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噻唑呋林

噻唑呋林用途

硫唑呋林是一种具有抗肿瘤活性的合成核苷类似物。噻唑呋林在细胞内合成代谢为噻唑-4-甲酰胺腺嘌呤二核苷酸(TAD),一种IMP脱氢酶(IMPDH)的有效抑制剂。

噻唑呋林名称

[ CAS 号 ]:
60084-10-8

[ 中文名 ]:
噻唑呋林

[ 英文名 ]:
Tiazofurin

[英文别名 ]:

Riboxamide
2-b-D-Ribofuranosyl-4-thiazolecarboxamide
Tiazofurina [Spanish]
4-Thiazolecarboxamide, 2-β-D-ribofuranosyl-
2-β-D-Ribofuranosyl-4-thiazolecarboxamide
[3H]-Tiazofurin
Tiazofurine
Tiazole
Tiazofurin
Tiazofurina

噻唑呋林生物活性

[ 描述 ]:

硫唑呋林是一种具有抗肿瘤活性的合成核苷类似物。噻唑呋林在细胞内合成代谢为噻唑-4-甲酰胺腺嘌呤二核苷酸(TAD),一种IMP脱氢酶(IMPDH)的有效抑制剂。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 核苷抗代谢药/类似物

[参考文献]

[1]. Tricot G, Jayaram HN, Weber G, Hoffman R. Tiazofurin: biological effects and clinical uses. Int J Cell Cloning. 1990;8(3):161-170.

噻唑呋林物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
641.3±55.0 °C at 760 mmHg

[ 分子式 ]:
C₉H₁₂N₂O₅S

[ 分子量 ]:
260.267

[ 闪点 ]:
341.6±31.5 °C

[ 精确质量 ]:
260.046692

[ PSA ]:
154.14000

[ LogP ]:
-1.13

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.675

[ 储存条件 ]:
2-8°C，避光，惰性气体保存

噻唑呋林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XJ3600000

CHEMICAL NAME :: 4-Thiazolecarboxamide, 2-beta-D-ribofuranosyl-

CAS REGISTRY NUMBER :: 60084-10-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C9-H12-N2-O5-S

MOLECULAR WEIGHT :: 260.29

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 1135 mg/kg/15D-I

TOXIC EFFECTS :: Behavioral - headache Musculoskeletal - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 892 mg/kg/10D-I

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1684 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3400 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Blood - other changes

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1090 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - food intake (animal) Behavioral - fluid intake

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 3425 mg/kg

SEX/DURATION :: male 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct

MUTATION DATA

TYPE OF TEST :: Mutation test systems - not otherwise specified

TEST SYSTEM :: Rodent - mouse Lymphocyte

DOSE/DURATION :: 20 umol/L

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 45,5512,1985

噻唑呋林安全信息

[ 危害码 (欧洲) ]:
Xi

[ 海关编码 ]:
2934100090

噻唑呋林合成路线

详细合成路线

噻唑呋林上下游产品

噻唑呋林上游产品

噻唑呋林下游产品

噻唑呋林海关

[ 海关编码 ]: 2934100090

[ 中文概述 ]:
2934100090. 结构上含有一个非稠合噻唑环的化合物(不论是否氢化). 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:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934100090 other compounds containing an unfused thiazole ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%