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327033-36-3

中文名称 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
英文名称 SMI-4a
CAS 327033-36-3
分子式 C11H6F3NO2S
分子量 273.23
MOL 文件 327033-36-3.mol
327033-36-3 结构式 327033-36-3 结构式

基本信息

中文别名
5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
英文别名
SMI-4q
CS-627
SMI-4a ≥95%(NMR)
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

物理化学性质

熔点181-183℃ (methanol )
储存条件Sealed in dry,2-8°C
溶解度≥ 9.4mg/mL in DMSO
形态白色至类白色固体

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H315-H319-H335
危险类别码36-43
安全说明26-36/37

常见问题列表

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)。
靶点

Pim

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.
"327033-36-3" 相关产品信息
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