中文名称: TCS-PIM-1-4a
英文名称: TCS-PIM-1-4a
CAS No: 327033-36-3
分子式: C11H6F3NO2S
分子量: 273.23
T11032 TCS-PIM-1-4a ≥98% (psaitong)
包装规格:
10mg 50mg 100mg in glass bottle
溶解性:
溶于DMSO(≥100mg/ml)
产品描述:

基本信息

产品编号:

T11032

产品名称:

TCS-PIM-1-4a

CAS:

327033-36-3

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C11H6F3NO2S

溶于液体

-80℃

6个月

分子量:

273.23

-20℃

1个月

化学名: 

(5E)-5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

3.6599mL

18.2996mL

36.5992mL

5mM

0.7320mL

3.6599mL

7.3198mL

10mM

0.3660mL

1.8300mL

3.6599mL

 

生物活性

产品描述

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0.8μM至40μM)。

靶点

Pim

 

体外研究

TCS-PIM-1-4a (10μM;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 (5μM;6 hours;6812/2 cells and Jurkat cells) induces cell death by the induction of apoptosis.TCS-PIM-1-4a (5μM;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:

10μM

Incubation Time:

24 hours,48 hours

Result:

Induced cell-cycle arrest.

Apoptosis Analysis

Cell Line:

6812/2 cells and Jurkat cells

Concentration:

5μM

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:

10μM

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;60mg/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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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