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カペシタビン

カペシタビン 化学構造式
154361-50-9
CAS番号.
154361-50-9
化学名:
カペシタビン
别名:
カペシタビン;5'-デオキシ-5-フルオロ-N4-[(ペンチルオキシ)カルボニル]シチジン;カペシチビン;カペシタビン (JAN)
英語化学名:
Capecitabine
英語别名:
XELODA;CS-1964;Captabin;RO-9-1978;Chi Pei he;Ro 09-1978;Capcitabine;Cpecitabine;CAPECITABINE;Capecitibine
CBNumber:
CB1324457
化学式:
C15H22FN3O6
分子量:
359.35
MOL File:
154361-50-9.mol

カペシタビン 物理性質

融点 :
110-121°C
比重(密度) :
1.49±0.1 g/cm3(Predicted)
闪点 :
87℃
貯蔵温度 :
2-8°C
溶解性:
H2O: soluble10mg/mL, clear (warmed)
外見 :
powder
酸解離定数(Pka):
5.41±0.40(Predicted)
色:
white to beige
Merck :
14,1754
InChIKey:
GAGWJHPBXLXJQN-UORFTKCHSA-N
CAS データベース:
154361-50-9(CAS DataBase Reference)
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  45-60-61-68
Sフレーズ  53-22-36/37-45
WGK Germany  3
RTECS 番号 HA3852500
HSコード  29349990
有毒物質データの 154361-50-9(Hazardous Substances Data)
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
H341 遺伝性疾患のおそれの疑い 生殖細胞変異原性 2 警告 P201,P202, P281, P308+P313, P405,P501
H350 発がんのおそれ 発がん性 1A, 1B 危険
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。
P281 指定された個人用保護具を使用すること。
P308+P313 暴露または暴露の懸念がある場合:医師の診断/手当てを 受けること。

カペシタビン 価格 もっと(29)

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) W01FLC048966 カペシチビン
Capecitibine
154361-50-9 1g ¥6300 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01FLC048966 カペシチビン
Capecitibine
154361-50-9 5g ¥6900 2021-03-23 購入
東京化成工業 C2878 カペシタビン >98.0%(HPLC)(T)
Capecitabine >98.0%(HPLC)(T)
154361-50-9 1g ¥11300 2021-03-23 購入
東京化成工業 C2878 カペシタビン >98.0%(HPLC)(T)
Capecitabine >98.0%(HPLC)(T)
154361-50-9 5g ¥39200 2021-03-23 購入
Sigma-Aldrich Japan Y0001642 European Pharmacopoeia (EP) Reference Standard
Capecitabine European Pharmacopoeia (EP) Reference Standard
154361-50-9 ¥35200 2021-03-23 購入

カペシタビン MSDS


Capecitabine

カペシタビン 化学特性,用途語,生産方法

外観

白色~ほとんど白色、結晶性粉末~粉末又は塊

溶解性

ベンジルアルコール及びエタノール(99.5)に溶けやすく、水にやや溶けにくい。

用途

生体内で 5- フルオロウラシ ルへと代謝されて DNA 合成阻害作用を示し ます。

用途

カペシタビン(Capecitabine)とは、フッ化ピリミジン系代謝拮抗剤に類する抗悪性腫瘍剤(抗がん剤)。 フッ化ピリミジン系抗悪性腫瘍剤の代表ともいえるフルオロウラシル(5-FU)は、これまで乳癌や消化器癌の治療に最も多く使われてきた抗がん剤の一つであるが、カペシタビンは、骨髄細胞や消化管では活性体になりにくく腫瘍組織内でより選択的に5-FUを生成することを目的として、日本ロシュ研究所(現中外製薬株式会社鎌倉研究所)で創製された。

効能

抗悪性腫瘍薬, 代謝拮抗薬

商品名

カペシタビン (ダイト); カペシタビン (日医工); カペシタビン (東和薬品); ゼローダ (中外製薬)

