cis-ジアンミン白金(II)ジクロリド

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

  H300：飲み込むと生命に危険

  H315：皮膚刺激

  H317：アレルギー性皮膚反応を起こすおそれ

  H319：強い眼刺激

  H334：吸入するとアレルギー、喘息または、呼吸困難 を起こすおそれ

  H335：呼吸器への刺激のおそれ

  H350：発がんのおそれ

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  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。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

cis-ジアンミン白金(II)ジクロリド 価格

MSDS Information

• Cisplatin

cis-ジアンミン白金(II)ジクロリド 化学特性,用途語,生産方法

• 外観

  わずかにうすい黄色〜黄色, 結晶性粉末〜粉末

• 溶解性

  水に溶けにくく、エタノール及びアセトンにほとんど溶けない。[溶解方法]　0.9% NaCl溶液に0.5mg/mlに溶解。使用時は実験に使用する溶液で希釈を行う。

• 解説

  シスプラチン,睾丸腫瘍，膀胱癌，卵巣癌などの化学療法剤として中心的な薬剤であり，構造式に白金を含む薬物。しかし，腎毒性や催吐作用など副作用も強いことがネックとなっていた。シスプラチンの副作用を軽減するために，カルボプラチンが開発され，日本では 1990年3月に承認が得られた。カルボプラチンは，すでに世界 30ヵ国で使用されており，シスプラチン投与時に必要な大量の水分負荷が不要なこと，蓄積毒性が少なく継続治療が可能であることから，その治療効果が注目されている。白金錯体 [PtCl2(NH3)2]2＋ のシス体．睾丸がん，卵巣がん，乳がんなどに有効であるが，トランス体には抗がん性はない．類似白金化合物として，カルボフラチンが臨床に用いられている．DNAに結合し，その複製を阻害する．

• 用途

  様々ながんに使用される細胞増殖抑制剤、抗がん剤

• 用途

  がん研究用試薬。

• 用途

  DNA 鎖内及び鎖間の白金 -DNA 架橋を形成し、DNA の複製及び転写阻 害作用を示します。

• 効能

  抗悪性腫瘍薬, 細胞増殖阻害薬

• 特徴

  平面四配位．シス体，トランス体とも，Pt－Cl 233 pm，Pt－N 201～205 pm

• 商品名

  アイエーコール (日本化薬); ランダ (日本化薬)

• 使用上の注意

  不活性ガス封入

• 化学的特性

  Cisplatin is a white powder or yellow crystalline solid with the melting point 268-272°C (decomposition). It is slightly soluble in water and easily soluble in dimethylformamide. In aqueous solution, it can be gradually transformed into trans-and hydrolysis.

• 使用

  Cisplatin is a cytostatic agent and it is used to treat various cancer types, including cancer of ovary, testis, lung, head, neck, bladder, neuroblastoma, and nephroblastoma, and Hodgkin’s disease and non-Hodgkin lymphoma.

• 調製方法

  Cisplatin is obtained by the method described by Kauffman and Cowan, in which potassium(II) tetrachloroplatinate is treated with buffered aqueous ammonia solution. Pure cisplatin is obtained by recrystallization from dilute hydrochloric acid.

• 適応症

  Cisplatin (Platinol) is an inorganic coordination complex with a broad range of antitumor activity. It is especially useful in the treatment of testicular and ovarian cancer. It binds to DNA at nucleophilic sites, such as the N7 and O6 of guanine, producing alterations in DNA structure and inhibition of DNA synthesis. Adjacent guanine residues on the same DNA strand are preferentially cross-linked. This platinating activity is analogous to the mode of action of alkylating agents. Cisplatin also binds extensively to proteins. It does not appear to be phase specific in the cell cycle.

• 定義

  ChEBI: Cisplatin is a diamminedichloroplatinum compound in which the two ammine ligands and two chloro ligands are oriented in a cis planar configuration around the central platinum ion. An anticancer drug that interacts with, and forms cross-links between, D A and proteins, it is used as a neoplasm inhibitor to treat solid tumours, primarily of the testis and ovary.

• 一般的な説明

  An anticancer drug. Orange-yellow to deep yellow solid or powder.

• 空気と水の反応

  Insoluble in water.

• 反応プロフィール

  Cisplatin is incompatible with oxidizing agents. Cisplatin is also incompatible with aluminum. Cisplatin may react with sodium bisulfite and other antioxidants.

• 火災危険

  Flash point data for Cisplatin are not available; however, Cisplatin is probably combustible.

• 応用例（製薬）

  CDDP, also referred to as cisplatinum or cisplatin, is a yellow powder and has found widespread use a chemotherapeutic agent.

• 生物活性

  Cisplatin is a platinum-containing compound that acts as a DNA-crosslinking agent and interferes with replication and transcription, culminating in apoptosis. It forms intra- and interstrand crosslinks with DNA with intrastrand guanine-to-guanine or guanine-to-alanine links accounting for the majority of DNA binding. Cisplatin halts the cell cycle at the G2/M phase in vitro and is active against murine tumors transplanted into mice and in mouse xenograft models, including a reduction in tumor growth in a model of squamous cell carcinoma of the head and neck when administered at doses ranging from 7.5 to 12.5 mg/kg. Cisplatin also inhibits the RecA recombinase of M. tuberculosis (IC50 = 2 μM), blocking protein splicing and cell growth. Formulations containing cisplatin have been used, alone and in combination therapy, in the treatment of a variety of cancers.

