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530510 OxPhos Inhibitor, VLX600 - Calbiochem

A cell-permeable compound with cytotoxicity towards quiescent cells in colon cancer 3-D microtissues (~ 6 µM). Reduces mitochondrial oxidative phosphorylation in tumor cells.

OxPhos Inhibitor, VLX600 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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-((2Z)-2-(1-(2-pyridinyl)ethylidene)hydrazino)-5H-[1,2,4]triazino[5,6-b]indole, VLX-600

Primary Target: mitochondria
530510
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

Empirical Formula
C₁₇H₁₅N₇

Products

KatalógusszámCsomagolás Menny./csomag
5.30510.0001 Üvegpalack 10 mg
Description
OverviewA 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.
Catalogue Number530510
Brand Family Calbiochem®
Synonyms1-(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-((2Z)-2-(1-(2-pyridinyl)ethylidene)hydrazino)-5H-[1,2,4]triazino[5,6-b]indole, VLX-600
References
ReferencesZhang, X., et al. 2014. Nat. Comm. 5, 3295.
Product Information
FormDark yellow powder
Hill FormulaC₁₇H₁₅N₇
Chemical formulaC₁₇H₁₅N₇
Quality LevelMQ100
Applications
Biological Information
Primary Targetmitochondria
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalógusszám GTIN
5.30510.0001 04055977260847

Documentation

OxPhos Inhibitor, VLX600 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Hivatkozások áttekintése
Zhang, X., et al. 2014. Nat. Comm. 5, 3295.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision09-May-2014 JSW
Synonyms1-(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-((2Z)-2-(1-(2-pyridinyl)ethylidene)hydrazino)-5H-[1,2,4]triazino[5,6-b]indole, VLX-600
DescriptionA 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).
FormDark yellow powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₇H₁₅N₇
Purity≥97% by HPLC
SolubilityDMSO (25 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesZhang, X., et al. 2014. Nat. Comm. 5, 3295.