VLX600

Catalog No.S8943

For research use only.

VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity.

VLX600 Chemical Structure

CAS No. 327031-55-0

Selleck's VLX600 has been cited by 1 Publication

Purity & Quality Control

Choose Selective OXPHOS Inhibitors

Biological Activity

Description VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity.
Targets
OXPHOS [2]
In vitro

VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation.[1] Mitochondrial inhibition with VLX600 has a direct antitumor effect in vitro while appearing to promote glycolysis through increased AKT signaling and glucose transporter expression. When combined with imatinib, VLX600 prevents imatinib-induced cell cycle escape and reduces p27 expression, leading to increased apoptosis when compared to imatinib alone.[3]

In vivo

VLX600 induces the formation of autolysosomes in vivo. VLX600 displays tumour growth inhibition in vivo.[1] When combined with imatinib, VLX600 reduces p27 expression in vivo, and prevents imatinib-induced cell cycle escape, likely potentiating the antitumoral effects of Kit inhibition.[3]

Protocol (from reference)

Cell Research:

[3]

  • Cell lines: human GIST-T1 cell line, human HG129 cell line, human GIST-882 cell line,
  • Concentrations: 2 μM, 6 μM, 12 μM
  • Incubation Time: 48–72h
  • Method:

    To measure cell viability, 1 × 104 GIST-T1, GIST-882, and HG129 cells are seeded in replicates of 5 in a 96-well flat-bottomed plate (Falcon) and cultured for 48–72h with VLX600 or DMSO-only solvent controls.

Animal Research:

[1]

  • Animal Models: female NMRI nu/nu mice (8–10 weeks old)
  • Dosages: 16 mg/kg
  • Administration: IV

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 317.35
Formula

C17H15N7

CAS No. 327031-55-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C2C(=CC=C1)C3=C(N2)N=C(N=N3)NN=C(C)C4=CC=CC=N4

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02222363 Terminated Drug: VLX600 Refractory Cancer Vivolux AB|Theradex February 18 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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