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5-氟尿嘧啶

5-氟尿嘧啶用途

5-Fluorouracil 是一种有效的抗肿瘤剂,通过抑制胸苷酸合成酶从而消耗细胞内dTTP来影响嘧啶合成。
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5-氟尿嘧啶名称

[ CAS 号 ]:
51-21-8

[ 中文名 ]:
5-氟脲嘧啶

[ 英文名 ]:
Fluorouracil

[中文别名 ]:

[英文别名 ]:

5-氟尿嘧啶生物活性

[ 描述 ]:

5-Fluorouracil 是一种有效的抗肿瘤剂,通过抑制胸苷酸合成酶从而消耗细胞内dTTP来影响嘧啶合成。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 核苷抗代谢药/类似物
研究领域 >> 癌症

[体外研究]

5-氟尿嘧啶(5-Fu)和多柔比星(Dox)显示出协同抗癌功效。 5-Fu/Dox-DNM对人乳腺癌(MDA-MB-231)细胞的IC50值为0.25μg/ mL,与Dox-DNM和5-Fu相比,细胞毒性增加11.2倍和6.1倍。 -DNM分别为[1]。在5-氟尿嘧啶(5-FU)和CDDP处理的NFBD1抑制的NPC细胞中,使用慢病毒介导的短发夹RNA消除NPC CNE1细胞系中的NFBD1表达,并且这些细胞的敏感性升高。 NFBD1敲低导致CDDP或5-FU处理的CNE1细胞明显诱导细胞凋亡[3]。

[体内研究]

5-氟尿嘧啶(23 mg/kg,3次/周)持续14天,在治疗开始后第3天诱导与急性肠道炎症相关的加速胃肠道转运,这可能导致第7天后观察到的ENS持续变化治疗有助于延迟胃肠道转运和结肠运动障碍[14]。

[动物实验]

小鼠接受腹膜内注射5-FU(23mg / kg),每周3次,通过26号针头。将5-FU溶于100%二甲基亚砜(DMSO)中,使1M / L储备溶液在-20℃冷藏。然后将原料解冻并用无菌水稀释以制备0.1M / L(10%DMSO)溶液用于腹膜内注射。计算5-FU的剂量等于每人体表面积的标准人剂量。低剂量的5-FU(10-40mg / kg)已经显示出在小鼠癌症模型中具有抗肿瘤功效。假处理的小鼠通过26号针头每周三次通过腹膜内注射在无菌水中接受10%DMSO。注射体积按体重计算;每次注射的最大体积不超过200μL。在第一次注射后3天(2次治疗),7次(3次治疗)和14次(6次治疗),通过颈脱位使小鼠安乐死,并收集结肠用于体外实验。

[参考文献]

[1]. Han R, et al. Amphiphilic dendritic nanomicelle-mediated co-delivery of 5-fluorouracil and doxorubicin for enhanced therapeutic efficacy. J Drug Target. 2016 Jun 29:1-28. [Epub ahead of print]

[2]. McQuade RM, et al. Gastrointestinal dysfunction and enteric neurotoxicity following treatment with anticancer chemotherapeutic agent 5-fluorouracil. Neurogastroenterol Motil. 2016 Jun 28.

[3]. Zeng Q, et al. Knockdown of NFBD1/MDC1 enhances chemosensitivity to cisplatin or 5-fluorouracil in nasopharyngeal carcinoma CNE1 cells. Mol Cell Biochem. 2016 Jul;418(1-2):137-46.

[4]. Yin L, et al. Antitumor effects of oncolytic herpes simplex virus type 2 against colorectal cancer in vitro and in vivo. Ther Clin Risk Manag. 2017 Feb 7;13:117-130.


[相关活性小分子]

阿扎胞苷 | 5-溴-2'-脱氧尿苷 | 盐酸呋咯地辛 | 5-氟-2'-脱氧脲核苷 | 雷替曲塞 | 曲氟尿苷 | 阿糖腺苷 | 盐酸Tipiracil | 克罗拉滨 | 去氧氟尿苷 | 奈拉滨 | 8-氮鸟嘌呤 | 氟环戊烯基胞嘧啶 | 替加氟 | LY2334737

5-氟尿嘧啶物理化学性质

[ 密度 ]:
1.7±0.1 g/cm3

[ 沸点 ]:
401.4±48.0 °C at 760 mmHg

[ 熔点 ]:
282-286 °C (dec.)(lit.)

