Chloroquinoxaline sulfonamide

Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle[1]. Antitumor activity[2].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

Research Areas >> Infection

topoisomerase II alpha

topoisomerase II beta

The Chloroquinoxaline sulfonamide IC50 for CV-1cells, obtained using an MTT cytotoxicity assay, was 1.8 mM. Chloroquinoxaline sulfonamide causes dose-dependent protein-DNA cross-links to CV-1 monkey kidney cell chromosomal DNA when drug treatment was terminated by lysis with GuHCl. Chloroquinoxaline sulfonamide-induced protein-DNA cross-links in CV-1 cells. Chloroquinoxaline sulfonamide-induced topoisomerase II-DNA cross-links[1]. Chloroquinoxaline sulfonamide (Chloroquinoxaline), a chlorinated derivative of sulfaquinoxaline, inhibits proliferation of murine B16 melanoma cells, but only when relatively high drug concentrations (1 mM) are used[2]. Cell Proliferation Assay[2] Cell Line: B16 murine melanoma cells Concentration: 10 μM, 100 μM, 1 mM Incubation Time: 24, 48, 72 hours Result: Inhibited proliferation of murine B16 melanoma cells, but only when relatively high drug concentrations (1 mM) were used.

[1]. Gao H, et al. Chloroquinoxaline sulfonamide (NSC 339004) is a topoisomerase IIalpha/beta poison. Cancer Res. 2000 Nov 1;60(21):5937-40.

[2]. Branda RF, et al. Cellular pharmacology of chloroquinoxaline sulfonamide and a related compound in murine B16 melanoma cells. Biochem Pharmacol. 1988 Dec 1;37(23):4557-64.

DATA ITEMS CITED :

4

MOLECULAR FORMULA :

C14-H11-Cl-N4-O2-S

MOLECULAR WEIGHT :

334.80

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

600 mg/kg

TOXIC EFFECTS :

Gastrointestinal - other changes Skin and Appendages - primary irritation (after topical exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :

NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB87-128658

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

607 mg/kg

TOXIC EFFECTS :

Gastrointestinal - other changes Skin and Appendages - primary irritation (after topical exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :

NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB87-128658

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

12 mg/kg

TOXIC EFFECTS :

Gastrointestinal - other changes Skin and Appendages - primary irritation (after topical exposure) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :

NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB87-128658 ** REPRODUCTIVE DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

DOSE :

600 mg/kg

SEX/DURATION :

male 1 day(s) pre-mating

TOXIC EFFECTS :

Reproductive - Paternal Effects - testes, epididymis, sperm duct

REFERENCE :

NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB87-128658