Chemical Structure : HP661
CAS No.:
2938220-60-9
HP661
(HP 661, HP-661)
Catalog No.: PC-20779Not For Human Use, Lab Use Only.
HP661 is a potent, and selective oral complex I OXPHOS inhibitor with 76% inhibition at 1u M in H460 cells using electron flow assays, inhibits high-OXPHOS H460 cell viability with IC50 of 5 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
HP661 is a potent, and selective oral complex I OXPHOS inhibitor with 76% inhibition at 1u M in H460 cells using electron flow assays, inhibits high-OXPHOS H460 cell viability with IC50 of 5 nM.
HP661 displays no inhibitory rates against complexes II-IV.
HP661 potently and preferentially blocked the mitochondrial OXPHOS function in high-OXPHOS cancer cells.
HP661 effectively inhibited MEKi tolerance-meditated mitochondrial OXPHOS, indicating the potential of HP661 to sensitize MEKi in KRAS-mutant lung cancer.
HP661 efficiently induced apoptosis of H460 and H441 cells, sensitizes KRAS-mutant NSCLC cells to MEKi therapy.
HP661 not only significantly suppressed tumor growth but also augmented the therapeutic efficacy of trametinib by impairing tumor mitochondrial respiration in mouse model of high-OXPHOS lung cancer.
Physicochemical Properties
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M.Wt
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661.61
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Formula
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C31H29F6N7O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-((5-methyl-4-(4-(4-(2,2,2-trifluoroethoxy)benzyl)piperazine-1-carbonyl)-1H-1,2,3-triazol-1-yl)methyl)-N-(4-(trifluoromethyl)phenyl)picolinamide
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References
1. Peng He, et al. Journal of Medicinal Chemistry, May 2, 2023
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