• 作用機序

  Cisplatin shows biphasic plasma decay with a distribution phase half-life of 25 to 49 minutes and an elimination half-life of 2 to 4 days. More than 90% of the drug is bound to plasma proteins, and binding may approach 100% during prolonged infusion. Cisplatin does not cross the blood-brain barrier. Excretion is predominantly renal and is incomplete.

• 臨床応用

  Cisplatin, combined with bleomycin and vinblastine or etoposide, produces cures in most patients with metastatic testicular cancer or germ cell cancer of the ovary. Cisplatin also shows some activity against carcinomas of the head and neck, bladder, cervix, prostate, and lung.

• 副作用

  Renal toxicity is the major potential toxicity of cisplatin. Severe nausea and vomiting that often accompany cisplatin administration may necessitate hospitalization. Cisplatin has mild bone marrow toxicity, yielding both leukopenia and thrombocytopenia. Anemia is common and may require transfusions of red blood cells. Anaphylactic allergic reactions have been described. Hearing loss in the high frequencies (4000 Hz) may occur in 10 to 30% of patients. Other reported toxicities include peripheral neuropathies with paresthesias, leg weakness, and tremors. Excessive urinary excretion of magnesium also may occur.

• 安全性プロファイル

  Confirmed carcinogen with experimental carcinogenic and tumorigenic data. Poison by ingestion, intramuscular, submtaneous, intravenous, and intraperitoneal routes. Human systemic effects: change in audttory acuity, change in kidney tubules, changes in bone marrow, corrosive to skin, depressed renal function tests, hallucinations, nausea or vomiting. Experimental teratogenic and reproductive effects. Human mutation data reported. When heated to decomposition it emits very toxic fumes of Cland NOx. See also PLATINUM COMPOUNDS.

• 職業ばく露

  A potential danger to those involved in the manufacture, formulation and administration of this anticancer chemotherapy agent. Contact with water causes decomposition.

• 発がん性

  Cisplatin is reasonably anticipated to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in experimental animals.

• 代謝

  It is rapidly hydrated, resulting in a short plasma half-life of less than 30 minutes. It is eliminated predominantly via the kidney, but approximately 10% of a given dose undergoes biliary excretion. It is highly nephrotoxic and can cause significant damage to the renal tubules, especially in patients with preexisting kidney disease or one kidney or who are concurrently receiving other nephrotoxic drugs (e.g., cyclophosphamide or ifosfamide). Dosages should be reduced in any of the above situations. Clearance decreases with chronic therapy, and toxicities can manifest at a late date. To proactively protect patients against kidney damage, patients should be hydrated with chloride-containing solutions. Saline or mannitol diuretics can be administered to promote continuous excretion of the drug and its hydrated analogues. Sodium thiosulfate, which accumulates in the renal tubules, also has been used to neutralize active drug in the kidneys in an effort to avoid nephrotoxicity.

• 輸送方法

  UN2928 Toxic solids, corrosive, organic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials, 8-Corrosive material, Technical Name Required. UN3290 Toxic solid, corrosive, inorganic, n.o.s., Hazard class: 6.1; Labels: 6.1-Poisonous materials, 8-Corrosive material. UN3288 Toxic solids, inorganic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials, Technical Name Required. UN3249 Medicine, solid, toxic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials

• 純化方法

  Recrystallise it from dimethylformamide and check the purity by IR and UV-VIS spectroscopy. [Raudaschl et al. Inorg Chim Acta 78 143 1983.] HIGHLY TOXIC, SUSPECTED CARCINOGEN.

• 不和合性

  Aluminum reacts with cisplatin and decreases the drug’s effectiveness. Do not use any aluminum equipment to prepare or administer cisplatin.

• 廃棄物の処理

  Disposal of unused product must be undertaken by qualified personnel who are knowledgeable in all applicable regulations and follow all pertinent safety precautions including the use of appropriate protective equipment. For proper handling and disposal, always comply with federal, state, and local regulations

• 参考文献

  G.H.W. Milburn, M.R. Truter, J. Chem. Soc. A, 1966, 1609, DOI: 10.1039/J19660001609.

• 参考文献

  1) Van Waardenburg et al. (2004), Platinated DNA adducts enhance poisoning of DNA topoisomerase I by camptothecin; J. Biol. Chem,, 279 54502 DOI:10.1074/JBC.M410103200
  2) Siddik et al. (2003), Cisplatin: mode of cytotoxic action and molecular basis of resistance; Oncogene, 22 7265 DOI:10.1038/sj.onc.1206933
  3) Seki et al. (2000), Cisplatin (CDDP) specifically induces apoptosis via sequential activation of caspase-8, -3 and -6 in osteosarcoma; Cancer Chemother. Pharmacol., 45 199 DOI:10.1007/s002800050030
  4) Nomura et al. (2004), Cisplatin inhibits the expression of X-linked inhibitor of apoptosis protein in human LNCaP cells; Urol. Oncol., 22 453 DOI:10.1016/J.UROLONC.2004.04.035
  5) Raghavan et al. (2015), Dimethylsulfoxide inactivates the anticancer effect of cisplatin against myelogenous leukemia cell lines in in vitro assays.; Indian J. Phamracol., 47 322 DOI:10.4103/0253-7613.157132
  6) Synthesis of Essential Drugs (2006, Elsevier) - libgen.lc
  7) Sittig's Pharmaceutical Manufacturing Encyclopedia
  8) Patty's Toxicology 6-Volume Set-Wiley (2012)
  9) Modern pharmacology with clinical applications (2004, LWW)

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