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Tretazicar
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tretazicar图片
CAS NO:21919-05-1
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
5-Aziridino-2,4-dinitrobenzamide
NSC 115829
CB1954
产品介绍
Tretazicar 是一种抗肿瘤前药,由 NAD(P)H 醌氧化还原酶 2 激活。它在酶促活化后生成细胞毒性双功能烷基剂,可以形成 DNA-DNA 链间交联。

产品描述

CB1954(Tretazicar), an anticancer prodrug, is activated by NAD(P)H quinone oxidoreductase 2. It is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent.

体外活性

In the NPC cell line CNE1, toxic CB1954 enhances cells killing. The overexpression of nitroreductase oxidored nitro domain-containing protein 1 (NOR1) reduce the 4 nitro group of CB1954, a potent cytotoxin, in order to convert the monofunctional alkylating agent CB1954 into a toxic form. In the HepG2 cell line, the NOR1 gene upregulates of Grb2 expression and activates of MAPK signal transduction leading to enhances CB1954 mediated cell cytotoxicity.

体内活性

The NTR/CB1954 system, which is in a dose-dependent effect, are used for specific ablation of cells in vivo. NTR-mediated cell killing by CB1954, which is activated cross-links, presumed through triggers the apoptosis cascade resulting in rapid cell death. Selective and potent cells killing by NTR-CB1954 does not require a functional p53.

细胞实验

HepG2 cells,which are maintained in RPMI 1640 supplemented with 10% fetal calf serum (FCS) in a humidified culture incubator at 37?C with 5% CO2 and 95% air, grow to ~80% confluence are washed with PBS and treated with r CB1954(4-10 μmol/L) for 48hours.

动物实验

RED 40 female mice,which express high levels of BLG-NTR transgene in the mammary gland and nontransgenic control mice on lactation day 6, were injected intraperitoneally (i.p.)with 50 mg/kg CB1954 dissolved in arachis oil containing 10% acetone.

Cas No.

21919-05-1

分子式

C9H8N4O5

分子量

252.186

别名

5-Aziridino-2,4-dinitrobenzamide;NSC 115829;CB1954

储存和溶解度

Ethanol:<1 mgml
H2O:<1 mgml
DMSO:47 mg/mL (186.4 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years