Catalog Number: 3599
Alternate Names: Mubritinib
Chemical Name: 1-[4-[4-[[2-[(1E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-4-oxazolyl]methoxy]phenyl]butyl]-1H-1,2,3-triazole
Biological Activity
Potent, irreversible human epithelial growth factor receptor 2 (ErbB2) inhibitor (IC50 = 6 nM) that displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Exhibits potent antiproliferative effects in ErbB2-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo.
Technical Data
  • M.Wt:
    468.47
  • Formula:
    C25H23F3N4O2
  • Solubility:
    Soluble to 75 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    366017-09-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Inhibitors of epidermal-growth-factor receptors: a review of clinical research with a focus on non-small-cell lung cancer.
    Sridhar et al.
    Lancet Oncol., 2003;4:397
  2. Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo.
    Nagasawa et al.
    Int.J.Urol., 2006;13:585

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