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Chemical Structure : Mubritinib
CAS No.: 366017-09-6
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $198 | In stock | |
| 50 mg | $298 | In stock | |
| 100 mg | $498 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 468.47 | |
| Formula | C25H23F3N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1H-1,2,3-Triazole, 1-[4-[4-[[2-[(1E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-4-oxazolyl]methoxy]phenyl]butyl]- |
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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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