[ 分子式 ]:
C4H3FN2O2

[ 分子量 ]:
130.077

[ 闪点 ]:
196.5±29.6 °C

[ 精确质量 ]:
130.017853

[ PSA ]:
65.72000

[ LogP ]:
-2.10

[ 外观性状 ]:
白色至几乎白色结晶粉末

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.596

[ 储存条件 ]:
Store at 0-5

[ 稳定性 ]:
Stable. Light sensitive. Combustible. Incompatible with strong oxidizing agents, strong bases.

[ 水溶解性 ]:
12.2 g/L 20 ºC

5-氟尿嘧啶MSDS

5-氟尿嘧啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
YR0350000
CHEMICAL NAME :
Uracil, 5-fluoro-
CAS REGISTRY NUMBER :
51-21-8
LAST UPDATED :
199710
DATA ITEMS CITED :
156
MOLECULAR FORMULA :
C4-H3-F-N2-O2
MOLECULAR WEIGHT :
130.09
WISWESSER LINE NOTATION :
T6MVMVJ EF

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
Standard Draize test
ROUTE OF EXPOSURE :
Administration onto the skin
SPECIES OBSERVED :
Human
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
450 mg/kg/30D
TOXIC EFFECTS :
Gastrointestinal - other changes Blood - changes in bone marrow (not otherwise specified) Tumorigenic - active as anti-cancer agent
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human
DOSE/DURATION :
6 mg/kg/3D
TOXIC EFFECTS :
Cardiac - EKG changes not diagnostic of specified effects Cardiac - other changes Lungs, Thorax, or Respiration - other changes
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
150 mg/kg/17W-I
TOXIC EFFECTS :
Blood - other hemolysis with or without anemia
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
39 mg/kg/1D-I
TOXIC EFFECTS :
Cardiac - changes in coronary arteries
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
27 mg/kg/4D-C
TOXIC EFFECTS :
Cardiac - other changes
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
230 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 :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
70 mg/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
217 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 - rat
DOSE/DURATION :
245 mg/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
240 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 :
Parenteral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
500 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 :
Rectal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
884 mg/kg
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea Gastrointestinal - other changes
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
115 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 :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
100 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 :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
169 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 :
81 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 :
Intracerebral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
41600 ug/kg
TOXIC EFFECTS :
Peripheral Nerve and Sensation - sensory change involving peripheral nerve Sense Organs and Special Senses (Eye) - ptosis Sense Organs and Special Senses (Eye) - effect, not otherwise specified
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intratracheal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
200 mg/kg
TOXIC EFFECTS :
Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
171 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 :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
30 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
18900 ug/kg
TOXIC EFFECTS :
Behavioral - muscle weakness Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
15 mg/kg
TOXIC EFFECTS :
Vascular - BP elevation not characterized in autonomic section
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
25 mg/kg
TOXIC EFFECTS :
Vascular - BP elevation not characterized in autonomic section
TYPE OF TEST :
LD10 - Lethal Dose
ROUTE OF EXPOSURE :
Parenteral
SPECIES OBSERVED :
Rodent - hamster
DOSE/DURATION :
140 mg/kg
TOXIC EFFECTS :
Tumorigenic - active as anti-cancer agent
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2520 mg/kg/12W-I
TOXIC EFFECTS :
Endocrine - changes in spleen weight Blood - changes in bone marrow (not otherwise specified) Related to Chronic Data - changes in testicular weight
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1092 mg/kg/30D-I
TOXIC EFFECTS :
Endocrine - changes in thymus weight Blood - normocytic anemia Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
6552 mg/kg/26W-I
TOXIC EFFECTS :
Endocrine - changes in thymus weight Liver - changes in liver weight Blood - changes in erythrocyte (RBC) count
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
700 mg/kg/40W-I
TOXIC EFFECTS :
Nutritional and Gross Metabolic - weight loss or decreased weight gain 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 :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1283 mg/kg/13W-C
TOXIC EFFECTS :
