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Entrectinib

(Synonyms: NMS-E628; RXDX-101)
30 Cited Publications
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Based on 30 publication(s) in Google Scholar

Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.

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  • Pureza: 98.98%
  • No. CAS: 1108743-60-7
  • Fòrmula: C31H34F2N6O2
  • Peso molecular:560.64
  • Almacenamiento:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • Entrectinib Chemical Structure
    Entrectinib Chemical Structure
  • Experimental Validation Results for Entrectinib
  • Experimental Validation Results for Entrectinib
  • Experimental Validation Results for Entrectinib
  • Experimental Validation Results for Entrectinib
  • Experimental Validation Results for Entrectinib
  • Experimental Validation Results for Entrectinib
No. CAS: 1108743-60-7
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  • Entrectinib Chemical Structure
    Entrectinib Chemical Structure
    1/16
  • 1/16

    Entrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Feb 24;12(1):1261. [Abstract]

    Customer Validation
     Phospho-ALK and its downstream signals in MR347 cells were evaluated by western blotting after the treatment of the indicated concentration of inhibitors (Entrectinib, 100 nM) for 6h.

  • 1/16

    Entrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Feb 24;12(1):1261. [Abstract]

    Customer Validation
     Phospho-ALK in each EML4- ALK mutations expressing Ba/F3 cells were evaluated by western blotting. Cells were treated with the indicated concentrations of entrectinib (0, 50, 100 nM) for 3 h.

  • 1/16

    Entrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Feb 24;12(1):1261. [Abstract]

    Customer Validation
     Suppression of phospho-NTRK1 and its downstream signals in KM12 cells were evaluated by western blotting. Cells were treated with the entrectinib (30 nM) or gilteritinib for 6 h

  • 1/16

    Entrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Feb 24;12(1):1261. [Abstract]

    Customer Validation
     Apoptosis assay by flow cytometry analysis with Annexin-V and PI staining after 72 h of 100 nM entrectinib or gilteritinib treatment to KM12 cells. The percentage of cells undergoing apoptosis is shown in red.

  • 1/16

    Entrectinib purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 Aug 4;32(5):107994. [Abstract]

    Customer Validation
     Immunoblot analysis of protein expression or modification in lysates of IMPETPR-NTRK1 cells treated with 10 nM Entrectinib for 0-24 h. pTRKA remained completely inhibited at 18 and 24 h, indicating that Entrectinib is still effectively inhibiting its direct target.

  • 1/16

    Entrectinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Oct;16(10):2130-2143. [Abstract]

    Customer Validation
     KM12 or CR20 cells are treated with increasing concentrations of Cabozantinib, Entrectinib or LOXO-101 for 3 hours. Cell lysates are immunoblotted to detect the indicated proteins.

  • Entrectinib