5-フルオロウラシル

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H301：飲み込むと有毒

  H351：発がんのおそれの疑い

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ と。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P310：飲み込んだ場合：直ちに医師に連絡すること。

5-フルオロウラシル 価格

MSDS Information

• 5-Fluoropyrimidine-2,4-dione

5-フルオロウラシル 化学特性,用途語,生産方法

• 外観

  白色, 結晶～粉末

• 溶解性

  ジメチルホルムアミドに溶けやすく、水にやや溶けにくく、エタノールに溶けにくく、アセトンにほとんど溶けない。

• 解説

  フルオロウラシル，化学式はC4II3FN2O2，核酸塩基ウラシルの５位の水素をフッ素原子で置換した誘導体で，代表的な抗癌剤の一つ。ウラシルをフッ素化すると得られる．白色の結晶．分解点280～282 ℃．λmax 265～266 nm(ε 7070，pH 1.0)．水に難溶，DMFに易溶．抗悪性腫瘍剤で，消化器がん，乳がん治療薬として使用される．LD50 226 mg/kg(マウス，経口)．融点約280℃。水に微溶，エタノールに難溶。腫瘍細胞内でDNA合成を妨げて増殖を阻止，またRNAに取り込まれて異常タンパク質を合成させ，細胞を死亡させる。乳癌や消化器癌などに用いられる。

• 用途

  抗癌剤研究用。

• 用途

  人間と動物医療域の抗腫瘍剤(乳房と消化管)

• 用途

  チミジル酸シンターゼを阻害 することにより DNA 合成阻害作用を示しま す

• 用途

  チミジル酸シンターゼを阻害 することにより DNA 合成阻害作用を示しま す。

• 効能

  抗悪性腫瘍薬, 代謝拮抗薬

• 商品名

  5−FU (協和発酵キリン); 5−FU (協和発酵キリン); 5−FU (協和発酵キリン)

• 説明

  5-Fluorouracil (5-FU) is a prodrug form of the thymidylate synthase inhibitor fluorodeoxyuridylate (FdUMP). It is also converted to the active metabolites FUTP and FdUTP, which induce RNA and DNA damage, respectively. In vivo, 5-FU (15 mg/kg) when administered in combination with docetaxel reduces tumor growth in B88 and CAL 27 oral squamous cell carcinoma (OSCC) mouse xenograft models. Formulations containing 5-FU have been used in the treatment of colorectal, breast, gastric, and pancreatic cancers.

• 化学的特性

  White or almost white, crystalline powder

• 使用

  5-Fluorouracil is used as an antitumor agent in the treatment of anal, breast, colorectal, oesophageal, stomach, pancreatic and skin cancers. It finds application as a suicide inhibitor due to its irreversible inhibition of thymidylate synthase. It is also used in the treatment of actinic keratoses and bowen's disease. Further, it serves as a potent antineoplastic agent in clinical use. In addition to this, it acts as a DNA synthesis inhibitor.

• 適応症

  Fluorouracil (5-fluorouracil, 5-fluorouracil, Efudex, Adrucil) is a halogenated pyrimidine analogue that must be activated metabolically. The active metabolite that inhibits DNA synthesis is the deoxyribonucleotide 5-fluoro-2'deoxyuridine-S'-phosphate (FdUMP). 5- Fluorouracil is selectively toxic to proliferating rather than non-proliferating cells and is active in both the G1- and S-phases. The target enzyme inhibited by 5-fluorouracilfluorouracil is thymidylate synthetase.
  methylenetetrahydrofolate dihydrofolate The carbon-donating cofactor for this reaction is N⁵,N¹⁰ methylenetetrahydrofolate, which is converted to dihydrofolate. The reduced folate cofactor occupies an allosteric site on thymidylate synthetase, which allows for the covalent binding of 5-FdUMP to the active site of the enzyme.

• 一般的な説明

  White to nearly white crystalline powder; practically odorless. Used as an anti neoplastic drug, chemosterilant for insects.

• 空気と水の反応

  Insoluble in water.

• 反応プロフィール

  5-Fluorouracil may be sensitive to prolonged exposure to light. Solutions discolor on storage. 5-Fluorouracil can react with oxidizing agents and strong bases. Incompatible with methotrexate sodium.

• 危険性

  Questionable carcinogen.

