2. Apoptosis PI3K/Akt/mTOR
  3. Caspase mTOR
  4. N1,N11-Diethylnorspermine

N1, N11-Diethylnorspermine (DENSPM tetrahydrochloride) 是一种有效的抗癌剂。N1, N11-Diethylnorspermine 激活多胺分解代谢，减少 mTOR 蛋白。N1,N11-Diethylnorspermine 诱导线粒体释放细胞色素 c，导致 caspase 3 的激活。N1,N11-Diethylnorspermine 通过诱导亚精胺/精胺 N1-乙酰转移酶 (SSAT) 结合产生过氧化氢杀灭多形胶质母细胞瘤 (GBM) 。

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N1,N11-Diethylnorspermine Chemical Structure

N1,N11-Diethylnorspermine Chemical Structure

CAS No. : 121749-39-1

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N1,N11-Diethylnorspermine 的其他形式现货产品:

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N1,N11-Diethylnorspermine 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

N1,N11-Diethylnorspermine (DENSPM tetrahydrochloride) is a potent anticancer agent. N1,N11-Diethylnorspermine activates polyamine catabolism and downregulates mTOR protein. N1,N11-Diethylnorspermine induces the release of cytochrome c from mitochondria, resulting in activation of caspase 3. N1,N11-Diethylnorspermine tetrahydrochloride kills glioblastoma multiforme (GBM) through induction of SSAT (spermidine/spermine N1-acetyltransferase) coupled with H2O2 production[1][2][3][4][5][6].

IC50 & Target

Caspase 3

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
B16 IC50
> 40 μM
Compound: BENSpm
Cytotoxicity against mouse B16 cells assessed as induction of cell death incubated for 24 hrs by MTT assay
Cytotoxicity against mouse B16 cells assessed as induction of cell death incubated for 24 hrs by MTT assay
[PMID: 36399911]
Jurkat IC50
0.65 μM
Compound: DENSPM
inhibitory activity against growth of JURKAT cells after 144h.
inhibitory activity against growth of JURKAT cells after 144h.
[PMID: 9748365]
KB 3-1 IC50
> 40 μM
Compound: BENSpm
Cytotoxicity against human KB-3-1 cells assessed as induction of cell death incubated for 24 hrs by MTT assay
Cytotoxicity against human KB-3-1 cells assessed as induction of cell death incubated for 24 hrs by MTT assay
[PMID: 36399911]
L1210 IC50
> 100 μM
Compound: 3
In vitro inhibition of L1210 growth after 48 hours.
In vitro inhibition of L1210 growth after 48 hours.
[PMID: 7932575]
L1210 IC50
2 μM
Compound: DENSPM
Growth inhibition of L1210 cells was measured in the presence of nine different concentrations: 0,0.03,0.1,0.3,1,3,10,30, and 100 uM after 96 hours
Growth inhibition of L1210 cells was measured in the presence of nine different concentrations: 0,0.03,0.1,0.3,1,3,10,30, and 100 uM after 96 hours
[PMID: 10649978]
L1210 IC50
2 μM
Compound: 3
In vitro inhibition of L1210 growth after 96 hours.
In vitro inhibition of L1210 growth after 96 hours.
[PMID: 7932575]
L1210 IC50
20 μM
Compound: DENSPM
Growth inhibition of L1210 cells was measured in the presence of nine different concentrations: 0,0.03,0.1,0.3,1,3,10,30, and 100 uM after 48 hours
Growth inhibition of L1210 cells was measured in the presence of nine different concentrations: 0,0.03,0.1,0.3,1,3,10,30, and 100 uM after 48 hours
[PMID: 10649978]
MCF7 IC50
> 40 μM
Compound: BENSpm
Cytotoxicity against human MCF7 cells assessed as induction of cell death incubated for 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as induction of cell death incubated for 24 hrs by MTT assay
[PMID: 36399911]
体内研究
(In Vivo)

N1,N11-Diethylnorspermine (40 mg/kg，每天三次，连续两个周期，每个周期 6 天) 可以明显抑制 DU-145 细胞异种移植瘤小鼠的肿瘤生长[1]。
N1,N11-Diethylnorspermine (120-360 mg/kg，皮下注射，4 天) 可长期抑制 MALME-3M 黑色素瘤异种移植瘤的裸鼠的肿瘤生长并使其长期消退[5]。
N1,N11-Diethylnorspermine (12.5-50 mg/kg，静脉注射，5 天) 耐受性良好，不会在 CD 大鼠中引起任何体征[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

244.42

Formula

C13H32N4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

N1,N11-Diethylnorspermine 相关分类

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Keywords:

N1,N11-Diethylnorspermine121749-39-1CaspasemTORMammalian target of Rapamycinprostate cancerPC-3TSU-pr1DU-145JCA-1spermine analoguebreast cancerGBM cellglioblastoma multiformeInhibitorinhibitorinhibit

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