AdipoGen Mubritinib

Supplier:  AdipoGen AGCR13755M005

Chemical. CAS 366017-09-6. Formula C25H23F3N4O2. MW 468.5. Mubritinib TAK-165 is a selective inhibitor of the human epidermal growth factor receptor 2 EGFR2 HER2, inhibiting HER2 phosphorylation with an IC50 value of 6nM. It is 4000-fold selective over EGFR, FGFR, PDGFR, JAK1, Src and Blk IC50 > 25μM. Mubritinib inhibits the proliferation of breast, bladder, kidney and prostate cancer cells in vitro and in vivo. Mubritinib was shown to inhibit autophagy in a HER2-independent manner in cancer cells. Recently shown to be a mitochondrial electron transport chain complex I NADH-CoQ reductase inhibitor. Mubritinib functions through ubiquinone-dependent inhibition of electron transport chain ETC complex I activity and consequently oxidative phosphorylation OXPHOS. This agent could be useful for immunometabolism research. Inhibition of electron transport chain in mitochondria leads to blocking of the transfer of electrons from iron-sulfur centers in complex I to ubiquinone.

Catalog No. 50-256-2172