Tretazicar (Synonyms: CB 1954)

目录号: HY-13543 纯度: 99.50%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

Tretazicar (CB 1954) 是一种抗肿瘤前体，对 Walker 256 大鼠肿瘤细胞系具有很高的效力和选择性。Tretazicar 酶促活化后生成双功能试剂，该试剂可以形成 DNA-DNA 链间交联。大鼠细胞中的 Tretazicar 涉及通过酶 NAD(P)H：醌氧化还原酶1 (NQO1) 将其 4-硝基还原为 4-羟基胺。

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Tretazicar Chemical Structure

CAS No. : 21919-05-1

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规格	价格	是否有货
1 mg	￥224	In-stock
5 mg	￥480	In-stock
10 mg	￥720	In-stock
25 mg	￥1440	In-stock
50 mg	￥2160	In-stock
100 mg	￥3338	In-stock
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生物活性
纯度 & 产品资料
参考文献

生物活性

Tretazicar (CB 1954), an antitumor proagent, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1)^[1]^[2].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO-AA8	IC₅₀	560 μM Compound: 23	Growth inhibition of aerobic chinese hamster ovary fibroblast AA8 cell line using an exposure time of 18 hours Growth inhibition of aerobic chinese hamster ovary fibroblast AA8 cell line using an exposure time of 18 hours	[PMID: 1507207]
CHO-AA8	IC₅₀	563 μM Compound: 7	Aerobic cytotoxicity was assessed in a growth inhibition assay using log phase cultures of the chinese hamster ovary fibroblast line AA8 Aerobic cytotoxicity was assessed in a growth inhibition assay using log phase cultures of the chinese hamster ovary fibroblast line AA8	[PMID: 8035424]
EMT6	IC₅₀	0.098 μM Compound: 1, CB-1954	Antiproliferative activity against mouse EMT6 NTRpuro cells after 18 hrs Antiproliferative activity against mouse EMT6 NTRpuro cells after 18 hrs	[PMID: 17326614]
EMT6	IC₅₀	83 μM Compound: 1, CB-1954	Antiproliferative activity against mouse wild type EMT6 NTR-ve cells after 18 hrs Antiproliferative activity against mouse wild type EMT6 NTR-ve cells after 18 hrs	[PMID: 17326614]
PC-3	IC₅₀	1.792 nM Compound: CB1954	Cytotoxicity against human PC3 cells expressing Staphylococcus saprophyticus nitroreductase NtrB assessed as reduction in cell viability in presence of NADH as cofactor after 48 hrs by SRB assay Cytotoxicity against human PC3 cells expressing Staphylococcus saprophyticus nitroreductase NtrB assessed as reduction in cell viability in presence of NADH as cofactor after 48 hrs by SRB assay	[PMID: 31841727]
PC-3	IC₅₀	1.792 nM Compound: CB1954	Cytotoxicity against human PC3 cells assessed as reduction in cell viability measured after 48 hrs in presence of Staphylococcus saprophyticus nitroreductase and NADH by SRB assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability measured after 48 hrs in presence of Staphylococcus saprophyticus nitroreductase and NADH by SRB assay	[PMID: 30928710]
RT-112	IC₅₀	0.15 μM Compound: CB-1954	Cytotoxicity against NQO2 expressing human RT112 cells in presence of NRH cofactor by MTT assay Cytotoxicity against NQO2 expressing human RT112 cells in presence of NRH cofactor by MTT assay	[PMID: 17643990]
RT-112	IC₅₀	88.75 μM Compound: CB-1954	Cytotoxicity against NQO2 expressing human RT112 cells by MTT assay Cytotoxicity against NQO2 expressing human RT112 cells by MTT assay	[PMID: 17643990]
SK-OV-3	IC₅₀	> 1000 μM Compound: 5-aziridinyl-2,4-dinitrobenzamide	Antiproliferative activity against human SKOV3 cells infected with 100 pfu/cell retrovirus after 18 hrs Antiproliferative activity against human SKOV3 cells infected with 100 pfu/cell retrovirus after 18 hrs	[PMID: 16821793]
