5.30510

OxPhos Inhibitor, VLX600

• Sinônimo(s): OxPhos Inhibitor, VLX600, 1-(2-Pyridinyl)ethanone(6-methyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl)hydrazone, ( Z)-6-Methyl-3-(2-(1-(pyridin-2-yl)ethylidene)hydrazinyl)-5H-[1,2,4]triazino[5,6-b]indole, 6-Methyl-3-((2 Z)-2-(1-(2-pyridinyl)ethylidene)hydrazino)-5H-[1,2,4]
• Fórmula empírica (Notação de Hill): C₁₇H₁₅N₇
• Peso molecular: 317.35
• Código UNSPSC: 12352200
• ID de substância PubChem: 6410104
• NACRES: NA.77

Propriedades

• Ensaio: ≥97% (HPLC)
• Nível de qualidade: 100
• Formulário: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: dark yellow
• solubilidade: DMSO: 25 mg/mL
• temperatura de armazenamento: −20°C
• cadeia de caracteres SMILES: CC1=C2C(=CC=C1)C3=C(N2)N=C(N=N3)NN=C(C)C4=CC=CC=N4

Descrição

Descrição geral

A cell-permeable, bioavailable triazinoindolyl-hydrazone compound that displays preferential cytotoxicity towards quiescent cells in colon cancer 3-D microtissues (~ 6 µM). Inhibits the proliferation of HCT116 and several other human colon carcinoma and mouse cell lines in monolayer culture. Causes a significant reduction in mitochondrial oxidative phosphorylation in tumor cells thereby lowering their ATP levels and limiting their ability to respond to metabolically compromised microenvironment. Shown to increase AMP kinase phosphorylation and inhibit the phosphorylation of 4EBP1 and p70S6K, two downstream targets of mTOR. Induces LC-3II formation and autophagy in HCT 116, HCT116 HIF-1α ^-/-, and HT29 cells in a dose-dependent manner. Its sensitivity in HCT116 cells is enhanced under conditions of glucose starvation. Also reduces the growth of HCT116 and HT29 colon cancer xenografts in NMRI mice (~16 mg/kg, i.v. b.i.d, 5 d) and enhances oxaliplatin, irinotecan and 5-fluorouracil chemosensitivity. Displays attractive PK profile (t_1/2 ~ 4 to 5 h).

A cell-permeable, bioavailable triazinoindolyl-hydrazone compound that displays preferential cytotoxicity towards quiescent cells in colon cancer 3-D microtissues (~ 6 µM). Inhibits the proliferation of HCT116 and several other human colon carcinoma and mouse cell lines in monolayer culture. Causes a significant reduction in mitochondrial oxidative phosphorylation in tumor cells thereby lowering their ATP levels and limiting their ability to respond to metabolically compromised microenvironment. Shown to increase AMP kinase phosphorylation and inhibit the phosphorylation of 4EBP1 and p70S6K, two downstream targets of mTOR. Induces LC-3II formation and autophagy in HCT 116, HCT116 HIF-1α ^-/-, and HT29 cells in a dose-dependent manner. Its sensitivity in HCT116 cells is enhanced under conditions of glucose starvation. Also reduces the growth of HCT116 and HT29 colon cancer xenografts in NMRI mice (~16 mg/kg, i.v. b.i.d, 5 d) and enhances oxaliplatin, irinotecan and 5-fluorouracil chemosensitivity. Displays attractive PK profile (t_1/2 ~ 4 to 5 h).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
mitochondria

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Zhang, X., et al. 2014. Nat. Comm.5, 3295.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable