5.30510
OxPhos Inhibitor, VLX600
別名:
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]
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この商品について
assay
≥97% (HPLC)
Quality Segment
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
dark yellow
solubility
DMSO: 25 mg/mL
storage temp.
−20°C
SMILES string
CC1=C2C(=CC=C1)C3=C(N2)N=C(N=N3)NN=C(C)C4=CC=CC=N4
General description
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 (t1/2 ~ 4 to 5 h).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
mitochondria
mitochondria
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Zhang, X., et al. 2014. Nat. Comm.5, 3295.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
WGK
WGK 3
引火点 (F)
Not applicable
引火点（°C）
Not applicable