Chloroquinoxaline sulfonamide

Chloroquinoxaline sulfonamide用途

Chloroquinoxaline sulfonamide (Chloroquinoxaline) 是 sulfaquinoxaline 的结构类似物,是拓扑异构酶 II alpha/beta (topoisomerase II alpha/beta) 毒物。Chloroquinoxaline sulfonamide 用于控制家禽,兔,绵羊和牛的球虫病。具有抗肿瘤活性。

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Chloroquinoxaline sulfonamide名称

[ CAS 号 ]:
97919-22-7

[ 英文名 ]:
Chloroquinoxaline sulfonamide

[英文别名 ]:

Chlorsulfaquinoxaline
chloroquinoxaline sulfonamide
Sulfanilsaeure-(5-chlor-chinoxalin-2-ylamid)
5-Chloroquinoxaline-2-sulfanilamide
sulfanilic acid-(5-chloro-quinoxalin-2-ylamide)

Chloroquinoxaline sulfonamide生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

研究领域 >> 感染

[ 靶点 ]

topoisomerase II alpha

topoisomerase II beta

[体外研究]

用MTT法测定CV-1细胞的氯喹啉磺胺IC50为1.8mm。氯喹恶啉磺胺类药物经GuHCl裂解终止药物治疗后,引起CV-1猴肾细胞染色体DNA与剂量依赖性蛋白DNA交联。氯喹恶啉磺胺诱导CV-1细胞蛋白质DNA交联。氯喹恶啉磺胺诱导拓扑异构酶II-DNA交联[1]。氯喹恶啉磺胺(氯喹恶啉)是磺胺喹恶啉的氯化衍生物,可抑制小鼠B16黑色素瘤细胞的增殖,但仅当使用相对较高的药物浓度(1 mM)时[2]。细胞增殖实验[2]细胞系：B16小鼠黑色素瘤细胞浓度：10μM、100μM、1mm孵育时间：24、48、72小时结果：抑制了小鼠B16黑色素瘤细胞的增殖,但仅在药物浓度相对较高(1mm)时。

[参考文献]

[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.

Chloroquinoxaline sulfonamide物理化学性质

[ 密度 ]:
1.569g/cm3

[ 沸点 ]:
576.3ºC at 760mmHg

[ 分子式 ]:
C₁₄H₁₁ClN₄O₂S

[ 分子量 ]:
334.78100

[ 闪点 ]:
302.3ºC

[ 精确质量 ]:
334.02900

[ PSA ]:
106.35000

[ LogP ]:
4.40120

[ 折射率 ]:
1.734

Chloroquinoxaline sulfonamide毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DA9467000

CHEMICAL NAME :: Benzenesulfonamide, 4-amino-N-(5-chloro-2-quinoxalinyl)-

CAS REGISTRY NUMBER :: 97919-22-7

BEILSTEIN REFERENCE NO. :: 0312075

LAST UPDATED :: 199612

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

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Chloroquinoxaline sulfonamide安全信息

[ 海关编码 ]:
2935009090

Chloroquinoxaline sulfonamide合成路线

详细合成路线

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Chloroquinoxaline sulfonamide海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%