Eflornithine (MDL-71782) hydrochloride hydrate

For research use only.

Catalog No.S4582 Synonyms: Difluoromethylornithine hydrochloride hydrate, DFMO hydrochloride hydrate, RMI-71782 hydrochloride hydrate, α-difluoromethylornithine hydrochloride hydrate

4 publications

Eflornithine (MDL-71782) hydrochloride hydrate Chemical Structure

CAS No. 96020-91-6

Eflornithine (Difluoromethylornithine, DFMO, MDL-71782, RMI-71782, α-difluoromethylornithine) 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.

Selleck's Eflornithine (MDL-71782) hydrochloride hydrate has been cited by 4 publications

Purity & Quality Control

Choose Selective Decarboxylase Inhibitors

Biological Activity

Description Eflornithine (Difluoromethylornithine, DFMO, MDL-71782, RMI-71782, α-difluoromethylornithine) 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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
J774.1 M1mzV2FvfGm2conwZY5we2:vYXygZZN{[Xl? MknEOFghcHK| NXHwdnE5SW62aYTyfZBidm:|b33hcEBi[3Srdnn0fUBi\2GrboP0JHRzgXCjbn;zc41iKGK{dXPlbUBjenWlZXmgWGMzOjFiaX7m[YN1\WRiaX6gcY92e2ViSke3OE4yKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDhcIFu[XJiYnz1[UBie3OjeTygTWM2OCB;IEKyMlkh|ryPLh?= NYjwPG1CRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzO|YxPzJpPkKyN|c3ODd{PD;hQi=>
A673 NH\XVoNyUFSVIHHzd4F6 M{\TXJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| NGrtTnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 NHfjO|hyUFSVIHHzd4F6 Mmq5dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC NH6xUpJyUFSVIHHzd4F6 NHjNbnFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> M12wOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
c-Myc / α-tubulin; 

PubMed: 25248858     


C. Effect of DFMO on c-Myc protein expression. A decrease in c-Myc expression was seen upon DFMO treatment.

25248858
Growth inhibition assay
2T1 cells; 

PubMed: 21093499     


AAT6 knockdown confers resistance to eflornithine. The RNAit program was used to design primers and the pRPaiSL construct was modified to target AAT6 for RNAi. The resulting hairpin RNAi constructs were transferred to 2T1 cells. For EC50 determination, cells were seeded at 2 × 103 ml−1 in 96-well plates in an eflornithine 2-fold dilution series. After 66 h growth, 20 μl of Alamar blue (AbD serotec) was added to each well and the plates incubated for a further 6 h. Fluorescence was determined using a Gemini Fluorescent Plate reader (Molecular Devices) at an excitation wavelength of 530 nm, an emission wavelength of 585 nm and a filter cut-off of 570 nm.

21093499
IHC
H&E staining of pancreas; 

PubMed: 25248858     


A. Histopathologic analysis of untreated and DFMO-treated pancreas using H&E staining. Pancreas from untreated animals showing poorly differentiated adenocarcinoma with some of the cells invading stroma (left panel). Pancreas from animals treated with DFMO showing PanIN lesions (right panels).

p21 / PCNA; 

PubMed: 25248858     


Effect of DFMO on pancreatic tumor cell proliferation. A. Immunohistochemical analysis for PCNA and p21 was performed on paraffin-embedded and micro-sectioned pancreatic tissues as described in the Methods section. A significantly decreased expression of PCNA and increased p21 expression was seen with DFMO treatment.

25248858
IHC/IF
ODC expression in pancreatic tumors; 

PubMed: 25248858     


Effect of DFMO on ODC expression in pancreatic tumors. Immunohistochemical and Immunofluorescence analyses were performed with paraffin-embedded and micro-sectioned pancreatic tissues as described in the Methods section. A significantly decreased expression of ODC was seen with DFMO treatment.

Cav-1 / β-catenin; 

PubMed: 25248858     


Effect of DFMO on cav-1 and β-catenin. Immunohistochemistry (top row of each set), Immunofluorescence (bottom row of each set) and mRNA analysis (bar graphs to the right) revealed a decrease in the cav-1 expression with both doses of DFMO; however, only the high dose (0.2%) caused a decrease in β-catenin expression.

25248858

Protocol

Cell Research:

[1]

- Collapse
  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro Water 47 mg/mL (198.61 mM)
DMSO Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 236.64
Formula

C6H12F2N2O2.HCl.H2O

CAS No. 96020-91-6
Storage powder
in solvent
Synonyms Difluoromethylornithine hydrochloride hydrate, DFMO hydrochloride hydrate, RMI-71782 hydrochloride hydrate, α-difluoromethylornithine hydrochloride hydrate
Smiles C(CC(C(F)F)(C(=O)O)N)CN.O.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04696029 Recruiting Drug: Difluoromethylornithine Medulloblastoma Giselle SaulnierSholler|Atrium Health March 29 2021 Phase 2
NCT03536728 Recruiting Drug: AMXT1501|Drug: DFMO Cancer|Solid Tumor|Solid Carcinoma|Advanced Cancer Aminex Therapeutics Inc. June 12 2018 Phase 1
NCT02794428 Recruiting Drug: Eflornithine|Other: Eflornithine placebo Gastric Cancer|Gastric Intestinal Metaplasia Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI)|Cancer Prevention Pharmaceuticals Inc. September 19 2016 Phase 2
NCT02636569 Active not recruiting Drug: topical diclofenac daily|Drug: placebo Non-melanoma Skin Cancer University of Alabama at Birmingham February 2016 Not Applicable
NCT01636128 Withdrawn Drug: difluoromethylornithine|Drug: Sulindac Focus of Study: Drug Response Biomarkers Chemoprevention Neoplasms Cancer Prevention Pharmaceuticals Inc.|University of Arizona March 2014 Phase 2
NCT01586260 Active not recruiting Drug: DFMO Neuroblastoma Giselle SaulnierSholler|Cancer Prevention Pharmaceuticals Inc.|University of Arizona|University of Hawaii|University of Vermont|Beat NB Cancer Foundation|Atrium Health June 2012 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID