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Tretazicar

Catalog No. T6798   CAS 21919-05-1
Synonyms: 5-Aziridino-2,4-dinitrobenzamide, CB1954, NSC 115829

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.

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Tretazicar Chemical Structure
Tretazicar, CAS 21919-05-1
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 72.00
25 mg In stock $ 147.00
50 mg In stock $ 222.00
100 mg In stock $ 328.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 99.7%
Purity: 96.76%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
In vitro In the NPC cell line CNE1, toxic CB1954 enhances cells killing. The overexpression of nitroreductase oxidored nitro domain-containing protein 1 (NOR1) reduce the 4 nitro group of CB1954, a potent cytotoxin, in order to convert the monofunctional alkylating agent CB1954 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 CB1954 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.
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.
Synonyms 5-Aziridino-2,4-dinitrobenzamide, CB1954, NSC 115829
Molecular Weight 252.18
Formula C9H8N4O5
CAS No. 21919-05-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)

TargetMolReferences and Literature

1. Gui R, et al. Oncol Lett. 2012, 4(3):566-570. 2. Cui W, et al. Gene Ther. 1999, 6(5):764-770. 3. Felmer R, et al. J Endocrinol. 2002, 175(2):487-98.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Compound Library Clinical Compound Library Apoptosis Compound Library Anti-Lung Cancer Compound Library Drug Repurposing Compound Library Bioactive Compounds Library Max

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Keywords

Tretazicar 21919-05-1 DNA Damage/DNA Repair DNA Alkylator/Crosslinker DNA Alkylation NQO1 5-Aziridino-2,4-dinitrobenzamide CB 1954 rat bifunctional Inhibitor inhibit agent cross-link 256 line 4-hydroxylamine Walker NSC115829 NSC-115829 DNA CB-1954 CB1954 NSC 115829 tumour inhibitor

 

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