Home Apoptosis OXPHOS inhibitor - Autophagy activator - Mitochondrial Metabolism inhibitor VLX600 For research use only.

VLX600

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

VLX600 Chemical Structure

CAS: 327031-55-0

Selleck's VLX600 has been cited by 1 publication

Purity & Quality Control

Batch: S894301 DMSO] 13 mg/mL] false] Water] ˂1 mg/mL] false] Ethanol] ˂1 mg/mL] false Purity: 99.68%
99.68

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models female NMRI nu/nu mice (8–10 weeks old)
Dosages 16 mg/kg
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02222363 Terminated
Refractory Cancer
Vivolux AB|Theradex
 February 18 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 317.35 Formula

C17H15N7
CAS No. 327031-55-0 SDF --
Smiles CC1=C2C(=CC=C1)C3=C(N2)N=C(N=N3)NN=C(C)C4=CC=CC=N4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 13 mg/mL ( (40.96 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL


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In vivo
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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.

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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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