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ダブラフェニブ

 ダブラフェニブ 化学構造式
1195765-45-7
CAS番号.
1195765-45-7
化学名:
ダブラフェニブ
别名:
ダブラフェニブ;ダブラフェニブ
英語化学名:
N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide
英語别名:
CS-658;Dabrafenib;GSK2118436A;Debrafenib API;Dabrafenib Base;Dabrafenib, >=98%;Dabrafenib KB-57246;Debrafenib free base;Dabrafenib(free base);Dabrafenib (GSK2118436)
CBNumber:
CB32604230
化学式:
C23H20F3N5O2S2
分子量:
519.5624096
MOL File:
1195765-45-7.mol

ダブラフェニブ 物理性質

沸点 :
653.7±65.0 °C(Predicted)
比重(密度) :
1.443
外見 :
White solid.
酸解離定数(Pka):
6.62±0.10(Predicted)

安全性情報

HSコード  29350090

ダブラフェニブ 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

ダブラフェニブ 化学特性,用途語,生産方法

効能

抗悪性腫瘍薬, BRAFキナーゼ阻害薬

説明

In May 2013, the US FDA approved dabrafenib (also referred to as GSK 2118436) for the treatment of patients with unresectable or metastatic melanoma with the BRAFV600E mutation as detected by a FDA-approved test. Dabrafenib was identified from a screen of an oncology-directed kinase collection, followed by extensive structure–activity relationships (SAR) on an initial thiazole lead. Dabrafenib is a potent inhibitor of B-BRAFV600E kinase (IC50=0.65 nM) compared to its potency against wild-type B-raf (IC50=3.2 nM). It also inhibits other kinases (e.g., CRAF) and other mutant B-raf kinases (BRAFV600E and BRAFV600D) with enzyme IC50s of <5 nM and is fairly selective versus a panel of 270 kinases. Consistent with its in vitro activity, oral administration of dabrafenib inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts growing subcutaneously in immunocompromised mice. Key steps in the synthesis of dabrafenib are condensation of an aryl sulfonamide ester with the lithium anion of 2-chloro-4-methylpyrimidine to generate a ketone intermediate and bromination of the ketone intermediate with N-bromosuccinamide followed by cyclization with tert-butyl thioamide to afford the desired thiazole core.

Originator

GlaxoSmithKline (United States)

定義

ChEBI: An organofluorine compound and antineoplastic agent, used as its mesylate salt in treatment of metastatic melanoma.

brand name

Tafinlar

ダブラフェニブ 上流と下流の製品情報

原材料

準備製品


ダブラフェニブ 生産企業

Global( 168)Suppliers
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1195765-45-7( ダブラフェニブ)キーワード:


  • 1195765-45-7
  • Dabrafenib
  • N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide
  • Dabrafenib free base(GSK2118436A)
  • Dabrafenib (GSK2118436)
  • GSK2118436A
  • Dabrafenib (GSK2118436A)
  • CS-658
  • GSK2118436A (Dabrafenib)
  • GSK2118436A (DABRAFENIB);GSK-2118436B (DABRAFENIB MESYLATE);GSK-2118436A;GSK-2118436;GSK2118436A;GSK2118436A;GSK 2118436;GSK 2118436
  • GSK-2118436B (Dabrafenib Mesylate)
  • N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide
  • Dabrafenib KB-57246
  • Debrafenib API
  • N-(3-(5-(2-aminopyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide
  • Dabrafenib N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide
  • N-[3-[5-(2-Amino-4-pyrimidinyl)-2-(tert-butyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide Dabrafenib
  • Dabrafenib Base
  • BenzenesulfonaMide, N-[3-[5-(2-aMino-4-pyriMidinyl)-2-(1,1-diMethylethyl)-4-thiazolyl]-2-fluorophenyl]-2,6-difluoro-
  • Dabrafenib(GSK2118436) KB-57246
  • Dabrafenib, >=98%
  • GSK2118436, Dabrafenib, GSK2118436A
  • Dabrafenib(free base)
  • Debrafenib free base
  • Dabrafenib, 98%, a mutant BRAFV600 specific inhibitor
  • N-(3-(5-(2-Aminopyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenes
  • ダブラフェニブ
  • ダブラフェニブ
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