97919-22-7

• 常用中文名：Chloroquinoxaline sulfonamide
• 常用英文名：Chloroquinoxaline sulfonamide
• CAS号：97919-22-7
• 分子式：C₁₄H₁₁ClN₄O₂S
• 分子量：334.78100
• 相关类别： 信号通路 细胞周期/DNA损伤 拓扑异构酶
• 发布时间：2016-08-10 08:27:56
• 更新时间：2024-01-18 16:18:52
• 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。

名称

• 英文名: 4-amino-N-(5-chloroquinoxalin-2-yl)benzenesulfonamide
• 英文别名: Chlorsulfaquinoxaline; chloroquinoxaline sulfonamide; Sulfanilsaeure-(5-chlor-chinoxalin-2-ylamid); 4-Amino-N-(5-chloro-2-quinoxalinyl)benzenesulfonamide; 5-Chloroquinoxaline-2-sulfanilamide; sulfanilic acid-(5-chloro-quinoxalin-2-ylamide)

物化性质

• 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

生物活性

• 描述: 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。
• 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.

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

安全

• 海关编码: 2935009090

合成路线

21745-41-5 ~% 97919-22-7

文献：Wolf et al. Journal of the American Chemical Society, 1949 , vol. 71, p. 6,7

121-60-8 ~% 97919-22-7

文献：Wolf et al. Journal of the American Chemical Society, 1949 , vol. 71, p. 6,7

55687-05-3 ~% 97919-22-7

文献：Wolf et al. Journal of the American Chemical Society, 1949 , vol. 71, p. 6,7

上下游产品

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55687-05-3 21745-41-5 121-60-8
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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%