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Afatinib

Cat. No.:YN340035

  • CAS No. :850140-72-6

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    • 产品名称: Afatinib
      CAS No.: 850140-72-6
      Chemical Name: (2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide
      Synonyms:阿法替尼; BIBW 2992
      分子量:485.94
      分子式:C₂₄H₂₅ClFN₅O₃
      SMILES:O=C(NC1=C(C=C2C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)=C1)O[C@H]4CCOC4)/C=C/CN(C)C.[(E)]
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
      Select Batch:
      Purity: 98%
    • 产品描述: Afatinib (BIBW 2992) 是不可逆的EGFR家族抑制剂,抑制EGFRwt,EGFRL858R,EGFRL858R/T790M和 HER2的IC50分别为0.5 nM,0.4 nM,10 nM 和 14 nM。
      IC50和靶点: [{name:"EGFR:0.5 nM (IC50)"},{name: "HER2:14 nM (IC50)"},{name: "EGFRL858R:0.4 nM (IC50)"},{name: "EGFRL858R/T790M:10 nM (IC50)"}]
      In Vitro:
      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • Eskens, F.A.L.M., Mom, C.H., Planting, A.S.T., et al.A phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumoursBr. J. Cancer98(1),80-85(2008)

      Zhang, Y., Wang, C.-Y., Duan, Y.-J., et al.Afatinib decreases P-glycoprotein expression to promote adriamycin toxicity of A549T cellsJ. Cell. Biochem.119(1),414-423(2018)

      Yoshioka, T., Shien, K., Namba, K., et al.Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancerCancer Sci.109(4),1166-1176(2018)

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