OxPhos Inhibitor, VLX600-Calbiochem

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一般描述

A cell-permeable, bioavailable triazinoindolyl-hydrazone compound that displays preferential cytotoxicity towards quiescent cells in colon cancer 3-D microtissues (~ 6 ?M). 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 ?M). 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.

生化/生理作用

Cell permeable: yes
Primary Target
mitochondria

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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

法律信息

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

基本信息

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安全信息