TAK 165

Catalog # Availability Size / Price Qty
3599/10
3599/50
TAK 165 | CAS No. 366017-09-6 | EGF Receptor Inhibitors
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Description: Potent and selective ErbB2 inhibitor
Alternative Names: Mubritinib

Chemical Name: 1-[4-[4-[[2-[(1E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-4-oxazolyl]methoxy]phenyl]butyl]-1H-1,2,3-triazole

Purity: ≥99%

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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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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
  3. Small molecule HER-2 tyrosine kinase inhibitors.
    Spector et al.
    Breast Cancer Res., 2007;9:205

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