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O-Desmethyl gefitinib

Cat. No.:YN340331

  • CAS No. :847949-49-9

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    • 产品名称: O-Desmethyl gefitinib
      CAS No.: 847949-49-9
      Chemical Name: 4-[(3-chloro-4-fluorophenyl)amino]-6-[3-(4-morpholinyl)propoxy]-7-quinazolinol
      Synonyms:
      分子量:432.9
      分子式:C21H22ClFN4O3
      SMILES:OC1=CC2=C(C(NC3=CC=C(F)C(Cl)=C3)=NC=N2)C=C1OCCCN4CCOCC4
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: O-Desmethyl gefitinib 是 Gefitinib 在人血浆中的活性代谢产物。O-Desmethyl gefitinib 的形成依赖于 CYP2D6 活性。在亚细胞试验中,O-Desmethyl gefitinib 抑制EGFR,IC50为 36 nM。
      IC50和靶点:
      In Vitro:
      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • McKillop, D., Hutchison, M., Partridge, E.A., et al.Metabolic disposition of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat, dog and manXenobiotica34(10),917-934(2004)

      McKillop, D., Guy, S.P., Spence, M.P., et al.Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibitionXenobiotica36(1),29-39(2006)

      Kobayashi, H., Sato, K., Niioka, T., et al.Effects of polymorphisms in CYP2D6 and ABC transporters and side effects induced by gefitinib on the pharmacokinetics of the gefitinib metabolite, O-desmethyl gefitinibMed. Oncol.33(6),1-8(2016)

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