中文名称: TrxR inhibitor D9
英文名称: TrxR inhibitor D9
CAS No: 1527513-89-8
分子式: C25H20AuOPS
分子量: 596.43
T10735 TrxR inhibitor D9 (psaitong)
包装规格:
1mg in glass bottle
产品描述:

基本信息

产品编号:T10735

产品名称:TrxR inhibitor D9

CAS:

1527513-89-8

 

储存条件

粉末

-20℃

四年

分子式:

C25H20AuOPS

溶于液体

-80℃

两年

分子量

596.43

 

 

化学名: 

 

 

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。

 

生物活性

产品描述

一种有效和选择性的硫氧还蛋白还原酶 (TrxR) 的抑制剂,EC50 值为 2.8nM。

靶点/IC50

EC50: 2.8nM (TrxR)

体外研究

TrxR inhibitor D9 (0.1-1μM; 72h) inhibits the cell proliferation with IC50s of 0.03 and 0.1μM for MCF-7 and HT-29 cells,respectively.TrxR inhibitor D9 (72h) completely inhibits all cancer cells (A549, KB, MDA MB-231, HeLa, MCF-7 and HT-29) viability at the concentration of 0.60μM, and the IC50s of all cancer cells could be as low as 0.55μM,and dose not significantly affects normal cells viability.TrxR inhibitor D9 (0.8μM;4 and 8h) induces HT-29 cells necrosis/apoptosis.TrxR inhibitor D9 (2-20nM; 1-60 s) inhibits TrxR activity in a concentration-dependent manner.TrxR inhibitor D9 (1-1000nM) does not significantly inhibits the catalytic activity of glutathione reductase (GR) even when the concentration increases to more than 1000nM.TrxR inhibitor D9 (0.4μM) could effectively avoid the ligand exchange with albumin.
Cell Proliferation Assay

Cell Line:

MCF-7 and HT-29 cells

Concentration:

0.1, 0.5, 1μM

Incubation Time:

72 hours

Result:

Killed 70% MCF-7 cells and 50% HT-29 cells with the concentration as low as 0.1μM.

Apoptosis Analysis

Cell Line:

MCF-7 cells

Concentration:

0.8μM

Incubation Time:

4 and 8 hours

Result:

Led to more than 50% necrosis/apoptosis of cells compared to control after 4h of treatment.Induced all cells necrosis/apoptosis after 8h of incubation.

体内研究

TrxR inhibitor D9 (5mg/kg; i.v. once every 2 d for 15 d) effectively inhibits the growth of tumors in mice.

Animal Model:

BALB/c nude mice (17-18g) bearing a MCF-7 tumor

Dosage:

5mg/kg

Administration:

I.v. once every 2 days for 15 days

Result:

Inhibited tumor growth with IR (inhibition ratio) of 91.5% and was well tolerated.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
参考文献 & 客户发表文献

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:
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摩尔浓度计算公式

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用本工具协助配置特定浓度的溶液,使用的计算公式为:
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    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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