Cat. No. 3599
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 ActivityPotent, 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
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.
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Keywords: TAK 165, supplier, Potent, selective, ErbB2, inhibitors, Epidermal, Growth, Factor, Receptors, Her, EGFR, Receptor, Tyrosine, Kinases, RTKs, TAK165
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December 16, 2013