Tivozanib

Tivozanib Chemische Eigenschaften,Einsatz,Produktion Methoden

• Charakteristisch

  Primary targets: VEGFR/multikinase
  Class: receptor tyrosine kinase
  Treatment: RCC
  Elimination half-life = 111 h
  Protein binding = >99%

• Verwenden

  Tivozanib is known as an oral VEGF receptor tyrosine kinase inhibitor, exhibiting antitumor effects towards renal cell carcinoma.. Tivozanib suppresses angiogenesis by selectively inhibiting against vascular endothelial growth factor. Potent VEGFR inhibitor.

• Verwenden

  Tivozanib also known as AV-951 is an orally bioavailable potent VEGFR-1, 2 and 3, c-Kit and PDGFR inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM, respectively.

• Definition

  ChEBI: 1-[2-chloro-4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-3-(5-methyl-3-isoxazolyl)urea is an aromatic ether.

• Trademarks

  Fotivda^TM

• Mechanism of action

  Tivozanib is a  tyrosine kinase inhibitor that exerts its actions by inhibiting the  phosphorylation of vascular endothelial growth factor receptor  (VEGFR)-1, VEGFR-2 and VEGFR-3 and inhibits other kinases such as c-kit  and platelet derived growth factor beta (PDGFR β).

• Nebenwirkungen

  • diarrhea
  • nausea
  • vomiting
  • fatigue
  • loss of appetite
  • weight loss
  • voice hoarseness
  • back pain
  • mouth sores
  • cough
  • shortness of breath

• Synthese

  The synthesis of Tivozanib is as follows:
  Phenyl chlorocarbonate (601 g) was added dropwise to 3-amino-5-methylisoxazole (377 g), pyridine (1215 g), and N,N-dimethylacetamide (4 L) at 0°C, and the mixture was stirred at 20°C for 2 hr. 4-[(4-Amino-3-chlorophenol)oxy]-6,7-dimethoxyquinoline (847 g) was added to the reaction solution, and the mixture was stirred at 80°C for 5 hr. The reaction solution was cooled to 5°C. Thereafter, methanol (8.5 L) and water (8.5 L) were added thereto, and the mixture was neutralized with an aqueous sodium hydroxide solution. The resultant precipitate was collected by filtration, and the filtered product was slurried in water (8.5 L) for washing. The slurry was filtered, and the filtered product was then dried under the reduced pressure to give Tivozanib (1002 g, yield 86.1%).
  

• target

  VEGFR-2

Tivozanib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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