530510 OxPhos Inhibitor, VLX600 - Calbiochem

530510
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₁₅N₇

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30510.0001
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          Glass bottle 10 mg
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          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
          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

          Documentation

          OxPhos Inhibitor, VLX600 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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 -20°C
          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.
          Toxicity Standard Handling
          ReferencesZhang, X., et al. 2014. Nat. Comm. 5, 3295.