HP661

Formulation: A crystalline solid

Formal Name: 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

Purity: ≥98%

Formula Markup: C31H29F6N7O3

Formula Weight: 661,6

Shelf life (days): 730

Notes: HP661 is an inhibitor of mitochondrial complex I, also known as NADH dehydrogenase.{68450} It is selective for complex I, inhibiting it by 77.6%, over complex III, which it inhibits by 28.1%, and complexes II and IV, which it does not inhibit, at 1 µM. HP661 selectively reduces viability of the human lung cancer cells H460, NCI H441, and trametinib-resistant A549 cells (IC50s = 10.6, 29.7, and 15.1 nM, respectively), which all have high levels of oxidative phosphorylation, over NCI H358 human lung cancer cells (IC50 = >10,000 nM), which have low levels of oxidative phosphorylation, and non-cancerous human pancreatic normal epithelial (HPNE) and MRC-5 human fetal lung fibroblast cells (IC50s = >10,000 nM for both). HP661 reduces tumor volume in an H460 mouse xenograft model when administered at a dose of 30 mg/kg twice per day and has an additive effect on trametinib-induced reduction of tumor growth.

• Artikelnummer: CAY38927-1
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 38927-1
• Green Labware: Nein
• Verpackungseinheit: 1 mg
• Mengeneinheit: STK