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アファチニブ, FREE BASE

アファチニブ, FREE BASE 化学構造式
850140-72-6
CAS番号.
850140-72-6
化学名:
アファチニブ, FREE BASE
别名:
アファチニブ, FREE BASE;アファチニブ
英語化学名:
Afatinib
英語别名:
fatinib;Afatinib;Tovok,BIBW;Afatinib API;Afatinib E-Isomer;Afatinib whatsapp;GILOTRIF(AFATINIB);Afatinib fandachem;Afatinib USP/EP/BP;BIBW 2992 BIBW 2992
CBNumber:
CB62507657
化学式:
C24H25ClFN5O3
分子量:
485.94
MOL File:
850140-72-6.mol

アファチニブ, FREE BASE 物理性質

融点 :
102 °C
沸点 :
676.9±55.0 °C(Predicted)
比重(密度) :
1.380
外見 :
Yellow powder.
酸解離定数(Pka):
11.79±0.43(Predicted)

安全性情報

HSコード  29420000

アファチニブ, FREE BASE 価格 もっと(3)

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) W01FLC050665 アファチニブ, Free Base
Afatinib, Free Base
850140-72-6 250mg ¥60000 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01FLC050665 アファチニブ, Free Base
Afatinib, Free Base
850140-72-6 1g ¥150000 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01FLC050665 アファチニブ, Free Base
Afatinib, Free Base
850140-72-6 5g ¥450000 2021-03-23 購入

アファチニブ, FREE BASE 化学特性,用途語,生産方法

外観

白色~黄赤色~緑色粉末~結晶

用途

抗悪性腫瘍薬, 受容体チロシンキナーゼ阻害薬。

効能

抗悪性腫瘍薬, 受容体チロシンキナーゼ阻害薬

使用

An aminocrotonylamino-substituted quinazoline derivative

定義

ChEBI: A quinazoline compound having a 3-chloro-4-fluoroanilino group at the 4-position, a 4-dimethylamino-trans-but-2-enamido group at the 6-position, and an (S)-tetrahydrofuran-3-yloxy group at the 7-position. Used (as its di aleate salt) for the first-line treatment of patients with metastatic non-small cell lung cancer.

適応症

The collection of ibrutinib (Imbruvica(R), Pharmacyclics Inc.), afatinib, and osimertinib represents the small, yet expanding, group of covalent SMKIs. Ibrutinib is a non-receptor Bruton’s tyrosine kinase inhibitor approved for the treatment of relapsed chronic lymphocytic leukemia. Afatinib, approved for NSCLC in 2013 and squamous NSCLC in 2016, is a second-generation irreversible EGFR inhibitor that targets wild-type EGFR, the mutant T790M EGFR, and HER2. Osimertinib (AZD9291), which was approved by FDA in November 2015, is a third-generation irreversible EGFR inhibitor that selectively targets the mutant T790M EGFR. Rociletinib, which shares a high degree of structural similarity with that of osimertinib, is a promising covalent EGFR inhibitor developed by Clovis Oncology aimed for the treatment of patients with EGFR T790M-mutated NSCLC, until the company terminated its development in May 2016 following a negative vote fromthe FDA’sOncologic Drugs Advisory Committee.

酵素阻害剤

This oral quinazoline derivative and EGFR/HER2-directed protein kinase inhibitor (FW = 485.94; CASs = 439081-18-2 (free base), 936631-70-8 (maleic acid salt), 1254955-21-9 (HCl salt); Solubility (at 25°C): 197 mg/mL DMSO, 1 mg/mL Water), also known by its code name BIBW2992, its trade names Gilotrif? Tomtovok?, Tovok?, and its systematic name (S,E)-N-(4-(3-chloro-4-fluorophenyl-amino)-7-(tetrahydrofuran- 3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide, irreversibly inactivates EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively. Mode of Action: The irreversible binding of afatinib to HER2 inactivates its interactions with a preferred partner of EGFR, and blocking the HER2- EGFR heterodimerization reduces their intrinsic tyrosine kinase activities. Irreversible inhibitors (such as afatinib and dacomitinib) that target all ErbB family receptor tyrosine kinases are intended to confer sustained disease control in ErbB-dependent cancers. Because nearly all EGFRmutated patients eventually develop resistance to reversible EGFR-TKIs after a median of 14 months, tafatinib’s irreversible action is thought to be a promising feature of its mode of action. Pharmacokinetics: Afatinib’s PK profile is best described by a two-compartment disposition model, with first-order absorption and linear elimination. There was a slightly more than proportional increase in exposure with increasing dose, most likely due to dose-dependent relative bioavailability. For the therapeutic dose of 40 mg, the estimated apparent total clearance rate at steady state was 734 mL/min.

アファチニブ, FREE BASE 上流と下流の製品情報

原材料

準備製品


アファチニブ, FREE BASE 生産企業

Global( 240)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
TianYuan Pharmaceutical CO.,LTD
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+86-755-23284190 sales@tianpharm.com CHINA 305 58
Shanghai Jinghao Pharmaceutical Co.,Ltd
+86-21-68900963
+86-21-68900963 sales@jinghaopharma.com CHINA 153 58
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sales@chemdad.com CHINA 37282 58
Handan Tongyi New Material Technology Co., Ltd
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Shenzhen Shengda Pharma Limited
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WeChat:shengdapharm sales@shengdapharm.com CHINA 310 58
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 886 50
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
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com China 9156 55

850140-72-6(アファチニブ, FREE BASE)キーワード:


  • 850140-72-6
  • Afatinib
  • (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide
  • 4-[(3-chloro-4-fluorophenyl)aMino]-6-{[4-(N,N-diMethylaMino)-1-oxo-2-buten-1-yl]aMino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline
  • 2-ButenaMide, N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(diMethylaMino)-, (2E)-
  • (S,E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dime
  • Afatinib API
  • Afatinib(BIBW2992MA2)
  • GILOTRIF(AFATINIB)
  • Afatinib (with 1 int.)
  • BIBW 2992 BIBW 2992
  • Afatinib E-Isomer
  • Hot sale Afatinib with best price and high quality CAS NO.850140-72-6
  • Afatinib whatsapp
  • Tovok,BIBW
  • BIBW-2992;BIBW2992;BIBW 2992
  • (2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-7-[(3S)-oxolan-3-yloxy]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide
  • (E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(S)-tetrahydrofuran-3-yl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide
  • Afatinib fandachem
  • fatinib
  • Afatinib USP/EP/BP
  • アファチニブ, FREE BASE
  • アファチニブ
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