使用上の注意

不活性ガス封入

説明

Capecitabine is a new oral fluoropyrimidine carbamate for patients with advanced neoplastic disease, approved as Xeloda for the treatment of refractory metastatic breast cancer after failure on Paclitaxel and an anthracycline-based chemotherapy regimen ; it is a prodrug of doxifluridine (5-fluorouracil ; 5-FU) activated by a cascade of 3 enzymes concentrated in human liver and cancer tissue, resulting in the selective release of 5-FU at the tumor site and offering a prolonged tumour exposure to 5-FU. Oral Capecitabine passes intact through the intestinal mucosa, is converted first by carboxylesterase to 5'-deoxy-5- fluorocytidine in the liver, then by cytidine deaminase to 5'-deoxy-5-fluorouridine in the liver and tumour tissues and finally by thymidine phosphorylase to 5-FU in tumors. Therefore, Xeloda is much safer and more effective than 5-FU (for example, in the HCT116 human colon cancer and the MX-1 breast cancer xenograft .models).

化学的特性

Colourless solid

Originator

Roche (Switzerland)

使用

An antineoplastic agent. A prodrug of doxifluridine.

使用

Capecitabine is an antineoplastic agent. Capecitabine is a prodrug of Doxifluridine (D556750).

使用

An antiproliferative 5-fluorouracil releasing compound

定義

ChEBI: A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted to its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agen used in the treatment of cancers.

Manufacturing Process

5-Deoxy-5-fluoro-N4-((n-pentyloxy)carbonyl)cytidine may be prepared according to US Patent No. 6,114,520.
From 2',3'-bis-O-(tert-butyldimethylsilyl)-5'-deoxy-5-fluorocytidine and n-pentylchloroformate in dichloromethane and pyridine may be obtained 2',3'- bis-O-(tert-butyldimethylsilyl)-5'-deoxy-5-fluoro-N4-((pentyloxy)carbonyl) cytidine.From 2',3'-bis-O-(tert-butyldimethylsilyl)-5'-deoxy-5-fluoro-N4- ((pentyloxy)carbonyl)cytidineand tetrabutylammonium fluoride in tetrahydrofuran at room temperature for 2 hours may be prepared the product which by hydrolyses may be converted to 5-deoxy-5-fluoro-N4- ((pentyloxy)carbonyl)cytidine. Purification of the product may be carried out by silica gel chromatography (using dichloromethane:methanol = 20:1 as an eluent).

brand name

Xeloda (Roche).

Therapeutic Function

Antitumor

一般的な説明

The drug is available in a 150- and 500-mg tablets for oraluse. This drug is a fluoropyrimidine carbamate prodrugform of 5-fluorouracil (5-FU). It is used to treat breast cancerand colorectal cancer. The drug is converted to 5-FU bythe enzyme thymidine phosphorylase following esterase activity to hydrolyze the carbamate moiety and deamination.Capecitabine is readily absorbed by the GI tract, and peakplasma levels of 5-FU occur about 2 hours after oral administration.Indications, drug interactions, and toxicities areequivalent to those of 5-FU.

Biochem/physiol Actions

Capecitabine is an anti-cancer drug, a prodrug of doxifluridine, metabolized to 5-fluorouracil at the tumor site. The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5′-Deoxy-5-fluorocytidine (5′-DFCR) and 5′-Deoxy-5-fluorouridine (5′-DFUR), to form 5-fluorouracil.

臨床応用

Capecitabine is indicated for use as first-line therapy in patients with colorectal cancer. It also is used alone or in combination with docetaxel in patients with metastatic breast cancer who have experienced disease progression or recurrence after anthracycline therapy. Given b.i.d. in tablet form, the total daily dose is calculated based on patient body surface area and is taken 30 minutes after eating to avoid food-induced decreases in absorption. In addition to bone marrow suppression, nausea, and vomiting, the drug can induce severe diarrhea and a potentially disabling disorder termed “hand-and-foot syndrome” (palmar-plantar erythrodysethesia). Capecitabine inhibits CYP2C9 and, along with competition for serum protein binding sites, results in clinically significant drug–drug interactions with both warfarin and phenytoin.

