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Tretazicar (CB1954) DNA alkylator chemical

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

Cat.No.S7829

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

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.63

Related Targets	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Other DNA alkylator Products	Lomeguatrib Methyl methanesulfonate Lobaplatin (D-19466) Semustine Treosulfan

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (198.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.

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.

Chemical Information, Storage & Stability

Molecular Weight	252.18	Formula	C₉H₈N₄O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	21919-05-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 115829			Smiles	C1CN1C2=C(C=C(C(=C2)C(=O)N)[N+](=O)[O-])[N+](=O)[O-]

Mechanism of Action

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, which is 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.
In vivo	The Tretazicar (CB1954) system is used for specific ablation of cells in vivo. The effect of this inducible ablation system is dose-dependent. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23741254/ [2] https://pubmed.ncbi.nlm.nih.gov/10505099/ [3] https://pubmed.ncbi.nlm.nih.gov/12429046/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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