| Name | Tretazicar |
| Description | 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. |
| Cell Research | 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. |
| Animal Research | 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. |
| In vitro | In the NPC cell line CNE1, toxic Tretazicar enhances cells killing. The overexpression of nitroreductase oxidored nitro domain-containing protein 1 (NOR1) reduce the 4 nitro group of Tretazicar, a potent cytotoxin, in order to convert the monofunctional alkylating agent Tretazicar 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 Tretazicar mediated cell cytotoxicity. |
| In vivo | 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | 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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| Keywords | 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 |
| Inhibitors Related | Cyclophosphamide hydrate | Bendamustine hydrochloride | Busulfan | N-Nitroso-N-methylurea | Ifosfamide | Oxaliplatin | Streptozocin | Temozolomide | Methyl methanesulfonate | Cyclophosphamide | Carboplatin | Cisplatin |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Target-Focused Phenotypic Screening Library | ReFRAME Related Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Aging Compound Library | Clinical Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
