TAK 165

Tocris Bioscience, part of Bio-Techne | Catalog # 3599

COA / SDS

Potent and selective ErbB2 inhibitor

Key Product Details

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% (HPLC)
Molecular Weight:	468.47

View Full Technical Details for TAK 165

Technical Data
Citations

Biological Activity for TAK 165

TAK 165 is a 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 for TAK 165

M. Wt	468.47
Formula	C₂₅H₂₃F₃N₄O₂
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	366017-09-6
PubChem ID	6444692
InChi Key	ZTFBIUXIQYRUNT-MDWZMJQESA-N
Smiles	FC(C(C=C2)=CC=C2/C=C/C1=NC(COC3=CC=C(CCCCN4C=CN=N4)C=C3)=CO1)(F)F

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.

Solubility for TAK 165

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	35.14	75

Preparing Stock Solutions for TAK 165

The following data is based on the product molecular weight 468.47.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.75 mM	2.85 mL	14.23 mL	28.46 mL
3.75 mM	0.57 mL	2.85 mL	5.69 mL
7.5 mM	0.28 mL	1.42 mL	2.85 mL
37.5 mM	0.06 mL	0.28 mL	0.57 mL

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References for TAK 165

References are publications that support the biological activity of the product.

Nagasawa Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo. Int.J.Urol. 2006 PMID: 16771730
Spector Small molecule HER-2 tyrosine kinase inhibitors. Breast Cancer Res.
Sridhar Inhibitors of epidermal-growth-factor receptors: a review of clinical research with a focus on non-small-cell lung cancer. Lancet Oncol. 2003 PMID: 12850190