Tretazicar (CB1954)

Catalog No.S7829 Batch:S782901

Technical Data

Formula	C₉H₈N₄O₅
Molecular Weight	252.18	CAS No.	21919-05-1
Solubility (25°C)*	In vitro	DMSO	50 mg/mL (198.27 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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	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].
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].

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[2]}	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.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[2]}

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.

References

Selleck's Tretazicar (CB1954) has been cited by 1 publication

Reporter cell lines to screen for inhibitors or regulators of the KRAS-RAF-MEK1/2-ERK1/2 pathway [ Biochem J, 2024, 481(6):405-422]	PubMed: 38381045

Reporter cell lines to screen for inhibitors or regulators of the KRAS-RAF-MEK1/2-ERK1/2 pathway [ Biochem J, 2024, 481(6):405-422]

PubMed: 38381045

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SHIPPING AND STORAGE
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