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TCS PIM-1 1
目录号: PC10090 纯度: ≥98%
CAS No. :491871-58-0
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中文名称
TCS PIM-1 1
中文别名
3-氰基-4-苯基-6-(3-溴-6-羟基苯基)-2(1H)-吡啶酮;TCS PIM-1 1 抑制剂
英文名称
TCS PIM-1 1
英文别名
TCS PIM-1 1;6-(5-Bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydro-3-pyridine carbonitrile;SC 204330;TCS PIM 1-1;6-(5-Bromo-2-hydroxyphenyl)-1,2-dihydro-2-oxo-4-phenyl-3-pyridinecarbonitrile;6-(5-bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydropyridine-3-carbonitrile;3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone;C18H11BrN2O2;6-(5-bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1H-pyridine-3-carbonitrile;2obj;PIM1i;pyridone-based compound, 1;BDBM26673;AOB4940;HMS3229J17;HMS3742G19;BCP15861;4091AH;Pim1-IN-1 (TCS PIM-1 1)
Cas No.
491871-58-0
分子式
C18H11BrN2O2
分子量
367.20
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM).

性状

Solid

IC50 & Target[1][2]

PIM1

50 nM (IC50)

体外研究(In Vitro)

TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked 体外研究 inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 100 mg/mL (272.33 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7233 mL 13.6166 mL 27.2331 mL
5 mM 0.5447 mL 2.7233 mL 5.4466 mL
10 mM 0.2723 mL 1.3617 mL 2.7233 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:
  • 1.

    TCS PIM-1 1 is dissolved in 0.5% DMSO.

搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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