5-Fluoro-5'-deoxyuridine 5'-脱氧-5-氟尿苷
CAS 3094-09-5 MFCD00866530
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资金保障
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信息真实价格透明
资金保障
专业采购外包团队在线服务
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现货库存
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分类
- {Chemicalbook} 药物: 抗肿瘤药: 抗代谢物抗肿瘤药物
- {SNA} Apoptosis and Cell Cycle, Bioactive Small Molecule Alphabetical Index, DNA Synthesis Inhibitors, DNA metabolism, F, 抗肿瘤药物, 生物活性小分子, 癌症研究, 细胞信号转导和神经科学, 细胞生物学
- {SNA} Antitumor Agents, Apoptosis and Cell Cycle, Bioactive Small Molecules, Cancer Research, Cell Biology, Cell Signaling and Neuroscience, DNA Synthesis Inhibitors, DNA metabolism, F
- {SNA} Antitumor Agents, Apoptosis and Cell Cycle, Bioactive Small Molecule Alphabetical Index, DNA Synthesis Inhibitors, DNA metabolism, F,
产品应用
- Doxifluridine, also known as 5'-Deoxy-5-fluorouridine, is a fluoropyrimidine derivative and oral prodrug of the antineoplastic agent 5-fluorouracil (5-FU) with antitumor activity. Doxifluridine, designed to circumvent the rapid degradation of 5-FU by dihydropyrimidine dehydrogenase in the gut wall, is converted into 5-FU in the presence of pyrimidine nucleoside phosphorylase.
安全信息
- H226 Flammable liquid and vapour 易燃液体和蒸气
- H303 May be harmfully swallowed 吞食可能有害
- H315 Causes skin irritation 会刺激皮肤
- H317 May cause an allergic skin reaction 可能导致皮肤过敏
- H319 Causes serious eye irritation 严重刺激眼睛
- H332 Harmful if inhaled 吸入有害
- H335 May cause respiratory irritation 可能导致呼吸道刺激
- H340 May cause genetic defects 可能导致遗传性缺陷
- H350 May cause cancer 可能致癌
- H351 Suspected of causing cancer 怀疑致癌
- H360 May damage fertility or the unborn child 可能对生育能力或未出生婴儿造成伤害
- H411 Toxictoaquaticlifewithlonglastingeffects 对水生生物有毒性并具有长期影响。
- P201 Obtain special instructions before use. 使用前获取专门指示。
- P202 Do not handle until all safety precautions have been read and understood. 已阅读并理解所有的安全预防措施之前,切勿操作。
- P203
- P210 Keep away from heat/sparks/open flames/hot surfaces. — No smoking. 远离热源/火花/明火/热的表面。——禁止吸烟。
- P233 Keep container tightly closed. ?保持容器密闭。
- P240 Ground/bond container and receiving equipment. 与地面接触/连接集装箱和接受设备。
- P241 Use explosion-proof electrical/ventilating/lighting/…/equipment. 使用防爆电气/通风/照明/ .../设备。
- P242 Use only non-sparking tools. 只能使用无火花工具。
- P243 Take precautionary measures against static discharge. 采取预防措施,防止静电放电。
- P260 Do not breathe dust/fume/gas/mist/vapours/spray. 不要吸入粉尘/烟/气体/烟雾/蒸汽/喷雾。
- P261 Avoid breathing dust/fume/gas/mist/vapours/spray. 避免吸入粉尘/烟/气体/烟雾/蒸汽/喷雾。
- P262 Do not get in eyes, on skin, or on clothing. 不要接触眼睛,皮肤或衣服。
- P264 Wash hands thoroughly after handling. 处理后要彻底洗净双手。
- P264+P265
- P271 Use only outdoors or in a well-ventilated area.? 只能在室外或通风良好的地方使用。
- P272 Contaminated work clothing should not be allowed out of the workplace. 污染的工作服不得带出工作场所。
- P273 Avoid release to the environment. 避免释放到环境中。
- P280 Wear protective gloves/protective clothing/eye protection/face protection. 戴防护手套/防护服/眼睛的保护物/面部保护物。
- P281 Use personal protective equipment as required. 使用所需的个人防护装备。
- P302+P350
- P302+P352
- P302+P352+P333+P313+P362+P364
- P303+P361+P353
- P304+P312
- P304+P340
- P305+P351+P338
- P308+P313
- P312 Call a POISON CENTER or doctor/physician if you feel unwell. 如果你感觉不适,呼叫解毒中心或医生/医师。
- P314 Get medical advice/attention if you feel unwell. 获取医疗咨询/就医,如果你觉得不舒服
- P317
- P318
- P319
- P321 Specific treatment (see … on this label). 具体治疗(见本标签上的)。
- P332+P313
- P332+P317
- P333+P313
- P337+P313
- P337+P317
- P362 Take off contaminated clothing and wash before reuse. 脱掉污染的衣服,清洗后方可重新使用
- P362+P364
- P363 Wash contaminated clothing before reuse. 被污染的衣服洗净后方可重新使用。
- P370+P378
- P391 Collect spillage. Hazardous to the aquatic environment 收集对水环境有危害的泄漏物。
- P403+P233
- P403+P235
- P405 Store locked up. 上锁保管。
- P501 Dispose of contents/container to..… 处理内容物/容器.....