SK-OV-3	IC₅₀	> 1000 μM Compound: 1	Inhibitory activity against SKOV3 (human ovarian carcinoma) cell line without Escherichia coli nitroreductase combination after 18 hours drug exposure Inhibitory activity against SKOV3 (human ovarian carcinoma) cell line without Escherichia coli nitroreductase combination after 18 hours drug exposure	[PMID: 14584930]
SK-OV-3	IC₅₀	> 625 μM Compound: 1	Inhibitory activity against SKOV3 (human ovarian carcinoma) cell line without Escherichia coli nitroreductase combination after 18 hours drug exposure Inhibitory activity against SKOV3 (human ovarian carcinoma) cell line without Escherichia coli nitroreductase combination after 18 hours drug exposure	[PMID: 14584930]
SK-OV-3	IC₅₀	> 790 μM Compound: 5-aziridinyl-2,4-dinitrobenzamide	Antiproliferative activity against human SKOV3 cells after 18 hrs Antiproliferative activity against human SKOV3 cells after 18 hrs	[PMID: 16821793]
SK-OV-3	IC₅₀	2 μM Compound: 5-aziridinyl-2,4-dinitrobenzamide	Antiproliferative activity against NTR expressing human SKOV3 cells after 18 hrs Antiproliferative activity against NTR expressing human SKOV3 cells after 18 hrs	[PMID: 16821793]
SK-OV-3	IC₅₀	4.7 μM Compound: 5-aziridinyl-2,4-dinitrobenzamide	Antiproliferative activity against NTR expressing human SKOV3 cells infected with 100 pfu/cell retrovirus after 18 hrs Antiproliferative activity against NTR expressing human SKOV3 cells infected with 100 pfu/cell retrovirus after 18 hrs	[PMID: 16821793]
SK-OV-3	IC₅₀	4.7 μM Compound: 1	Inhibitory activity against SKOV3 (human ovarian carcinoma) cell line with Escherichia coli nitroreductase combination after 18 hours drug exposure Inhibitory activity against SKOV3 (human ovarian carcinoma) cell line with Escherichia coli nitroreductase combination after 18 hours drug exposure	[PMID: 14584930]
SK-OV-3	IC₅₀	52 μM Compound: 5-aziridinyl-2,4-dinitrobenzamide	Antiproliferative activity against NTR expressing human SKOV3 cells infected with 10 pfu/cell retrovirus after 18 hrs Antiproliferative activity against NTR expressing human SKOV3 cells infected with 10 pfu/cell retrovirus after 18 hrs	[PMID: 16821793]
SK-OV-3	IC₅₀	52 μM Compound: 1	Inhibitory activity against SKOV3 (human ovarian carcinoma) cell line infected at lower infection rate of 10 pfu/cell with Escherichia coli nitroreductase combination after 18 hours drug exposure Inhibitory activity against SKOV3 (human ovarian carcinoma) cell line infected at lower infection rate of 10 pfu/cell with Escherichia coli nitroreductase combination after 18 hours drug exposure	[PMID: 14584930]
SK-OV-3	IC₅₀	625 μM Compound: 5-aziridinyl-2,4-dinitrobenzamide	Antiproliferative activity against human SKOV3 cells infected with 10 pfu/cell retrovirus after 18 hrs Antiproliferative activity against human SKOV3 cells infected with 10 pfu/cell retrovirus after 18 hrs	[PMID: 16821793]
UV4	IC₅₀	11.7 μM Compound: 23	Growth inhibition of aerobic chinese hamster ovary fibroblast UV4 cells using an exposure time of 18 hours Growth inhibition of aerobic chinese hamster ovary fibroblast UV4 cells using an exposure time of 18 hours	[PMID: 1507207]
V79	IC₅₀	> 100 μM Compound: 5-aziridinyl-2,4-dinitrobenzamide	Antiproliferative activity against chinese hamster V79 cells after 1 hr Antiproliferative activity against chinese hamster V79 cells after 1 hr	[PMID: 16821793]
V79	IC₅₀	> 100 μM Compound: 1	Inhibitory activity against V79 (chinese hamster fibroblast) cell line without Escherichia coli nitroreductase combination after 1 hour drug exposure Inhibitory activity against V79 (chinese hamster fibroblast) cell line without Escherichia coli nitroreductase combination after 1 hour drug exposure	[PMID: 14584930]