代謝

Although capecitabine is a carbamylated analogue of cytidine , the drug actually is another 5-fluoro-dUMP prodrug. Given orally, it is extensively metabolized to fluorouracil, which is then converted to the active fluorinated deoxyribonucleotide as previously described. Thymidine phosphorylase, an enzyme involved in this biotransformation, is much more active in tumors than in normal tissue, which improves the tumor-selective generation of fluorouracil. Levels of active drug in the tumor can be up to 3.5-fold higher than in surrounding tissue, leading to a lower incidence of side effects compared to fluorouracil therapy. Because capecitabine is biotransformed to fluorouracil, it follows the same catabolic and elimination pathways reported for 5-fluorouracil.

カペシタビン 上流と下流の製品情報

原材料

準備製品


カペシタビン 生産企業

Global( 611)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
Shenzhen Shengda Pharma Limited
+86-755-85269922
WeChat:shengdapharm sales@shengdapharm.com CHINA 310 58
AFINE CHEMICALS LIMITED
008657185134551
008657185134895 info@afinechem.com CHINA 15559 58
Jinan Ande Pharmaceutical Co.,Ltd.
+8613256107535
andepharm@163.com CHINA 220 58
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20012 60
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55
Shanghai Time Chemicals CO., Ltd.
+8618017249410 +86-021-57951555
+86-021-57951555 jack.li@time-chemicals.com China 1807 55
Guangzhou PI PI Biotech Inc
+8618371201331
020-81716319 sales@pipitech.com;87478684@qq.com China 3284 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
Hubei XinRunde Chemical Co., Ltd.
+8615102730682
02783214688 bruce@xrdchem.cn CHINA 567 55

154361-50-9(カペシタビン)キーワード:


  • 154361-50-9
  • Capcitabine
  • 5'-DEOXY-5-FLUOROCYTISINE
  • 5'-DEOXY-5-FLUORO-N-[(PENTYLOXY)CARBONYL]CYTIDINE
  • Pentyl (1-((2R,3R,4S,5R)-3,4-dihydroxy-5-methyltetrahydrofuran-2-yl)-5-fluoro-2-oxo-1,2-dihydr
  • RO-9-1978
  • pentyl [1-(3,4-dihydroxy-5-methyl-oxolan-2-yl)-5-fluoro-2-oxo-pyrimidin-4-yl]aminoformate
  • XELODA
  • CAPECITABINE
  • Cpecitabine
  • 5Deoxy-5-fluoro-N-[(pentyloxy)carbonyl]cytidine, Ro-9-1978, Xeloda
  • Cytidine, 5'-deoxy-5-fluoro-N-[(pentyloxy)carbonyl]-
  • 5''-Deoxy-5-fluoro-N4-(pentyloxycarbonyl)cytidine
  • Capecitabines CAS 154361-50-9
  • Capecitabine Pentyl [1-(3,4-dihydroxy-5-methyl-oxolan-2-yl)-5-fluoro-2-oxo-pyrimidin-4-yl]aminoformate
  • Capecitabine, >=98%
  • Chi Pei he
  • CS-1964
  • (158798-73-3) capecitabine
  • pentyl N-{1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-methyloxolan-2-yl]-5-fluoro-2-oxo-1,2-dihydropyrimidin-4-yl}carbamate
  • Capecitabine*( CEP available)
  • Capecitabine Ready Made Solution
  • Capecitabine(CEP)
  • Ro 09-1978
  • Ro 09-1978/000
  • 5''-DEOXY-5-FLUORO-N-[(PENTYLOXY)CARBONYL]CYTIDINE (CAPECITABINE)
  • Capecitabine (200 mg)
  • Capecitibine
  • Capecitabine(Xeloda)
  • Capecitabine, USP
  • pentyl N-{1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxyMethyl)oxolan-2-yl]-5-fluoro-2-oxo-1,2-dihydropyriMidin-4-yl}carbaMate
  • カペシタビン
  • 5'-デオキシ-5-フルオロ-N4-[(ペンチルオキシ)カルボニル]シチジン
  • カペシチビン
  • カペシタビン (JAN)
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