Home Metabolism Carbohydrate Metabolism modulator - Other inhibitor Lonidamine For research use only.

Lonidamine

Synonyms: AF-1890, Diclondazolic Acid, DICA

Lonidamine is an orally administered small molecule hexokinase inactivator.

Lonidamine Chemical Structure

Lonidamine Chemical Structure

CAS No. 50264-69-2

Purity & Quality Control

Lonidamine Related Products

Biological Activity

Description Lonidamine is an orally administered small molecule hexokinase inactivator.
Targets
hexokinase [1]
In vitro
In vitro

Lonidamine reduces the oxygen consumption in both normal and neoplastic cells, while it increases the aerobic glycolysis of normal cells but inhibited that of tumor cells. [1]

Lonidamine induces the permeabilization of ANT proteoliposomes in a cell-free system, yet has no effect on protein-free liposomes. Lonidamine adds to synthetic planar lipid bilayers containing ANT, eliciting ANT channel activities with clearly distinct conductance levels. [2]

Lonidamine provokes a disruption of the mitochondrial transmembrane potential which precedes signs of nuclear apoptosis and cytolysis. Lonidamine causes the dissipation of the mitochondrial inner transmembrane potential and the release of apoptogenic factors capable of inducing nuclear apoptosis in vitro. [3]

Lonidamine (50 mg/mL) induces apoptosis in resistant cells (MCF-7 ADR(r) human breast cancer cell line, and LB9 glioblastoma multiform cell line), as demonstrated by sub-G1 peaks in DNA content histograms, condensation of nuclear chromatin, and internucleosomal DNA fragmentation. [4]

Lonidamine has a stronger effect on glioblastoma cell proliferation and metabolism in vitro than did either agent used alone. [5]
In Vivo
In vivo

Lonidamine (160 mg/kg) in combination is significantly more effective in reducing glioblastoma tumor growth than either drug alone in mice, this tumor growth retardation is maintained as long as treatment is given. [5]
Animal Research Animal Models Female nu/nu mice
Dosages 80 mg/kg
Administration Tail vein
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02758860 Completed
Colonic Diverticula
University of Roma La Sapienza
 June 2016 --
NCT00182078 Completed
Posttraumatic Stress Disorder|Depression
Massachusetts General Hospital
 November 2002 Phase 4

Chemical Information & Solubility

Molecular Weight 321.16 Formula

C15H10Cl2N2O2
CAS No. 50264-69-2 SDF Download Lonidamine SDF
Smiles C1=CC=C2C(=C1)C(=NN2CC3=C(C=C(C=C3)Cl)Cl)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 64 mg/mL ( (199.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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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Frequently Asked Questions

Question 1:
Could you please test an in vivo formulation for this drug? Can it be administrated via i.p. injection?

Answer:
The suggested IP formula of S2610 is 5%DMSO+30%PEG300+5%Tween-80+ddH2O.

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