Mubritinib (TAK-165) | HER2 inhibitor | Probechem Biochemicals

Chemical Structure : Mubritinib

CAS No.: 366017-09-6

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Mubritinib (TAK-165, TAK165)

货号: 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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25 mg	￥880	In stock
50 mg	￥1380	In stock
100 mg	￥2280	In stock
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	468.47
分子式	C25H23F3N4O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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]-

参考文献

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.

Mubritinib (TAK-165, TAK165)

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Mubritinib (TAK-165, TAK165)

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