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カルボプラチン

カルボプラチン 化学構造式
41575-94-4
CAS番号.
41575-94-4
化学名:
カルボプラチン
别名:
カルボプラチン;cis-ジアミン(1,1-シクロブタンジカルボキシラト)白金(II);1,1-シクロブタンジカルボシラトジアンミン白金(II);カルボプラチン (JP17)
英語化学名:
Carboplatin
英語别名:
JM-8;Ercar;cbdca;CarbopL;Carboplat;PARAPLATIN;nsc-241240;CARBOPLATIN;Carbopaltin;Carboplotin
CBNumber:
CB6702418
化学式:
C6H12N2O4Pt
分子量:
371.25
MOL File:
41575-94-4.mol

カルボプラチン 物理性質

融点 :
228-230°C
貯蔵温度 :
2-8°C
溶解性:
Sparingly soluble in water, very slightly soluble in acetone and in ethanol (96 per cent).
外見 :
crystal
色:
white
水溶解度 :
Soluble in water.
Merck :
14,1822
安定性::
Stable. Incompatible with strong oxidizing agents.
EPAの化学物質情報:
Carboplatin (41575-94-4)
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
主な危険性  T
Rフレーズ  46-61-20/21/22-42/43-20/21
Sフレーズ  53-22-26-36/37/39-45
RIDADR  2811
WGK Germany  3
RTECS 番号 TP2300000
HSコード  28439000
有毒物質データの 41575-94-4(Hazardous Substances Data)
毒性 LD50 in mice (mg/kg): 150 i.p., 140 i.v.; in rats (mg/kg): 85 i.v. (Lelieveld)
絵表示(GHS)
注意喚起語 Danger
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H302 飲み込むと有害 急性毒性、経口 4 警告 P264, P270, P301+P312, P330, P501
H312 皮膚に接触すると有害 急性毒性、経皮 4 警告 P280,P302+P352, P312, P322, P363,P501
H315 皮膚刺激 皮膚腐食性/刺激性 2 警告 P264, P280, P302+P352, P321,P332+P313, P362
H317 アレルギー性皮膚反応を起こすおそれ 感作性、皮膚 1 警告 P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 P264, P280, P305+P351+P338,P337+P313P
H332 吸入すると有害 急性毒性、吸入 4 警告 P261, P271, P304+P340, P312
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 感作性、呼吸器 1 危険 P261, P285, P304+P341, P342+P311,P501
H340 遺伝性疾患のおそれ 生殖細胞変異原性 1A, 1B 危険
H360 生殖能または胎児への悪影響のおそれ 生殖毒性 1A, 1B 危険
注意書き
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。
P271 屋外または換気の良い場所でのみ使用すること。
P501 内容物/容器を...に廃棄すること。

カルボプラチン 価格 もっと(25)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01BVI1553-100
Carboplatin
41575-94-4 100mg ¥75000 2020-09-21 購入
富士フイルム和光純薬株式会社(wako) W01CHDASB-00003165 カルボプラチン
Carboplatin
41575-94-4 10mg ¥43700 2018-12-26 購入
東京化成工業 C2043 カルボプラチン >98.0%(HPLC)
Carboplatin >98.0%(HPLC)
41575-94-4 100mg ¥10100 2021-03-23 購入
東京化成工業 C2043 カルボプラチン >98.0%(HPLC)
Carboplatin >98.0%(HPLC)
41575-94-4 1g ¥47600 2021-03-23 購入
Sigma-Aldrich Japan BP711 British Pharmacopoeia (BP) Reference Standard
Carboplatin British Pharmacopoeia (BP) Reference Standard
41575-94-4 ¥36200 2021-03-23 購入

カルボプラチン 化学特性,用途語,生産方法

外観

白色~灰色、結晶性粉末~粉末

溶解性

水にやや溶けにくく、アセトン及びエタノール(99.5)に極めて溶けにくい。

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

商品名

パラプラチン (ブリストル・マイヤーズスクイブ)

説明

Carboplatin is a second generation, platinum-containing antineoplastic agent with significantly reduced nephro-, neuro-, and ototoxicity in comparison to cisplatin. It is effective in the treatment of advanced ovarian carcinoma of epithelial origin and small cell carcinoma of the lung.

化学的特性

White Crystals

Originator

Johnson Matthey (United Kingdom)

使用

Data on carboplatin production have not been found. Carboplatin is used in chemotherapy to treat cancer, and more particularly to treat cancer of ovary, embryonal carcinoma of the testis, microcellular carcinoma of the lung, neuroblastoma, and squamous cell carcinomas of the head and neck.