GHS Symbol
- R36/37/38 Irritating to eyes, respiratory system and skin 对眼睛、呼吸系统和皮肤有刺激性
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 3390 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Skin and Appendages - hair REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13(Suppl 2),209,1985
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Skin and Appendages - hair REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13(Suppl 2),209,1985
TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXP
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >1 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13(Suppl 2),209,1985
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >1 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume
TYPE OF TEST : Mutation test systems - not otherwise specified TEST SYSTEM : Rodent - mouse Leukocyte DOSE/DURATION : 615 umol/L REFERENCE : CCCCAK Collection of Czechoslovak Chemical Communications. (Academic Press Inc. Ltd., 24-28 Oval Rd., London NW1 7DX, UK) V.1- 1929- Volume(issue)/page/year: 49,2551,1984
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE : 5950 mg/kg SEX/DURATION : male 14 week(s) pre-mating female 2 week(s) pre-mating - 7 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) REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 13(Suppl 2),469,1985
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE : 1100 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : YACHDS Yakuri to Chiryo.
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE : 550 mg/kg SEX/DURATION : female 7-17 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 REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972-
其他信息
- 用途一:氟尿嘧啶类抗肿瘤药,为氟尿嘧啶的前体药物。在肿瘤组织内存在着的胸腺嘲嚏核苷磷酸化酶,对其进行作用而使其在肿瘤内转化为氟尿嘧啶,从而发挥抗肿瘤的作用。其抗肿瘤的专一性较强,毒性较低。临床用于胃癌、结肠直肠癌、乳腺癌,缓解率可达30%以上。
- MOL 文件:3094-09-5.mol
- 方法一:50g(191mmo1)的5-氟尿嘧啶核苷和39.3g对甲苯磺酸单水合物悬浮于750ml丙酮和94m12,2-二甲氧基丙烷中,在室温下搅拌50min至澄清,加入过量的碳酸氢钠固体,继续搅拌至中性。过滤,滤饼用丙酮洗,洗液和滤液一起蒸发至干,剩余物用2L醋酸乙酯重结晶,得48g 5-氟尿嘧啶核苷的缩酮化物,收率83%,熔点196~197℃。 上述46.4g(153.5mmo1)的5-氟尿嘧啶核苷的缩酮化物溶于250ml二甲基甲酰胺中,加入86.7g三苯磷甲基碘化合物,在室温下放置50min。加入250ml甲醇,放置30min后,蒸去溶剂。剩余的油状物用1L醋酸乙酯和1L 5%的硫代硫酸钠水溶液一起摇晃,静置分层。分出的醋酸乙酯层用2×1L水洗,无水硫酸钠干燥过夜,蒸发至干。剩余的油状物用醋酸乙酯重结晶,得52.9g的5’-去氧-5’-碘代-2’,3’-O-异丙亚基-5-氟尿嘧啶核苷,收率85%,熔点202~203.5℃。 上述得到的氟尿衍生物24g溶于800ml甲醇和15ml三乙胺中,在12g 5%钯-炭催化剂存在下,于常压、室温和剧烈搅拌下加氢还原90min。过滤除去催化剂,并用甲醇洗。洗液和滤液一起蒸发至干,剩余物和200ml醋酸乙酯搅拌1h。过滤除去形成的结晶,滤液蒸发掉一半的溶剂,放置过夜,再次过滤除去结晶。滤液减压蒸至干,得到的5'-去氧-2’,3’-O-异丙亚基-5-氟尿嘧啶核苷和200ml90%的三氟乙酸水溶液反应1h。反应蒸发至干,加入乙醇,共沸除去水和三氟乙酸,并蒸发至干。剩余物用醋酸乙酯重结晶,得11.35g的去氧氟尿苷,收率79%,熔点189~190℃。
- Hazard Note:Irritant
- 上游原料:乙酸乙酯 --> 碘甲烷 --> 对甲苯磺酸水合物 --> 钯炭催化剂 --> 三苯基锑 --> 2,2-二甲氧基丙烷
- TCI Shanghai:去氧氟尿苷 5'-Deoxy-5-fluorouridine,>;98.0%(T)(3094-09-5)
- 用途二:医药中间体。
- 去氧氟尿苷价格(试剂级):更新日期 产品编号 产品名称 包装 价格 2014/06/02 D3579 5'-脱氧-5-氟尿苷 5'-Deoxy-5-fluorouridine 5G 2710元 2014/06/02 D3579 5'-脱氧-5-氟尿苷 5'-Deoxy-5-fluorouridine 1G 900元
- 外观性质:白色结晶粉末。熔点:188-192 °C