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Raltitrexed Basic information
Raltitrexed Chemical Properties
  • Melting point:176-1800C
  • Density 1.49±0.1 g/cm3(Predicted)
  • storage temp. Hygroscopic, -20°C Freezer, Under Inert Atmosphere
  • solubility H2O: ≥10mg/mL
  • pka3.50±0.10(Predicted)
  • form solid
  • color off-white to light yellow
  • CAS DataBase Reference112887-68-0(CAS DataBase Reference)
Safety Information
Raltitrexed Usage And Synthesis
  • DescriptionTomudex was launched in Ireland, France, Luxembourg and the UK for advanced colorectal cancer and it was prepared in a convergent manner (6 steps) from diethyl L-glutamate and 6-bromomethyi-2-methyl-quinazolin4(3H)-one. Tomudex is a highly selective inhibitor of thymidylate synthase (TS), the key enzyme in the biochemical conversion of dUMP to dTMP. It enters the cell via the reduced folatefmethotrexate cell membrane carrier and is converted to the polyglutamate species by folylpolyglutamate synthase within 4h where it then binds to the folate substrate site of TS. Clinically, it had a 29% response rate in patients with advanced colorectal cancer. It is water soluble, can be administered as a single dose every three weeks and had no hepto- or nephrotoxicity.
  • Chemical PropertiesYellow Crystalline Powder
  • OriginatorZeneca (UK)
  • UsesFolate-based inhibitor of thymidylate synthase; rapidly and extensively metabolized to its more potent polyglutamate derivatives. Antineoplastic
  • brand nameTomudex (Zeneca).
Raltitrexed Preparation Products And Raw materials
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