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- 详细信息
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
CB1954
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
21919-05-1
- 规格：
50mg/25mg/10mg/1mg/5mg
| 规格： | 50mg | 产品价格： | ￥2150.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥1430.0 |
| 规格： | 10mg | 产品价格： | ￥710.0 |
| 规格： | 1mg | 产品价格： | ￥214.0 |
| 规格： | 5mg | 产品价格： | ￥470.0 |
| 基本信息 | |
| CAS | No.21919-05-1 |
| 中文名称 | 5-(氮丙啶-1-基)-2,4-二NB甲酰胺 |
| 英文名称 | CB1954 |
| 别名 | CB1954;R18134nitrate;CB1954;CB-1954;Tretazicar; |
| 分子式 | C9H8N4O5 |
| 分子量 | 252.18 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Light yellow to yellow Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00869490 |
| SMILES | C1CN1C2=C(C=C(C(=C2)C(=O)N)[N+](=O)[O-])[N+](=O)[O-] |
| 靶点 | DNA Alkylator |
| 通路 | DNA Damage/DNA Repair |
| 背景说明 | 据报道，是一种抗癌前体化合物，酶促活化后可转化为有效的双功能烷化剂。 |
| 生物活性 | CB 1954 [5-(aziridin-1-yl)-2，4-dinitrobenzamide] is an antitumor prodrug that is activated in certain rat tumors via its 4-hydroxylamine derivative to a potent bifunctional alkylating agent. [1] The basis for the anti-tumor selectivity of CB 1954 is that it is a prodrug that is enzymatically activated to generate a difunctional agent， which can form DNA-DNA interstrand crosslinks. The bioactivation of CB 1954 in rat cells involves the aerobic reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NQO1 (DT-diaphorase). [2] |
| In Vitro | There is a very large(100-3000-fold)increase in CB 1954 cytotoxicity toward either NQO2-transfected rodent or nontransfected human tumor cell lines in the presence of NRH. [1] DNA cross-link formation in affected cells is a result of the bioactivation of the drug by the enzyme DT diaphorase(NAD(P)H dehydro-genase(quinone))in the Walker cells which reduces the 4-nitro group of Tretazicar. The product of this reaction is a difunctional alkylating agent，5-aziridin-1-yl-4-hydroxylamino-2-nitrobenzamide[4]. |
| 细胞实验 | NRH and reduced pyridinium derivatives that，like NRH，act as co-substrates for NQO2，produce a dramatic increase in the cytotoxicity of CB 1954 against human cell lines in vitro and its anti-tumor activity against certain human xenografts in vivo. [2] |
| 动物实验 | Tretazicar(CB 1954)(80 mg/kg; i.p. on days 2 and 9)results in a significant increase in survival[3]. |
| 数据来源文献 | [1]. Knox RJ，et al. Bioactivation of 5-(aziridin-1-yl)-2，4-dinitrobenzamide (CB 1954) by human NAD(P)H quinone oxidoreductase 2: a novel co-substrate-mediated antitumor prodrug therapy. Cancer Res. 2000 Aug 1;60(15):4179-86. [2]. Knox RJ， et al. CB 1954: from the Walker tumor to NQO2 and VDEPT. Curr Pharm Des. 2003;9(26):2091-104. [3]. Green NK， et al. Immune enhancement of nitroreductase-induced cytotoxicity: studies using a bicistronicadenovirus vector. Int J Cancer. 2003 Mar 10;104(1):104-12. [4]. Drabek D， et al. The expression of bacterial nitroreductase in transgenic mice results in specific cell killing by the prodrug CB1954. Gene Ther. 1997 Feb;4(2):93-100. |
| 单位 | 瓶 |
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IC4750 5-(氮丙啶-1-基)-2,4-二NB甲酰胺 抑制剂/拮抗剂/激动剂 索莱宝
￥214 - 2150
