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Tretazicar (NSC-115829) 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。
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Tretazicar (NSC-115829) 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 179 | 现货 | |
5 mg | ¥ 395 | 现货 | |
10 mg | ¥ 597 | 现货 | |
25 mg | ¥ 1,190 | 现货 | |
50 mg | ¥ 1,790 | 现货 | |
100 mg | ¥ 2,670 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 437 | 现货 |
产品描述 | CB1954(Tretazicar (NSC-115829)), 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 | 在NPC细胞系CNE1中,Tretazicar增强了细胞杀伤效果。在HepG2细胞系中,NOR1基因上调Grb2表达并激活MAPK信号转导,从而增强Tretazicar介导的细胞毒性。 |
体内活性 | NTR/CB1954系统通过剂量依赖的方式,用于体内特异性细胞的消融。NTR介导的CB1954活化产生交联,推测是通过触发凋亡级联反应迅速导致细胞死亡。NTR-CB1954的选择性和强效细胞杀伤作用不需要p53功能。 |
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. |
别名 | 5-Aziridino-2,4-dinitrobenzamide, CB1954, NSC 115829 |
分子量 | 252.18 |
分子式 | C9H8N4O5 |
CAS No. | 21919-05-1 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 47 mg/mL (186.4 mM) | |||||||||||||||||||||||||||||||||||
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DMSO
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