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Tretazicar

 

Description of Tretazicar: Tretazicar (CB1954) is a dinitrobenzamide 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. 

  

Descritpion of caricotamide/tretazicar:  caricotamide/tretazicar  is a combination therapy consisting of the prodrug tretazicar and the enzyme co-substrate caricotamide with potential antineoplastic activity. In the presence of separately and simultaneously administered caricotamide, tretazicar is converted to the short-lived cytotoxic DNA cross-linking agent dinitrobenzamide by NAD(P)H quinine oxidoreductase 2 (NQO2), resulting in the inhibition of DNA replication and the induction of apoptosis. NQO2 has been found to be elevated in certain cancers such as hepatocellular carcinoma (HCC). Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

 

Current developer: Protherics PLC.

  

MedKoo Code#: 202980

Name: Tretazicar

CAS#: 21919-05-1

  

Synonym:   CB1954;Lopac-C-2235;Lopac0_000200;2,4-Dinitroethyleneiminobenzamide;C2235_SIGMA;CB 1954;5-Aziridino-2,4-dinitrobenzamide;CCRIS 1631;2,4-Dinitro-5-ethyleneiminobenzamide;5-(1-Aziridinyl)-2,4-dinitrobenzamide;5-Aziridinyl-2,4-dinitrobenzamide; Prolarix™。

  

IUPAC/Chemical name: 

5-(aziridin-1-yl)-2,4-dinitrobenzamide

  

Chemical structure: Theoretical analysis

  

 

  

 

  

MedKoo Code#: 202980
Name: Tretazicar
CAS#: 21919-05-1

Chemical Formula: C9H8N4O5

Exact Mass: 252.04947

Molecular Weight: 252.18

Elemental Analysis: C, 42.86; H, 3.20; N, 22.22; O, 31.72

  

  

Availability and price:

 

This agent is not in stock, which may be available through custom synthesis.

 

To inquire quotation and lead time or to ask questions, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.

 

Quality control data:

Product will be shipped with supporting analytical data.

  

 

Information about this agent

 

 

  

References

 

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94: Chaplin DJ. Hydralazine-induced tumor hypoxia: a potential target for cancer chemotherapy. J Natl Cancer Inst. 1989 Apr 19;81(8):618-22. PubMed PMID: 2704051.

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103: Adams GE. Radiosensitizers: a conference preview. Int J Radiat Oncol Biol Phys. 1984 Aug;10(8):1181-4. PubMed PMID: 6236183.

104: Tisdale MJ, Habberfield AD. Selective inhibition of ribonucleotide reductase by the monofunctional alkylating agent 5(1-aziridinyl)-2,4-dinitrobenzamide (CB 1954). Biochem Pharmacol. 1980 Oct 15;29(20):2845-53. PubMed PMID: 7002161.

105: Tisdale MJ, Phillips BJ. Guanosine 3',5'-monophosphate and the action of alkylating agents. Chem Biol Interact. 1977 Dec;19(3):375-81. PubMed PMID: 202413.

106: Jarman M, Melzack DH, Ross WC. The metabolism of the anti-tumour agent 5-(1-aziridinyl)-2,4-dinitrobenzamide (CB 1954). Biochem Pharmacol. 1976 Nov 15;25(22):2475-8. PubMed PMID: 985569.

 

 

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