1. Metabolic Enzyme/Protease Autophagy
  2. Oxidative Phosphorylation Mitochondrial Metabolism Autophagy
  3. VLX600

VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. Anticancer activity.

For research use only. We do not sell to patients.

VLX600 Chemical Structure

VLX600 Chemical Structure

CAS No. : 327031-55-0

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5 mg USD 61 In-stock
10 mg USD 99 In-stock
25 mg USD 209 In-stock
50 mg USD 352 In-stock
100 mg USD 605 In-stock
250 mg USD 1210 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. Anticancer activity[1][2].

In Vitro

VLX600 (6 μM; 72 hours) induces an autophagic response[2].
VLX600 is cytotoxic to HCT116 spheroids. VLX600 induces a HIF-1α-dependent glycolytic response. VLX600 inhibits oxygen consumption in HCT116 cells. VLX600 inhibits phosphorylation of the mTOR downstream effectors 4EBP1 and p70-S6K by an HIF-1α-independent mechanism. VLX600 preferentially leads to decreased ATP levels in cancer but not normal cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: HCT116, HT29, SW620, HT8, DLD and RKO cells
Concentration: 0.1, 1, 10, 100μM
Incubation Time: 72 hours
Result: Inhibited the proliferation of these cells.

Western Blot Analysis[2]

Cell Line: HCT116 cells
Concentration: 6 μM
Incubation Time: 72 hours
Result: LC3-II was induced.
In Vivo

VLX600 (16 mg/kg; i.v.; every third day for 16 days) shows anti-tumor activity in human tumor xenografts[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NMRI nu/nu mice (HCT116 and HT29 colon cancer xenografts)[2]
Dosage: 16 mg/kg
Administration: Intravenously; every third day for 16 days
Result: Anti-tumor activity was observed in both HCT116 and HT29 colon cancer xenografts.
Clinical Trial
Molecular Weight

317.35

Formula

C17H15N7

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(NC2=C3N=NC(N/N=C(C4=CC=CC=N4)\C)=N2)C3=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (78.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.08 mg/mL (6.55 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.08 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1511 mL 15.7555 mL 31.5109 mL 78.7774 mL
5 mM 0.6302 mL 3.1511 mL 6.3022 mL 15.7555 mL
10 mM 0.3151 mL 1.5755 mL 3.1511 mL 7.8777 mL
15 mM 0.2101 mL 1.0504 mL 2.1007 mL 5.2518 mL
20 mM 0.1576 mL 0.7878 mL 1.5755 mL 3.9389 mL
25 mM 0.1260 mL 0.6302 mL 1.2604 mL 3.1511 mL
30 mM 0.1050 mL 0.5252 mL 1.0504 mL 2.6259 mL
40 mM 0.0788 mL 0.3939 mL 0.7878 mL 1.9694 mL
50 mM 0.0630 mL 0.3151 mL 0.6302 mL 1.5755 mL
60 mM 0.0525 mL 0.2626 mL 0.5252 mL 1.3130 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
VLX600
Cat. No.:
HY-12406
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