Eflornithine (DFMO) hydrochloride hydrate

Synonyms: Difluoromethylornithine hydrochloride hydrate, MDL-71782 hydrochloride hydrate, RMI-71782 hydrochloride hydrate, α-difluoromethylornithine hydrochloride hydrate

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.

Eflornithine (DFMO) hydrochloride hydrate Chemical Structure

Eflornithine (DFMO) hydrochloride hydrate Chemical Structure

CAS No. 96020-91-6

Purity & Quality Control

Eflornithine (DFMO) hydrochloride hydrate Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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

Biological Activity

Description 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.
Targets
Orn decarboxylase [2]
In vitro
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].

Cell Research Cell lines BY2 cell
Concentrations 2 mM
Incubation Time 48 h
Method

BY2 cells are treated with or without cryptogein in the presence or absence of DFMO(Difluoromethylornithine) and monitered the effect of chemicals on cell growth.

Experimental Result Images Methods Biomarkers Images 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
In Vivo
In vivo

Eflornithine alters changes in vascular responsiveness associated with coarctation hypertension

Animal Research Animal Models Rats
Dosages 400 mg/kg
Administration s.c.
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

Chemical Information & Solubility

Molecular Weight 236.64 Formula

C6H12F2N2O2.HCl.H2O

CAS No. 96020-91-6 SDF Download Eflornithine (DFMO) hydrochloride hydrate SDF
Smiles C(CC(C(F)F)(C(=O)O)N)CN.O.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 47 mg/mL

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

Ethanol : Insoluble


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In vivo
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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.
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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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