使用

Analog of Cisplatin with reduced nephrotoxicity. Antineoplastic

使用

anthelmintic

使用

antitumor agent,

適応症

Carboplatin (Paraplatin) is an analogue of cisplatin. Its plasma half-life is 3 to 5 hours, and it has no significant protein binding. Renal excretion is the major route of drug elimination.
Despite its lower chemical reactivity, carboplatin has antitumor activity that is similar to that of cisplatin against ovarian carcinomas, small cell lung cancers, and germ cell cancers of the testis. Most tumors that are resistant to cisplatin are cross-resistant to carboplatin.
The major advantage of carboplatin over cisplatin is a markedly reduced risk of toxicity to the kidneys, peripheral nerves, and hearing; additionally, it produces less nausea and vomiting. It is, however, more myelosuppressive than cisplatin. Other adverse effects include anemia, abnormal liver function tests, and occasional allergic reactions.

Manufacturing Process

cis-Diammine platinum diiodide was reacted with silver sulfate to give cis-diaquodiammine platinum sulfate. This was reacted with the barium salt of 1,1-cyclobutanedicarboxylic acid to yield Carboplatin.

brand name

Paraplatin (Bristol-Myers Squibb).

Therapeutic Function

Antitumor

一般的な説明

Carboplatin is available in 50-, 150-, and 450-mg vials for IVadministration in the treatment of ovarian cancer, bladdercancer, germ cell tumors, head and neck cancers, small celllung cancer, and NSCLC. Activation of the agent occurs byaquation in a manner similar to that seen for cisplatin. Thepresence of the chelating 1,1-cyclobutane-dicarboxylateslows this reaction 100-fold and reduces the toxicity of theagent. The sites of alkylation and mechanisms of resistanceare like those seen for cisplatin, and the two agents showcross-resistance. The agent is widely distributed upon IV administration but, because of its greater stability, it bindsslowly to plasma proteins, requiring 24 hours to reach 90%bound drug compared with 4 hours for cisplatin. The agent iseliminated in the urine with a terminal elimination half-lifeof 2 to 6 hours. Adverse effects include myelosuppression,which is dose limiting. Other adverse effects include renaltoxicity, nausea, vomiting, and peripheral neuropathy, butthese occur much less frequently than with cisplatin.

応用例(製薬)

Carboplatin, cis-diammine(1,1-cyclobutanedicarboxylato)platinum(II), is a second-generation platinum drug. Its structure is based on cisplatin with the difference that the chloride ligands are exchanged for a bidentate chelating ligand. A consequence is that carboplatin is less reactive than cisplatin and therefore is less nephrotoxic and orthotoxic than the parent compound. Unfortunately, it is more myelosuppressive than cisplatin, which reduces the patients’ white blood cell count and makes them susceptible to infections. Carboplatin was licensed by the FDA in 1989 under the brand name Paraplatin and has since then gained worldwide recognition. Carboplatin on its own or in combination with other anticancer agents is used in the treatment of a variety of cancer types including head and neck, ovarian, small-cell lung, testicular cancer and others.
Carboplatin is a pale-white solid showing good aqueous solubility. The synthesis starts with potassium tetrachloroplatinate, which is reacted to the orange [PtI4]2- anion.

生物活性

Antitumor agent that forms platinum-DNA adducts. Causes intra- and interstrand DNA crosslinks blocking DNA replication and transcription. Enhances radiation-induced single-strand DNA breakage and displays lower nephrotoxicity than analog cisplatin (cis-Diaminodichloroplatinum ).

Biochem/physiol Actions

Carboplatin is a platinum-based antineoplastic drug that damages DNA by forming intrastrand cross-links with neighboring guanine residues. Tumors acquire resistance to these drugs through the loss of DNA-mismatch repair (MMR) activity and the resultant decrease in the induction of programmed cell death.

作用機序

Carboplatin, another square planar Pt(II) complex, forms the same cytotoxic hydrated intermediate as cisplatin but does so at a slower rate, making it a less potent chemotherapeutic agent.

臨床応用

This drug induces fewer nonhematological toxicities (e.g., emesis, nephrotoxicity, and ototoxicity) compared to cisplatin, and it is approved for use only in the treatment of ovarian cancer. Unlabeled uses include combination therapy in lung, testicular, and head and neck cancers.

副作用

The ultimate damage done to cells as a result of carboplatin use, however, approaches that of cisplatin. The plasma half-life of carboplatin is 3 hours, and the drug is less extensively bound to serum proteins. Excretion is predominantly renal, and doses must be reduced in patients with kidney disease. Suppression of platelets and white blood cells is the most significant toxic reaction of carboplatin use.

Chemical Synthesis

Carboplatin, cis-diamino-(1,1-cyclobutandicarboxylate)platinum(II), is made from cisplatin by reacting it with a solution of silver nitrate, and then with cyclobutan-1,1-dicarboxylic acid to form the desired carboplatin (30.2.5.2).

