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Mubritinib

Chemical Structure : Mubritinib

CAS No.: 366017-09-6

Mubritinib (TAK-165, TAK165)

Catalog No.: PC-20781Not For Human Use, Lab Use Only.

Mubritinib (TAK-165) is a potent inhibitor of human epidermal growth factor receptor 2 (HER2, ERBB2) tyrosine kinase with IC50 of 6 nM, also is a potent Complex I inhibitor with IC50 of 51 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Mubritinib (TAK-165) is a potent inhibitor of human epidermal growth factor receptor 2 (HER2, ERBB2) tyrosine kinase with IC50 of 6 nM, also is a potent Complex I inhibitor with IC50 of 51 nM.
Mubritinib (TAK-165) does not inhibit other types tyrosine kinase up to 25,000 nM.
Mubritinib (TAK-165) inhibits HER2 phosphorylation and its down-stream Akt and MAPK in HER2 strongly expressing cells (BT474 breast cancer cell line).
Mubritinib (TAK-165) shows synergistic effect with trametinib in KRAS-mutant cell lines.
Mubritinib exhibits strong anti-leukemic effects in vitro and in vivo, functions through ubiquinone-dependent inhibition of electron transport chain (ETC) complex I activity.
Mubritinib (TAK-165) inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo.

Physicochemical Properties

M.Wt 468.47
Formula C25H23F3N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-1,2,3-Triazole, 1-[4-[4-[[2-[(1E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-4-oxazolyl]methoxy]phenyl]butyl]-

References

1. Nagasawa J, et al. Int J Urol. 2006 May;13(5):587-92.

2. Baccelli I, et al. Cancer Cell. 2019 Jul 8;36(1):84-99.e8.

3. Ding Xue, et al. J Med Chem. 2022 Jan 13;65(1):343-368.

4. Uitdehaag JC, et al. PLoS One. 2015 May 27;10(5):e0125021.

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