TAK 165

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Cat.No. 3599 - TAK 165 | C25H23F3N4O2 | CAS No. 366017-09-6
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
Literature

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.

Compound Libraries

TAK 165 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 468.47. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.13 mL 10.67 mL 21.35 mL
5 mM 0.43 mL 2.13 mL 4.27 mL
10 mM 0.21 mL 1.07 mL 2.13 mL
50 mM 0.04 mL 0.21 mL 0.43 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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:

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


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

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