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Tretazicar (CB1954) DNA alkylator chemical

Name: Tretazicar (CB1954)
Brand: Selleck Chemicals
SKU: S7829
Availability: InStock
Rating: 5 (1 reviews)

Catalog No.S7829 Purity:99.63%

Tretazicar (CB1954) is an 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.

Chemical Structure

Molecular Weight: 252.18

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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Mechanism of Action

In vitro
In vitro	The overexpression of nitroreductase oxidored nitro domain containing protein 1 (NOR1) is capable of converting the monofunctional alkylating agent Tretazicar (CB1954) into a toxic form by reducing its 4-nitro group, resulting in a potent cytotoxin. This compound enhances cell 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 Tretazicar (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/Tretazicar (CB1954) system is used for specific ablation of cells in vivo. The effect of this inducible ablation system is dose-dependent^[3]. NTR-mediated cell killing by this compound does not require cell proliferation. The activated form cross-links DNA which presumably triggers the apoptosis cascade, resulting in rapid cell death. Specific and effective cell 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04374240	Completed	Prostate Cancer	University of Birmingham\|Janssen LP\|Department of Health United Kingdom\|Medical Research Council	March 19 2013	Phase 1

References

https://pubmed.ncbi.nlm.nih.gov/23741254/
https://pubmed.ncbi.nlm.nih.gov/10505099/
https://pubmed.ncbi.nlm.nih.gov/12429046/

Chemical Information

Molecular Weight	252.18	Formula	C₉H₈N₄O₅
CAS No.	21919-05-1	SDF	Download SDF
Synonyms	NSC 115829
Smiles	C1CN1C2=C(C=C(C(=C2)C(=O)N)[N+](=O)[O-])[N+](=O)[O-]

Storage and Stability

Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
			1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.410mg/ml (1.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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