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曲氟尿苷

曲氟尿苷用途

Trifluridine是不可逆的胸苷酸合酶抑制剂,从而抑制DNA合成。 Trifluridine是用于单纯疱疹病毒 (HSV) 感染的抗病毒药物。

曲氟尿苷名称

[ CAS 号 ]:
70-00-8

[ 中文名 ]:
三氟胸苷

[ 英文名 ]:
Trifluorothymidine

[中文别名 ]:

[英文别名 ]:

Viroptic
α,α,α-Trifluorothymidine
2'-Deoxy-5-(trifluoromethyl)uridine
UNII-RMW9V5RW38
Trifluorothymidine
Trifluridine
EINECS 200-722-8
2'-Deoxy-5-trifluoromethyluridine
Virophta
Uridine, 2'-deoxy-5-(trifluoromethyl)-

曲氟尿苷生物活性

[ 描述 ]:

Trifluridine是不可逆的胸苷酸合酶抑制剂,从而抑制DNA合成。 Trifluridine是用于单纯疱疹病毒 (HSV) 感染的抗病毒药物。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 核苷抗代谢药/类似物

信号通路 >> 细胞凋亡 >> 胸苷酸合成酶

研究领域 >> 癌症

[参考文献]

[1]. Suzuki N, et al. Mode of action of trifluorothymidine (TFT) against DNA replication and repair enzymes. Int J Oncol. 2011 Jul;39(1):263-70.

[2]. Suzuki N, et al. Trifluorothymidine exhibits potent antitumor activity via the induction of DNA double-strand breaks. Exp Ther Med. 2011 May;2(3):393-397.

[3]. Temmink OH, et al. Irinotecan-induced cytotoxicity to colon cancer cells in vitro is stimulated by pre-incubation withtrifluorothymidine. Eur J Cancer. 2007 Jan;43(1):175-83.

[4]. Okayama T, et al. Involvement of concentrative nucleoside transporter 1 in intestinal absorption of trifluorothymidine, a novel antitumor nucleoside, in rats. J Pharmacol Exp Ther. 2012 Feb;340(2):457-62.

[相关活性小分子]

曲氟尿苷物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 熔点 ]:
190-193 °C(lit.)

[ 分子式 ]:
C₁₀H₁₁F₃N₂O₅

[ 分子量 ]:
296.200

[ 精确质量 ]:
296.062012

[ PSA ]:
104.55000

[ LogP ]:
0.07

[ 外观性状 ]:
白色结晶粉末

[ 折射率 ]:
1.534

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
水溶性：可溶

曲氟尿苷MSDS

曲氟尿苷毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XP2087500

CHEMICAL NAME :: Thymidine, alpha,alpha,alpha-trifluoro-

CAS REGISTRY NUMBER :: 70-00-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C10-H11-F3-N2-O5

MOLECULAR WEIGHT :: 296.23

WISWESSER LINE NOTATION :: T6NVMVJ EXFFF A- ET5OTJ B1Q CQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2946 mg/kg

TOXIC EFFECTS :: Liver - other changes

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1931 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 :: 3381 mg/kg

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 400 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 187 mg/kg/15D-I

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of salivary glands Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Blood - leukopenia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 2600 mg/kg/90D-I

TOXIC EFFECTS :: Liver - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 2100 mg/kg/14D-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - chronic pulmonary edema Gastrointestinal - hypermotility, diarrhea Related to Chronic Data - death

MUTATION DATA

TYPE OF TEST :: Mutation in mammalian somatic cells

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 4 mg/L

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 86,180,1986 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3218 No. of Facilities: 3 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 82 (estimated) No. of Female Employees: 14 (estimated)

曲氟尿苷安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302 + H312 + H332-H351

[ 警示性声明 ]:
P261-P280-P301 + P312 + P330

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi:Irritant

[ 风险声明 (欧洲) ]:
R20/21/22;R40

[ 安全声明 (欧洲) ]:
S22-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
XP2087500

曲氟尿苷合成路线

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曲氟尿苷上游产品

曲氟尿苷下游产品

曲氟尿苷文献

Mechanistic evaluation of Ginkgo biloba leaf extract-induced genotoxicity in L5178Y cells.

Toxicol. Sci. 139(2) , 338-49, (2014)

Ginkgo biloba has been used for many thousand years as a traditional herbal remedy and its extract has been consumed for many decades as a dietary supplement. Ginkgo biloba leaf extract is a complex m...

Quantitative high-throughput identification of drugs as modulators of human constitutive androstane receptor.

Sci. Rep. 5 , 10405, (2015)

The constitutive androstane receptor (CAR, NR1I3) plays a key role in governing the transcription of numerous hepatic genes that involve xenobiotic metabolism/clearance, energy homeostasis, and cell p...

Differential activation of cell death and autophagy results in an increased cytotoxic potential for trifluorothymidine compared to 5-fluorouracil in colon cancer cells.

Int. J. Cancer 126 , 2457-2468, (2010)

Trifluorothymidine (TFT) is part of the oral drug formulation TAS-102. Both 5-fluorouracil (5-FU) and TFT can inhibit thymidylate synthase and be incorporated into DNA. TFT shows only moderate cross-r...

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