Behavioral - fluid intake Endocrine - changes in thymus weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
360 mg/kg/60D-I
TOXIC EFFECTS :
Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
780 mg/kg/30D-I
TOXIC EFFECTS :
Endocrine - changes in thymus weight Blood - normocytic anemia Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2340 mg/kg/13W-I
TOXIC EFFECTS :
Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Blood - normocytic anemia
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
21 mg/kg/7D-I
TOXIC EFFECTS :
Blood - changes in bone marrow (not otherwise specified) Blood - changes in leukocyte (WBC) count Blood - changes in platelet count
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Rectal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
4920 mg/kg/90D-I
TOXIC EFFECTS :
Gastrointestinal - other changes Endocrine - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Rectal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9540 mg/kg/26W-I
TOXIC EFFECTS :
Gastrointestinal - other changes Endocrine - other changes Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
300 mg/kg/60D-I
TOXIC EFFECTS :
Endocrine - changes in spleen weight Related to Chronic Data - death Related to Chronic Data - changes in testicular weight
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
455 mg/kg/13W-I
TOXIC EFFECTS :
Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
175 mg/kg/5W-I
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Blood - changes in bone marrow (not otherwise specified) Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1500 mg/kg/50W-I
TOXIC EFFECTS :
Tumorigenic - Carcinogenic by RTECS criteria Lungs, Thorax, or Respiration - tumors Blood - tumors
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
150 mg/kg
SEX/DURATION :
female 20-31 week(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - other neonatal measures or effects
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
240 mg/kg
SEX/DURATION :
female 11-14 week(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
35 mg/kg
SEX/DURATION :
female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
175 mg/kg
SEX/DURATION :
female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
15 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
30 mg/kg
SEX/DURATION :
female 12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - gastrointestinal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
30 mg/kg
SEX/DURATION :
female 12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - homeostasis
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
20 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
20 mg/kg
SEX/DURATION :
female 14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
30 mg/kg
SEX/DURATION :
female 14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
330 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
175 mg/kg
SEX/DURATION :
female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
245 mg/kg
SEX/DURATION :
female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetal death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
50 mg/kg
SEX/DURATION :
female 13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
20 mg/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
20 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
30 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
10 mg/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
30 mg/kg
SEX/DURATION :
female 12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
67 mg/kg
SEX/DURATION :
male 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
DOSE :
24 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
DOSE :
28 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
DOSE :
56 mg/kg
SEX/DURATION :
female 11 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - homeostasis
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
DOSE :
20 mg/kg
SEX/DURATION :
female 9 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
TYPE OF TEST :
Specific locus test
TYPE OF TEST :
DNA inhibition
TYPE OF TEST :
Mutation test systems - not otherwise specified
TYPE OF TEST :
Mutation test systems - not otherwise specified
TYPE OF TEST :
Micronucleus test
TYPE OF TEST :
Cytogenetic analysis
TYPE OF TEST :
Micronucleus test
TYPE OF TEST :
Micronucleus test
TYPE OF TEST :
Mutation test systems - not otherwise specified
TYPE OF TEST :
Unscheduled DNA synthesis
TYPE OF TEST :
Unscheduled DNA synthesis
TYPE OF TEST :
Unscheduled DNA synthesis
TYPE OF TEST :
DNA inhibition
TYPE OF TEST :
Mutation test systems - not otherwise specified
TYPE OF TEST :
Cytogenetic analysis
TYPE OF TEST :
Cytogenetic analysis
TYPE OF TEST :
Sperm Morphology
TYPE OF TEST :
Sperm Morphology
TYPE OF TEST :
Micronucleus test
TYPE OF TEST :
Cytogenetic analysis

