TAK 165

Cat. No. 3599

TAK 165 C25H23F3N4O2 [366017-09-6]

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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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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

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.

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.

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Keywords: TAK 165, supplier, Potent, selective, ErbB2, inhibitors, inhibits, Epidermal, Growth, Factor, Receptors, Her, EGFR, Receptor, Tyrosine, Kinases, RTKs, TAK165, Tocris Bioscience, EGFR Inhibitor products

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