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
上下游产品信息
上游原料
下游产品
5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
生产厂家
327033-36-3, 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮 相关搜索:
- 药靶配体
- 对照品
- 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
- 327033-36-3
- 5-(3-(Trifluoromethyl)benzylidene)thiazolidine-2,4-dione
- 2 Kinase Inhibitor V
- 2,4-Thiazolidinedione, 5-[[3-(trifluoromethyl)phenyl]methylene]-
- SMI-4a5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione
- SMI-4q
- CS-627
- SMI-4a ≥95%(NMR)
- 5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione