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TAK 165

Cat. No. 3599 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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)
Datasheet
Citations
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

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 Data for TAK 165

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets for TAK 165

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for TAK 165

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

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 PMID: 16771730

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

If you know of a relevant reference for TAK 165, please let us know.

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Citations for TAK 165

Citations are publications that use Tocris products.

Currently there are no citations for TAK 165. Do you know of a great paper that uses TAK 165 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

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