• 健康ハザード

  Minimum toxic dose in humans is approximately 450 mg/kg (total dose) over 30 days for the ingested drug. Intravenous minimum toxic dose in humans is a total dose of 6 mg/kg over three days. Depression of white blood cells occurred after intravenous administrative of a total dose of 480 mg/kg over 32 days. Occasional neuropathy and cardiac toxicity have been reported. Do not use during pregnancy. Patients with impaired hepatic or renal function, with a history of high-dose pelvic irradiation or previous use of alkylating agents should be treated with extreme caution. Patients with nutritional deficiencies and protein depletion have a reduced tolerance to 5-Fluorouracil.

• 火災危険

  Emits very toxic fumes of flourides and nitrogen oxides when heated to decomposition. Avoid decomposing heat.

• 生物活性

  Anticancer agent. Metabolized to form fluorodeoxyuridine monophosphate (FdUMP), fluorodeoxyuridine triphosphate (FdUTP) and fluorouridine (FUTP). FdUMP inhibits thymidylate reductase causing a reduction in dTMP synthesis. FUTP and FdUTP are misincorporated into RNA and DNA respectively.

• 作用機序

  Another action proposed for 5-fluorouracil may involve the incorporation of the nucleotide 5-fluorouridine triphosphate (5-FUTP) into RNA. The cytotoxic role of these “fraudulent” 5-fluorouracil-containing RNAs is not well understood.
  Several possible mechanisms of resistance to 5-fluorouracil have been identified, including increased synthesis of the target enzyme, altered affinity of thymidylate synthetase for FdUMP, depletion of enzymes (especially uridine kinase) that activate 5-fluorouracil to nucleotides, an increase in the pool of the normal metabolite deoxyuridylic acid (dUMP), and an increase in the rate of catabolism of 5-fluorouracil.
  The drug has been administered orally, but absorption by this route is erratic. The plasma half-life of 5- fluorouracil after intravenous injection is 10 to 20 minutes. It readily enters CSF. Less than 20% of the parent compound is excreted into the urine, the rest being largely metabolized in the liver.

• 薬理学

  Local inflammatory reactions characterized by erythema, edema, crusting, burning, and pain are common (and, some would argue, desirable) but may be minimized by reduced frequency of application or use in combination with a topical corticosteroid.

• 臨床応用

  5-Fluorouracil (FU) is widely used in the treatment of a range of cancers including breast and cancers of the aerodigestive tract, but has had the greatest impact in colorectal cancer. 5-FU-based chemotherapy improves overall and disease-free survival of patients with resected stage III colorectal cancer. Nonetheless, response rates for 5-FU-based chemotherapy as a first-line treatment for advanced colorectal cancer are only between 10 and 15%. Combination of 5-FU with newer chemotherapies, such as irinotecan and oxaliplatin, has improved the response rates for advanced colorectal cancer to between 40 and 50%.

• 副作用

  Patients who are genetically deficient in this enzyme will experience a more pronounced effect from this drug and are at significant risk for use-limiting toxicity. In general, women clear fluorouracil faster than men do. Dosage adjustments usually are not required in hepatic or renal dysfunction. Major toxicities are related to bone marrow depression, stomatitis/esophagopharyngitis, and potential GI ulceration. Nausea and vomiting are common. Solutions of fluorouracil are light sensitive, but discolored products that have been properly stored and protected from light are still safe to use.

• 安全性プロファイル

  Poison by ingestion, intraperitoneal, subcutaneous, and intravenous routes. Moderately toxic by parented and rectal routes. Experimental teratogenic and reproductive effects. Human systemic effects: EKG changes, bone marrow changes, cardiac, pulmonary, and gastrointestinal effects. Human mutation data reported. A human skin irritant. Questionable carcinogen. When heated to decomposition it emits very toxic fumes of Fand NOx.

• 職業ばく露

  This material is used as an antineo plastic drug for cancer treatment and as a chemosterilant for insects.

• 輸送方法

  UN2811 Toxic solids, organic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials, Technical Name Required.

• 不和合性

  Incompatible with oxidizers (chlorates, nitrates, peroxides, permanganates, perchlorates, chlorine, bromine, fluorine, etc.); contact may cause fires or explo sions. Keep away from alkaline materials, strong bases, strong acids, oxoacids, epoxides, methotrexrate sodium, sources of heat.

5-フルオロウラシル 上流と下流の製品情報

5-フルオロウラシル 生産企業

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5-フルオロウラシル スペクトルデータ(¹HNMR、ESR、IR1、IR2、MS、Raman)

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