V79	IC₅₀	0.036 μM Compound: 5-aziridinyl-2,4-dinitrobenzamide	Antiproliferative activity against NTR expressing chinese hamster V79 cells after 72 hrs Antiproliferative activity against NTR expressing chinese hamster V79 cells after 72 hrs	[PMID: 16821793]
V79	IC₅₀	0.036 μM Compound: 1	Inhibitory activity against V79 (chinese hamster fibroblast) cell line with Escherichia coli nitroreductase combination after 72 hours drug exposure Inhibitory activity against V79 (chinese hamster fibroblast) cell line with Escherichia coli nitroreductase combination after 72 hours drug exposure	[PMID: 14584930]
V79	IC₅₀	0.26 μM Compound: 1, CB-1954	Antiproliferative activity against chinese hamster V79 NTRpuro cells after 18 hrs Antiproliferative activity against chinese hamster V79 NTRpuro cells after 18 hrs	[PMID: 17326614]
V79	IC₅₀	0.31 μM Compound: 5-aziridinyl-2,4-dinitrobenzamide	Antiproliferative activity against NTR expressing chinese hamster V79 cells after 1 hr Antiproliferative activity against NTR expressing chinese hamster V79 cells after 1 hr	[PMID: 16821793]
V79	IC₅₀	0.31 μM Compound: 1	Inhibitory activity against V79 (chinese hamster fibroblast) cell line with Escherichia coli nitroreductase combination after 1 hour drug exposure Inhibitory activity against V79 (chinese hamster fibroblast) cell line with Escherichia coli nitroreductase combination after 1 hour drug exposure	[PMID: 14584930]
V79	IC₅₀	254 μM Compound: 5-aziridinyl-2,4-dinitrobenzamide	Antiproliferative activity against chinese hamster V79 cells after 72 hrs Antiproliferative activity against chinese hamster V79 cells after 72 hrs	[PMID: 16821793]
V79	IC₅₀	254 μM Compound: 1	Inhibitory activity against V79 (chinese hamster fibroblast) cell line without Escherichia coli nitroreductase combination after 72 hours drug exposure Inhibitory activity against V79 (chinese hamster fibroblast) cell line without Escherichia coli nitroreductase combination after 72 hours drug exposure	[PMID: 14584930]
V79	IC₅₀	374 μM Compound: 1, CB-1954	Antiproliferative activity against chinese hamster wild-type V79 NTR-ve cells after 18 hrs Antiproliferative activity against chinese hamster wild-type V79 NTR-ve cells after 18 hrs	[PMID: 17326614]
V79	IC₅₀	543 μM Compound: CB-1954	Cytotoxicity against chinese hamster V79 cells after 6 days by Alamar blue assay Cytotoxicity against chinese hamster V79 cells after 6 days by Alamar blue assay	[PMID: 20679506]
Vero	IC₅₀	> 250 μM Compound: CB-1954	Cytotoxicity against african green monkey Vero cells after 6 days by Alamar blue assay Cytotoxicity against african green monkey Vero cells after 6 days by Alamar blue assay	[PMID: 20679506]
Vero	IC₅₀	0.57 μM Compound: CB-1954	Antitrypanosomal activity against Trypanosoma cruzi clone Cl-Brener infected in african green monkey Vero cells assessed as growth inhibition after 3 days by luciferase reporter gene assay Antitrypanosomal activity against Trypanosoma cruzi clone Cl-Brener infected in african green monkey Vero cells assessed as growth inhibition after 3 days by luciferase reporter gene assay	[PMID: 20679506]
WiDr	IC₅₀	1.14 μM Compound: 1, CB-1954	Antiproliferative activity against human WiDr NTRneo cells after 18 hrs Antiproliferative activity against human WiDr NTRneo cells after 18 hrs	[PMID: 17326614]
WiDr	IC₅₀	54.5 μM Compound: 1, CB-1954	Antiproliferative activity against human wild type WiDr NTR-ve cells after 18 hrs Antiproliferative activity against human wild type WiDr NTR-ve cells after 18 hrs	[PMID: 17326614]

