CB-1954 is a prodrug that is enzymatically activated to generate an antitumor agent that forms DNA-DNA interstrand crosslinks. In rat Walker 256 carcinoma cells, CB-1954 is reduced by NAD(P)H:quinone oxidoreductase (NQO1) to the cytotoxic derivative 5-(aziridin-1-yl)-4-hydroxylamineo 2 nitrobenzamide, a bifunctional alkylating agent.
5-Aziridino-2,4-dinitrobenzamide is an anticancer prodrug used in gene therapy research and is known to be activated by NAD(P)H Quinone Oxidoreductase 2.
Tretazicar is an anticancer prodrug used in gene therapy research and is known to be activated by NAD(P)H Quinone Oxidoreductase 2.
CB 1954 is an anticancer prodrug used in gene therapy research; activated by NAD(P)H quinone oxidoreductase2.
Tretazicar (CB 1954) (80 mg/kg; i.p. on days 2 and 9) results in a significant increase in survival[3].
| Animal Model: | Female BALB/c mice (AB22-nr, SKOV3 human ovarian tumour xenograft)[3] |
| Dosage: | 80 mg/kg |
| Administration: | i.p. on days 2 and 9 |
| Result: | The median survival of the AB22-nr was 49 days. Resulted in a significant increase in survival. |
[1] R J KNOX. Bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954) by human NAD(P)H quinone oxidoreductase 2: a novel co-substrate-mediated antitumor prodrug therapy.[J]. Cancer research, 2000, 60 15: 4179-4186.
