VLX600

Cat No.:V12024 Purity: ≥98%
VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS).
VLX600 Chemical Structure CAS No.: 327031-55-0
Product category: OXPHOS
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of VLX600:

  • VLX600
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description
VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and results in a strong shift toward glycolysis. VLX600 displays selective cytotoxic activity against malignant cells and induces autophagy. Has anti-cancer activity.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
VLX600 (6 μM; 72 hours) promotes autophagy response [2]. VLX600 is cytotoxic to HCT116 spheroids. VLX600 induces HIF-1α-dependent glycolysis. VLX600 inhibits oxygen consumption in HCT116 cells. VLX600 suppresses the phosphorylation of mTOR downstream effectors 4EBP1 and p70-S6K through an HIF-1α-independent mechanism. VLX600 preferentially causes a decrease in ATP levels in cancer cells but not in normal cells [2].
ln Vivo
In human tumor xenografts, VLX600 (16 mg/kg; intravenously; every three days for 16 days) demonstrated anticancer efficacy [2].
Cell Assay
Cell proliferation experiment [2]
Cell Types: HCT116, HT29, SW620, HT8, DLD and RKO Cell
Tested Concentrations: 0.1, 1, 10, 100μM
Incubation Duration: 72 hrs (hours)
Experimental Results: Inhibition of proliferation of these cells.

Western Blot Analysis[2]
Cell Types: HCT116 Cell
Tested Concentrations: 6 μM
Incubation Duration: 72 hrs (hours)
Experimental Results: LC3-II was induced.
Animal Protocol
Animal/Disease Models: NMRI nu/nu (nude) mice (HCT116 and HT29 colon cancer xenografts) [2]
Doses: 16 mg/kg
Route of Administration: IV; every three days for 16 days
Experimental Results: In HCT116 and HT29 colon Antitumor activity was observed in cancer xenografts.
References
[1]. Karlsson H, et al. A novel tumor spheroid model identifies selective enhancement of radiation by an inhibitor of oxidative phosphorylation. Oncotarget. 2019 Sep 3;10(51):5372-5382.
[2]. Zhang X, et al. Induction of mitochondrial dysfunction as a strategy for targeting tumour cells in metabolically compromised microenvironments. Nat Commun. 2014;5:3295.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H15N7
Molecular Weight
317.348
CAS #
327031-55-0
Related CAS #
327031-55-0;1622945-04-3;VLX600 HCl;
SMILES
CC1=C2C(=CC=C1)C3=C(N2)N=C(N/N=C(\C)/C4=CC=CC=N4)N=N3
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~25 mg/mL (~78.78 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 2.08 mg/mL (6.55 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.1511 mL 15.7555 mL 31.5110 mL
5 mM 0.6302 mL 3.1511 mL 6.3022 mL
10 mM 0.3151 mL 1.5755 mL 3.1511 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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