Home DNA Damage/DNA Repair DNA alkylator chemical Tretazicar (CB1954) For research use only.

Tretazicar (CB1954)

Synonyms: NSC 115829

Tretazicar (CB1954) is a anticancer prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent. It can be activated by NAD(P)H quinone oxidoreductase 2.

Tretazicar (CB1954) Chemical Structure

Tretazicar (CB1954) Chemical Structure

CAS: 21919-05-1

Purity & Quality Control

Batch: S782901 DMSO] 50 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.63%
99.63

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Biological Activity

Description Tretazicar (CB1954) is a anticancer prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent. It can be activated by NAD(P)H quinone oxidoreductase 2.
In vitro
In vitro The overexpression of nitroreductase oxidored nitro domain containing protein 1 (NOR1) is capable of converting the monofunctional alkylating agent CB1954 into a toxic form by reducing the 4 nitro group of CB1954 which is a potent cytotoxins. Toxic CB1954 enhances cells killing in the NPC cell line CNE1. the NOR1 gene enhances CB1954 mediated cell cytotoxicity through the upregulation of Grb2 expression and the activation of MAPK signal transduction in the HepG2 cell line[1].
Cell Research Cell lines HepG2 Cells
Concentrations 4-10 μmol/L
Incubation Time 48 h
Method

The human hepatocellular carcinoma cells, HepG2 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. Cell cyto-toxicity assays are conducted as previously described. HepG2 cells grown to ~80% confluence are washed with PBS and treated with a signal transduction inhibitor and/or CB1954. Measurements are collected from 10-12 individual microscopic fields in each experiment and data are summarized from 3-5 experiments.
In Vivo
In vivo The NTR/CB1954 system are used to specific ablation of cells in vivo. The effect of this inducible ablation system is dose-dependent[3]. NTR-mediated cell killing by CB1954 does not require cell proliferation. The activated CB1954 cross-links DNA which presumably triggers the apoptosis cascade, resulting in rapid cell death. specific and effective cells killing by NTR-CB1954 does not require a functional p53[2].
Animal Research Animal Models RED 40 female mice expressing high levels of BLG-NTR transgene in the mammary gland and nontransgenic control mice on lactation day 6
Dosages 50 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04374240 Completed
Prostate Cancer
University of Birmingham|Janssen LP|Department of Health United Kingdom|Medical Research Council
 March 19 2013 Phase 1

Chemical Information & Solubility

Molecular Weight 252.18 Formula

C9H8N4O5
CAS No. 21919-05-1 SDF Download Tretazicar (CB1954) SDF
Smiles C1CN1C2=C(C=C(C(=C2)C(=O)N)[N+](=O)[O-])[N+](=O)[O-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (198.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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