体外研究
(In Vitro)

Tretazicar (CB 1954) (0.1-1000 μM；3 天) 对逆转录病毒转导的 AB22 (AB22-nr) 细胞具有敏感性，IC₅₀ 为 3 μM^[3]。
受影响细胞中的 DNA 交联形成是由于 Walker 细胞中的酶 DT 脱氢酶 (NAD(P)H 脱氢酶 (醌)) 对该药物进行生物活化，从而还原 Tretazicar 的 4-硝基。该反应的产物是双功能烷化剂 5-氮杂环丙烷-1-基-4-羟氨基-2-硝基苯甲酰胺^[4]。

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

体内研究
(In Vivo)

Tretazicar (CB 1954) (80 mg/kg；腹腔注射，第 2 天和第 9 天) 可显著提高存活率^[3]。

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

Animal Model:	Female BALB/c mice (AB22-nr, SKOV3 human ovarian tumour xenograft)^[3]
Dosage:	80 mg/kg
Administration:	i.p. on days 2 and 9
Result:	The median survival of the AB22-nr was 49 days. Resulted in a significant increase in survival.

分子量

252.18

Formula

C₉H₈N₄O₅

CAS 号

21919-05-1

性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 125 mg/mL (495.68 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.9654 mL	19.8271 mL	39.6542 mL
5 mM	0.7931 mL	3.9654 mL	7.9308 mL
10 mM	0.3965 mL	1.9827 mL	3.9654 mL

查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (8.25 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.25 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.65%

选择批次：

Data Sheet (641 KB) SDS (392 KB)

COA (290 KB) HNMR (243 KB) LCMS (272 KB)

产品使用指南 (1538 KB)

参考文献

[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. [Content Brief]

[2]. Knox RJ, et al. CB 1954: from the Walker tumor to NQO2 and VDEPT. Curr Pharm Des. 2003;9(26):2091-104. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Tretazicar 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.9654 mL	19.8271 mL	39.6542 mL	99.1355 mL
	5 mM	0.7931 mL	3.9654 mL	7.9308 mL	19.8271 mL
	10 mM	0.3965 mL	1.9827 mL	3.9654 mL	9.9136 mL
	15 mM	0.2644 mL	1.3218 mL	2.6436 mL	6.6090 mL
	20 mM	0.1983 mL	0.9914 mL	1.9827 mL	4.9568 mL
	25 mM	0.1586 mL	0.7931 mL	1.5862 mL	3.9654 mL
	30 mM	0.1322 mL	0.6609 mL	1.3218 mL	3.3045 mL
	40 mM	0.0991 mL	0.4957 mL	0.9914 mL	2.4784 mL
	50 mM	0.0793 mL	0.3965 mL	0.7931 mL	1.9827 mL
	60 mM	0.0661 mL	0.3305 mL	0.6609 mL	1.6523 mL
	80 mM	0.0496 mL	0.2478 mL	0.4957 mL	1.2392 mL
	100 mM	0.0397 mL	0.1983 mL	0.3965 mL	0.9914 mL

Help & FAQs

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tretazicar (Synonyms: CB 1954)

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Tretazicar (Synonyms: CB 1954)

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