化合物Tretazicar T6798

Product Introduction
Bioactivity


英文名: Tretazicar

描述: 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。

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.

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 47 mg/mL (186.4 mM)


关键字: NQO1 | DNA Alkylator/Crosslinker | CB 1954 | rat | bifunctional | Inhibitor | inhibit | agent | cross-link | 256 | line | 4-hydroxylamine | Walker | NSC115829 | NSC-115829 | DNA | Tretazicar | CB-1954 | tumour

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相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Human Metabolite Library | Anti-Cancer Clinical Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | DNA Damage & Repair Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library

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