Home Apoptosis OXPHOS inhibitor - Autophagy activator - Mitochondrial Metabolism inhibitor VLX600

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VLX600 OXPHOS inhibitor

Cat.No.S8943

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

Chemical Structure

Molecular Weight: 317.35

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 317.35 Formula

C17H15N7

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 327031-55-0 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=C2C(=CC=C1)C3=C(N2)N=C(N=N3)NN=C(C)C4=CC=CC=N4

Solubility

In vitro
Batch:

DMSO : 13 mg/mL (40.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
OXPHOS [2]
In vitro

VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation.[1] Mitochondrial inhibition with this compound has a direct antitumor effect in vitro while appearing to promote glycolysis through increased AKT signaling and glucose transporter expression. When combined with imatinib, this chemical 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. This compound displays tumour growth inhibition in vivo.[1] When combined with imatinib, it reduces p27 expression in vivo, and prevents imatinib-induced cell cycle escape, likely potentiating the antitumoral effects of Kit inhibition.[3]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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