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Eflornithine (DFMO) hydrochloride hydrate Decarboxylase inhibitor

Name: Eflornithine (DFMO) hydrochloride hydrate
Brand: Selleck Chemicals
SKU: S4582
Availability: InStock
Rating: 5 (9 reviews)

Cat.No.S4582

Eflornithine (DFMO) hydrochloride hydrate inhibits polyamine biosynthesis by the selective, irreversible inhibition of ornithine decarboxylase (ODC). A chemoprotective agent that blocks angiogenesis. Its biological half-life is 8 hours.

Chemical Structure

Molecular Weight: 236.64

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: >97%

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR Acyltransferase
Related Products	Benserazide HCl

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
J774.1	Antitrypanosomal assay	48 hrs	Antitrypanosomal activity against Trypanosoma brucei brucei TC221 infected in mouse J774.1 cells after 48 hrs by alamar blue assay, IC50 = 22.9 μM.	22376072
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	236.64	Formula	C₆H₁₂F₂N₂O₂.HCl.H₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	96020-91-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Difluoromethylornithine hydrochloride hydrate, MDL-71782 hydrochloride hydrate, RMI-71782 hydrochloride hydrate, α-difluoromethylornithine hydrochloride hydrate			Smiles	C(CC(C(F)F)(C(=O)O)N)CN.O.Cl

Solubility

In vitro
Batch:

Water : 47 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble

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+ %

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.

Mechanism of Action

Targets/IC₅₀/Ki	Orn decarboxylase ^[2]
In vitro	When cultured cells are treated with α-difluoromethyl-Orn, an inhibitor of polyamine biosynthesis, production of hydrogen peroxide is suppressed and programmed cell death did not occur^[1].
In vivo	Eflornithine alters changes in vascular responsiveness associated with coarctation hypertension
References	https://pubmed.ncbi.nlm.nih.gov/16844838/ https://pubmed.ncbi.nlm.nih.gov/12913153/ https://pubmed.ncbi.nlm.nih.gov/9107438/

Applications

Methods	Biomarkers	PMID
Western blot	c-Myc / α-tubulin	25248858
Growth inhibition assay	2T1 cells	21093499
IHC	H&E staining of pancreas p21 / PCNA	25248858
IHC/IF	ODC expression in pancreatic tumors Cav-1 / β-catenin	25248858

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05594563	Recruiting	Type 1 Diabetes	Emily K. Sims\|Juvenile Diabetes Research Foundation\|Cancer Prevention Pharmaceuticals Inc.\|Indiana University	March 14 2023	Phase 2
NCT05500508	Recruiting	Cancer\|Solid Tumor\|Solid Carcinoma\|Advanced Cancer\|DIPG Brain Tumor\|Ovary Cancer\|Breast Cancer\|Papillary Thyroid Cancer\|Head and Neck Cancer\|Gastric Cancer\|Nsclc\|Mesotheliomas Pleural\|Mesothelioma Peritoneum\|Esophageal Cancer\|Diffuse Midline Glioma H3 K27M-Mutant\|Endometrial Cancer\|Cervical Cancer\|Melanoma\|Colorectal Cancer\|Glioma Malignant	Aminex Therapeutics Inc.	November 29 2022	Phase 1\|Phase 2
NCT04696029	Recruiting	Medulloblastoma	Giselle Sholler\|Milton S. Hershey Medical Center	March 29 2021	Phase 2
NCT03536728	Completed	Cancer\|Solid Tumor\|Solid Carcinoma\|Advanced Cancer	Aminex Therapeutics Inc.	June 12 2018	Phase 1
NCT02636569	Active not recruiting	Non-melanoma Skin Cancer	University of Alabama at Birmingham	October 25 2017	Phase 2

Tech Support

Handling Instructions

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