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VLX600 OXPHOS inhibitor

Name: VLX600
Brand: Selleck Chemicals
SKU: S8943
Rating: 5 (1 reviews)

Cat.No.S8943

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

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%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.68

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Other OXPHOS Inhibitors	IACS-010759 (IACS-10759) ME-344 FCCP Gboxin S-Gboxin 4-Methyl-2-oxovaleric acid BAY-179 Diphenylamine Hydrochloride DX3-213B MS-L6

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	1 year-80°Cin solvent 1 month-20°Cin solvent
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
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	OXPHOS
In vitro	VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. Mitochondrial inhibition with this compound has a direct antitumour effect in vitro while appearing to promote glycolysis through increased AKT signalling 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.
In vivo	VLX600 induces the formation of autolysosomes in vivo. This compound displays tumour growth inhibition in vivo. When combined with imatinib, it reduces p27 expression in vivo, and prevents imatinib-induced cell cycle escape, likely potentiating the antitumoural effects of Kit inhibition.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24548894/ [2] https://pubmed.ncbi.nlm.nih.gov/31523395/ [3] https://pubmed.ncbi.nlm.nih.gov/29246941/

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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