Lonidamine (AF-1890)

Catalog No.S2610 Synonyms: Diclondazolic Acid, DICA

For research use only.

Lonidamine (AF 1890, Diclondazolic Acid, DICA) is an orally administered small molecule hexokinase inactivator.

Lonidamine (AF-1890) Chemical Structure

CAS No. 50264-69-2

Selleck's Lonidamine (AF-1890) has been cited by 7 Publications

Purity & Quality Control

Choose Selective Carbohydrate Metabolism Inhibitors

Biological Activity

Description Lonidamine (AF 1890, Diclondazolic Acid, DICA) is an orally administered small molecule hexokinase inactivator.
Targets
hexokinase [1]
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 adriamycin and nitrosourea-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 Lonidamine (160 mg/kg) combined with Diazepam 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]

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%DMSO+30% PEG300+5%Tween-80+ddH2O
For best results, use promptly after mixing.

6mg/mL

Chemical Information

Molecular Weight 321.16
Formula

C15H10Cl2N2O2

CAS No. 50264-69-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C2C(=C1)C(=NN2CC3=C(C=C(C=C3)Cl)Cl)C(=O)O

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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 %

Calculation results:

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.

Molarity Calculator

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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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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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