MUTATION DATA

TYPE OF TEST :
DNA inhibition
TEST SYSTEM :
Mammal - species unspecified Cells - not otherwise specified
DOSE/DURATION :
100 umol/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 120,139,1983 *** REVIEWS *** IARC Cancer Review:Animal Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 26,217,1981 IARC Cancer Review:Human Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 26,217,1981 IARC Cancer Review:Group 3 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,210,1987 TOXICOLOGY REVIEW NEJMAG New England Journal of Medicine. (Massachusetts Medical Soc., 10 Shattuck St., Boston, MA 02115) V.198- 1928- Volume(issue)/page/year: 291,75,1974 TOXICOLOGY REVIEW MIMDAL Minnesota Medicine. (Minnesota Medical Assoc., 2221 University Ave., SE, Suite 400, Minneapolis, MN 55414) V.1- 1918- Volume(issue)/page/year: 57,19,1974 TOXICOLOGY REVIEW JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 172,1765,1960 TOXICOLOGY REVIEW 32XPAD "Teratology," Berry, C.L., and D.E. Poswillo, eds., New York, Springer, 1975 Volume(issue)/page/year: -,49,1975 TOXICOLOGY REVIEW JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 144,429,1964 TOXICOLOGY REVIEW ARVPAX Annual Review of Pharmacology. (Palo Alto, CA) V.1-15, 1961-75. For publisher information, see ARPTDI. Volume(issue)/page/year: 5,447,1965 TOXICOLOGY REVIEW CRTXB2 CRC Critical Reviews in Toxicology. (CRC Press, Inc., 2000 Corporate Blvd., NW, Boca Raton, FL 33431) V.1- 1971- Volume(issue)/page/year: 2,159,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4035 No. of Facilities: 681 (estimated) No. of Industries: 2 No. of Occupations: 9 No. of Employees: 23501 (estimated) No. of Female Employees: 15547 (estimated)
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5-氟尿嘧啶安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H412

[ 警示性声明 ]:
P273-P301 + P310

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R20/21/22

[ 安全声明 (欧洲) ]:
S36-S36/37

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
YR0350000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2933599090

5-氟尿嘧啶合成路线

5-氟尿嘧啶上下游产品

5-氟尿嘧啶制备

1.由氟乙酸乙酯经缩合,环合水解而得。1.缩合,环合将甲醇钠甲醇溶液投入干燥的不锈钢反应锅内,搅拌下减压浓缩至甲醇钠成白色粉末,冷却至50℃,加入甲苯,再冷至10℃以下,滴加甲酸乙酯。加完后仍保持10℃以下滴加氟乙酸乙酯。加毕,在30℃左右搅拌反应8小时。静置,得淡黄色稠厚的混合物。在缩合物中加入甲醇和甲基异尿素硫酸盐,搅拌加热至66-70℃回流反应6h。常压回收甲醇至反应物呈现稀糊状时,再减压蒸至粘稠状为止。加水加热溶解,加入活性炭。过滤,滤液用浓盐酸酸化至pH3-4,析出结晶,冷却过滤,用冷水洗涤滤饼,以沸水调浆浸泡过认,过滤,冷水洗涤,干燥,得5-氟-4-羟基-2-四氧基嘧啶(C5H5FN2O2)。2.水解上述环合产物5-氟-4-羟基-2-甲氧基嘧啶加入20%盐酸中,在60℃水解4h,经后处理即得5-氟尿嘧啶。

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5-氟尿嘧啶海关

[ 海关编码 ]: 2933599090

[ 中文概述 ]:
2933599090. 其他结构上有嘧啶环的化合物(包括其他结构上有哌嗪环的化合物. 增值税率:17.0%. 退税率:13.0%. 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, 乌洛托品请注明外观, 6-己内酰胺请注明外观, 签约日期

[ Summary ]:
2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

5-氟尿嘧啶文献

TAp73 promotes cell survival upon genotoxic stress by inhibiting p53 activity.

Oncotarget 5(18) , 8107-22, (2014)

p53 plays a key role in regulating DNA damage response by suppressing cell cycle progression or inducing apoptosis depending on extent of DNA damage. However, it is not clear why mild genotoxic stress...

cIEF for rapid pKa determination of small molecules: a proof of concept.

Eur. J. Pharm. Sci. 63 , 14-21, (2014)

A capillary isoelectric focusing (cIEF) method was developed for the determination of the ionization constants (pKa) of small molecules. Two approaches used to decrease the electroosmotic flow (EOF) w...

Establishment and characterization of cell lines from chromosomal instable colorectal cancer.

World J. Gastroenterol. 21(1) , 164-76, (2015)

To generate novel tumor models for preclinical validation of biomarkers that allow drug response prediction and individual therapeutic decisions.Cell line establishment was conducted by both direct in...


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【5-氟尿嘧啶】化源网提供5-氟尿嘧啶CAS号51-21-8,5-氟尿嘧啶MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询5-氟尿嘧啶上化源网,专业又轻松。>>电脑版:5-氟尿嘧啶

标题:5-氟尿嘧啶_MSDS_用途_密度_5-氟尿嘧啶CAS号【51-21-8】_化源网 地址:https://m.chemsrc.com/mip/cas/51-21-8_161653.html