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ダサチニブ

ダサチニブ 化学構造式
302962-49-8
CAS番号.
302962-49-8
化学名:
ダサチニブ
别名:
ダサチニブ;ダサチニブ (JAN)
英語化学名:
Dasatinib
英語别名:
CS-1968;Dasatinib;BMS-354825;NCGC00181129;25MG/100MG/1G;Dasatinib, 95+%;sprycel Dasatinib;DASATINIB HCL 99%;Dasatinib Tablets;BMS-354825; SPRYCEL
CBNumber:
CB4506696
化学式:
C22H26ClN7O2S
分子量:
488.01
MOL File:
302962-49-8.mol

ダサチニブ 物理性質

融点 :
275-286°C
比重(密度) :
1.408±0.06 g/cm3(Predicted)
貯蔵温度 :
Sealed in dry,Store in freezer, under -20°C
外見 :
White powder.
酸解離定数(Pka):
10.94±0.70(Predicted)
CAS データベース:
302962-49-8(CAS DataBase Reference)

安全性情報

HSコード  29341000

ダサチニブ 価格

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

ダサチニブ 化学特性,用途語,生産方法

用途

ダサチニブ(dasatinib)は、BCR-ABLをはじめとした複数のチロシンキナーゼを標的とした、分子標的治療薬であるチロシンキナーゼ阻害薬(Tyrosine-Kinase Inhibitor:TKI)としてブリストル?マイヤーズ スクイブ社により開発された抗悪性腫瘍剤(抗がん剤)である。慢性骨髄性白血病 (CML)、および既存の治療に抵抗性または不耐容のフィラデルフィア染色体陽性急性リンパ性白血病 (Ph+ALL) の治療に用いられる。

効能

抗悪性腫瘍薬, チロシンキナーゼ阻害薬

説明

Dasatinib, developed and marketed by Bristol Myers, is the first approved oral tyrosine kinase inhibitor which binds to multiple conformations of ABL kinase for the treatment of two leukemia indications: chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Dasatinib is a highly potent, ATPcompetitive ATPcompetitive kinase inhibitor which, at nanomolar concentrations, inhibits BCR-ABL, SRC family, c-KIT, EPHA2 and PDGFR-B.

化学的特性

Pale-Yellow Solid

Originator

Bristol–Myers Squibb (US)

使用

A new, oral, small-molecule Tyrosine Kinase Inhibitor (TKI) for the treatment of CML. Antineoplastic

使用

Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.

使用

Directly targets wild-type and mutant c-Abl kinase domains

brand name

Sprycel (Bristol-Myers Squibb).

一般的な説明

Dasatinib is available in 20-, 50-, and 70-mg tablets fororal administration in the treatment of CML and ALL thatare Ph1 positive. Although dasatinib is more potent thanimatinib, bioavailability is much lower with values rangingbetween 14% to 34%. The agent is extensively metabolizedwith as many as 29 metabolites seen as result of oxidationby primarily CYP3A4 and phase II conjugation.The agent may act as an inhibitor of CYP3A4 andCYP2C8. Metabolism does give an active metabolite, but this accounts for only 5% of the total and is not believed tobe important for the overall activity of the agent. Dasatinibis 95% protein bound with a terminal half-life of 3 to5 hours. The majority of the drug and metabolites are eliminatedin the feces. The most common side effects are skinrash, nausea, diarrhea, and fatigue. Serious side effects includemyelosuppression appearing as neutropenia andthrombocytopenia, bleeding of the brain and GI tract, andfluid retention.

Chemical Synthesis

A concise and efficient route was developed for the synthesis of dasatinib. Reaction of 2-chlorothioa-zole (18) with n-butyllithium at low temperature followed by addition of 2-chloro-6-methylphenyl isocyanate (19) gave anilide 20 in 86% yield. The amide 20 was protected as corresponding 4-methoxy benzyl (PMB) anilide 22 in 95% yield which was subsequently reacted with 4- amino-6-chloro-2-methylpyrimidine (23) in the presence of sodium hydride in hot THF to give compound 24 in 83% yield. The PMB protecting group was then removed with triflic acid to give compound 25 in 99% yield. Compound 25 was reacted with 1-(2-hydroxyethyl)piperazine (26) in refluxing dioxane to give dasatinib (III) in 91% yield.

ダサチニブ 上流と下流の製品情報

原材料

準備製品


ダサチニブ 生産企業

Global( 407)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
Biocare Pharmaceutical Ltd
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AFINE CHEMICALS LIMITED
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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
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Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55
Hangzhou FandaChem Co.,Ltd.
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Guangzhou PI PI Biotech Inc
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020-81716319 sales@pipitech.com;87478684@qq.com China 3283 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26782 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 341 58
Shanxi Naipu Import and Export Co.,Ltd
+8613734021967
kaia@neputrading.com CHINA 1011 58

302962-49-8(ダサチニブ)キーワード:


  • 302962-49-8
  • SPRYCEL;BMS354825;DASATINIB (BMS 354825)
  • CS-1968
  • N-(2-chloro-6-Methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-Methyl-4-pyriMidinyl]aMino]-1,3-thiazole-5-carboxaMide
  • sprycel Dasatinib
  • BMS-354825; SPRYCEL
  • 25MG/100MG/1G
  • NCGC00181129
  • Dasatinib (Dasatinib Monohydrate) Tablet
  • Dasatinib (anhydrous)
  • Dasatinib, 95+%
  • Dasatinib, Free Base, >99%
  • DASATINIB HCL 99%
  • Dasatinib(BMS-354825)
  • N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide
  • 2-{6-[4-(2-HYDROXY-ETHYL)-PIPERAZIN-1-YL]-2-METHYL-PYRIMIDIN-4-YLAMINO}-THIAZOLE-5-CARBOXYLIC ACID (2-CHLORO-6-METHYL-PHENYL)-AMIDE
  • BMS-354825
  • N-[2-Chloro-6-methylphenyl]-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide
  • 5-Thiazolecarboxamide, N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-
  • Dasatinib
  • N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide
  • N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylhexahydropyrimidin-4-ylamino)-2,3-dihydrothiazole-5-carboxamide
  • Dasatinib Tablets
  • Dasatinib(BMS-354825,Sprycel)
  • N-[2-Chloro-6-Methylphenyl]-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-MethylpyriMidin-4-yl]aMino]-5-thiazolecarboxaMide
  • 2-{6-[4-(2-Hydroxy-ethyl)-piperazin-1-yl]-2-Methyl-pyriMidin-4-ylaMino}-thiazole
  • Dasatinib fandachem
  • Dasatinib USP/EP/BP
  • Dasatinib/Dasatinib monohydrate
  • ダサチニブ
  • ダサチニブ (JAN)
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