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TAK 165

Cat. No. 3599

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Alternative Name: 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 and to 5 mM in ethanol

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.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Sridhar et al (2003) Inhibitors of epidermal-growth-factor receptors: a review of clinical research with a focus on non-small-cell lung cancer. Lancet Oncol. 4 397. PMID: 12850190.

Nagasawa et al (2006) Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int.J.Urol. 13 585.

Spector et al (2007) Small molecule HER-2 tyrosine kinase inhibitors. Breast Cancer Res. 9 205.

If you know of a relevant citation for this product please let us know.

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