Veterinary Drugs and Treatments

Like cisplatin, carboplatin may be useful in a variety of veterinary neoplastic diseases including squamous cell carcinomas, ovarian carcinomas, mediastinal carcinomas, pleural adenocarcinomas, nasal carcinomas and thyroid adenocarcinomas. Carboplatin’s primary use currently in small animal medicine is in the adjunctive treatment (post amputation) of osteogenic sarcomas. Its effectiveness in treating transitional cell carcinoma of the bladder has been disappointing; however, carboplatin may have more efficacy against melanomas than does cisplatin.
Carboplatin, unlike cisplatin, appears to be relatively safe to use in cats.
Carboplatin may be considered for intralesional use in conditions such as equine sarcoids or in treating adenocarcinoma in birds.
Whether carboplatin is more efficacious than cisplatin for certain cancers does not appear to be decided at this point, but the drug does appear to have fewer adverse effects (less renal toxicity and reduced vomiting) in dogs.

カルボプラチン 上流と下流の製品情報

原材料

準備製品


カルボプラチン 生産企業

Global( 412)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales04@yibaibiotech.com CHINA 420 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com China 9165 55
Guangzhou PI PI Biotech Inc
+8618371201331
020-81716319 sales@pipitech.com;87478684@qq.com China 3284 55
Shanxi Naipu Import and Export Co.,Ltd
+8613734021967
kaia@neputrading.com CHINA 1011 58
career henan chemical co
+86-0371-55982848
sales@coreychem.com China 29953 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58
Shenzhen Nexconn Pharmatechs Ltd
15013857715
admin@nexconn.com CHINA 3004 58
Hebei Jimi Trading Co., Ltd.
+86 319 5273535
bestoneforyou@sina.com CHINA 292 58
Accela ChemBio Inc.
(+1)-858-699-3322
(+1)-858-876-1948 info@accelachem.com United States 19969 58

41575-94-4(カルボプラチン)キーワード:


  • 41575-94-4
  • PARAPLATIN
  • 1,1-cyclobutanedicarboxylatediammineplatinum(ii)
  • 1-cyclobutanedicarboxylato(2-)-o,o’)-diammine((sp-4-2)-platinu
  • 1-cyclobutanedicarboxylato)diammine-(cis-platinum(ii
  • DIAMMINE(1,1-CYCLOBUTANEDICARBOXYLATO)PLATINUM(II)
  • CARBOPLATIN
  • CARBOPLATINUM
  • CIS-DIAMINE(1,1-CYCLOBUTANEDICARBOXYLATO)PLATINUM
  • CIS-DIAMINE(1,1-CYCLOBUTANEDICARBOXYLATO)PLATINUM(II)
  • CIS-DIAMMINE-[1,1-CYCLOBUTANE-DICARBOXYLATO]PLATIN
  • CIS-DIAMMINE[1,1-CYCLOBUTANE-DICARBOXYLATO] PLATINUM
  • CIS-DIAMMINE [1,1-CYCLOBUTANEDICARBOXYLATO] PLATINUM (II)
  • CIS-DIAMMINE[1,1-CYCLOBUTANE-DICARBOYLATO]PLATINUM
  • JM-8
  • 1,1-CYCLOBUTANEDICARBOXYLATODIAMMINEPLATINUM(II)
  • 1,1-Cyclobutanedicarboxylate diamine platinum(II)
  • cis-(1,1-Cyclobutanedicarboxylato)diamineplatinum(II)
  • diammine(1,1-cyclobutanedicarboxylato)-platinum(I
  • Platinum, diamine(1,1-cyclobutanedicarboxylato(2-)-O,O')-, (SP-4-2)-
  • diammine[cyclobutane-1,1-dicarboxylato(2-)-O,O']platinum
  • Carboplatin usp25
  • Carbopaltin
  • Carboplatin99%
  • CarboplatinUsp24
  • CarboplatinUsp28
  • (SP-4-2)-Diamimine[1,1-cyclobutanedi(carboxylato-kO)(2-)]platinum
  • 1,1-Cyclobutanedicarboxylatodiammineplatinum(II),99%CARBOPLATIN
  • Platinum, diammine1,1-cyclobutanedi(carboxylato-.kappa.O)(2-)-, (SP-4-2)-
  • CARBONPLATIN
  • 1,1-cyclobutanedicarboxylate diammine platinum
  • カルボプラチン
  • cis-ジアミン(1,1-シクロブタンジカルボキシラト)白金(II)
  • 1,1-シクロブタンジカルボシラトジアンミン白金(II)
  • カルボプラチン (JP17)
  • シクロブタン & シクロブテン
  • 白金化合物
  • 構造分類
  • 金属別化合物
  • 遷移金属化合物
  • 生化学
  • 試験研究用抗腫瘍剤
  • 四員環化合物
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