| 中文名称: | TCS-PIM-1-4a | ||||
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| 英文名称: | TCS-PIM-1-4a | ||||
| 别名: | TCS-PIM-1-4a SMI-4a | ||||
| CAS No: | 327033-36-3 | 分子式: | C11H6F3NO2S | 分子量: | 273.23 |
| CAS No: | 327033-36-3 | ||||
| 分子式: | C11H6F3NO2S | ||||
| 分子量: | 273.23 | ||||
基本信息
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产品编号： |
T11032 |
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产品名称： |
TCS-PIM-1-4a |
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CAS: |
327033-36-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
273.23 |
-20℃ |
1个月 |
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化学名： |
(5E)-5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
3.6599mL |
18.2996mL |
36.5992mL |
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5mM |
0.7320mL |
3.6599mL |
7.3198mL |
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10mM |
0.3660mL |
1.8300mL |
3.6599mL |
生物活性
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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)。 |
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靶点 |
Pim |
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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 |
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Cell Line: |
6812/2 cells and Jurkat cells |
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Concentration: |
10μM |
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Incubation Time: |
24 hours,48 hours |
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Result: |
Induced cell-cycle arrest. |
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Apoptosis Analysis |
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Cell Line: |
6812/2 cells and Jurkat cells |
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Concentration: |
5μM |
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Incubation Time: |
6 hours |
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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%. |
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Western Blot Analysis |
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Cell Line: |
6812/2 cells and Jurkat cells |
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Concentration: |
10μM |
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Incubation Time: |
4 hours,8 hours |
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Result: |
Prevented the increase in 4E-BP1 protein levels and inhibited mTOR-directed phosphorylation on Thr37/46. |
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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. |
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Animal Model: |
18 Nu/nu nude mice with 6812/2 murine pre–T-LBL cells |
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Dosage: |
60 mg/kg |
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Administration: |
Oral gavage;twice daily;for 21 days |
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Result: |
Caused a significant delay in the tumor growth. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
