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Afatinib

(Synonyms: BIBW 2992)
107 Cited Publications
고객리뷰

Based on 107 publication(s) in Google Scholar

Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

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  • Purity: 99.92%
  • CAS No.: 850140-72-6
  • 화학식: C24H25ClFN5O3
  • 분자량:485.94
  • 보관:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • Afatinib Chemical Structure
    Afatinib Chemical Structure
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
  • Experimental Validation Results for Afatinib
CAS No.: 850140-72-6
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  • Afatinib Chemical Structure
    Afatinib Chemical Structure
    1/16
  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2026 Feb 12:800:153165.

    Customer Validation
     ActE_21 binding to A549, SK-BR-3 and A431 after incubation with Afatinib (Afatinib dimaleate; 50 nM) for 120 min at 37 °C. Afatinib increases EGF-EGFR complex surface levels in A549 and SK-BR-3 cell.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1032-1041. [Abstract]

    Customer Validation
     Immunoblot analysis of cell lines (K562 HER2WT or HER2C805S Nluc-3xFLAG reporter cell lines) treated for 15 h with AV-412 (HY-10346; 2.5 µM), neratinib (HY-32721; 10 µM), afatinib (HY-10261; 10 µM), WZ4002 (HY-12026; 10 µM).

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1032-1041. [Abstract]

    Customer Validation
     Luminescent reporter assay of K562 HER2WT or HER2C805S Nluc-3xFLAG reporter cell lines treated for 15 h with the indicated compounds (AV-412 (HY-10346; 2.5 µM), neratinib (HY-32721; 10 µM), afatinib (HY-10261; 10 µM), WZ4002 (HY-12026; 10 µM)) shown as normalized luminescence per genetic construct (two-way ANOVA, Sidak corrected) (n = 3).

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Jan;57(1):165-179. [Abstract]

    Customer Validation
     Afatinib (10 mg/kg/day; daily, 5 days per week by oral gavage) decreased the intensity of EGFR phosphorylation (pY845) in NOD-SCID mice.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Jan;57(1):165-179. [Abstract]

    Customer Validation
     Afatinib (10 mg/kg/day; daily, 5 days per week by oral gavage) reduced the number of Ki-67-positive proliferating cells in NOD-SCID mice.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Jun 10:10.1158/0008-5472.CAN-24-3904. [Abstract]

    Customer Validation
     Growth curves of NF1Mut melanoma STCs treated with 0.1, 0.5, 1, 5, or 10 μM Afatinib.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Jun 10:10.1158/0008-5472.CAN-24-3904. [Abstract]

    Customer Validation
     Growth curves of NF1Mut melanoma STCs treated with 0.1, 0.5, 1, 5, or 10 μM Afatinib.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1237. [Abstract]

    Customer Validation
     mRNA expression for CPT1A in cetuximab-sensitive (-S) and -resistant (-R) FaDu cells upon treatment with gefitinib, afatinib, selumetinib or buparlisib (2 µM each, for 24 h) (N = 3, n = 3).

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1237. [Abstract]

    Customer Validation
     mRNA expression for CPT1A in cetuximab-sensitive (-S) and -resistant (-R) SC263 cells upon treatment with gefitinib, afatinib, selumetinib or buparlisib (2 µM each, for 24 h) (N = 3, n = 3).

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 May 9:2025.05.04.652129. [Abstract]

    Customer Validation
     Afatinib dimaleate (15 mg/kg; oral gavage; once daily for 8 weeks) reduced tumor burden and tumor diameter in BrafCAT mice.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 May 9:2025.05.04.652129. [Abstract]

    Customer Validation
     Afatinib dimaleate (Afatinib; 15 mg/kg; oral gavage; once daily for 8 weeks). Immunohistochemistry analyses of phosphorylated ERK (pT202, Y204) in BrafCAT formalin fixed paraffin embedded (FFPE) mouse lung tissue.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 May 9:2025.05.04.652129. [Abstract]

    Customer Validation
     Afatinib dimaleate (A; 50 nM; 2 or 24 h), alone or in combination with dabrafenib and trametinib (D+T+A), enhances pathway blockade in HCC364 human BRAFV600E+ lung cancer cells.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2023 Jan 9;41(1):88-105.e8. [Abstract]

    Customer Validation
     Cell viability assays of Kmt2d KO LUSC cell lines, Kmt2d WT LUSC cell lines, and LUAD (KP) cell line treated with afatinib for 72h. Data presented as mean ± SD (n = 3). The calculated IC50 values of afatinib is shown below.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]

    Customer Validation
     Immunoblot analysis of U-CH1, MUG-Chor1 and Chor-IN-1 cells treated with Afatinib for 2 h or 48 h. Protein cell extracts were resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC50s for each cell line are reported.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]

    Customer Validation
     Immunoblot analysis of U-CH1 cells treated with the indicated doses of inhibitors (Afatinib, Erlotinib and Lapatinib) for 2 h (upper panel) or 48 h (lower panel). Protein cell extracts were resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC50s of the different inhibitors are reported.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Apr;109(4):1166-1176. [Abstract]

    Customer Validation
     Influence of Afatinib or Neratinib on human epidermal growth factor receptor 2 (HER2) and the downsignal pathway in gastric cancer cell lines.

  • 1/16

    Afatinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2014 Dec 15;5(23):11971-85. [Abstract]

    Customer Validation
     H460/MX20 cells are treated with varying concentrations (0–2.0 μM) of Afatinib for 48 h, or with 1.0 μM Afatinib for 24 h, 48 h and 72 h, respectively. ABCG2 protein levels are analyzed by Western blot. GAPDH is used as a loading control.

  • Afatinib