Eflornithine (DFMO) |
Katalog-Nr.GC30283 |
Eflornithin (DFMO) ist ein spezifischer, irreversibler Inhibitor des Enzyms Ornithindecarboxylase.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 70052-12-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
OVCAR5 and SKOV3 cells |
Preparation Method |
Cells were treated with 0.5 mM Eflornithine (DFMO) and rucaparib. |
Reaction Conditions |
0.5 mM Eflornithine ;72h |
Applications |
Eflornithine Sensitizes homologous recombination (HR)-Competent Ovarian Cancer Cells to Rucaparib. |
Animal experiment [2]: | |
Animal models |
Pancreas of athymic (nu/nu) mice (Human pancreatic L3.6pl tumor model) |
Preparation Method |
Mice were treated for two weeks with control, GW5074 (1 mg/kg), Eflornithine (1% w/v) and Eflornithine + GW5074 after a week post orthotopic tumor cell implantation. |
Dosage form |
1% w/v Eflornithine in the drinking water; 48-72 h |
Applications |
Eflornithinealone markedly increases survival of pancreatic tumor-bearing mice in contrast with GW5074 across multiple dosing and tumor seeding strategies. |
References: [1]. El Naggar O, Doyle B, et,al. Difluoromethylornithine (DFMO) Enhances the Cytotoxicity of PARP Inhibition in Ovarian Cancer Cells. Med Sci (Basel). 2022 May 26;10(2):28. doi: 10.3390/medsci10020028. PMID: 35736348; PMCID: PMC9230675. |
Eflornithine(DFMO) inhibits polyamine biosynthesis by irreversible inhibition of ornithine decarboxylase(ODC). It is a chemotherapeutic protectant that blocks angiogenesis. Its biological half-life is 8 hours[1-2].
Eflornithine (0.5 mM DFMO;72h) sensitizes homologous recombination (HR)-Competent Ovarian Cancer Cells to Rucaparib [3]. Combination of Eflornithine (1 mM; 48 h) and Thymoquinone (TQ) significantly reduced cell viability and resulted in significant synergistic effects on apoptosis when compared to either Eflornithine or TQ alone in Jurkat cells [4]. Eflornithine (5 mM;72h) treatment leads to the accumulation of the cyclin-dependent kinase inhibitor p27(Kip1) protein and causes p27(Kip1)/Rb-coupled G (1) cell cycle arrest in MYCN-amplified NB tumor cells through a process that involves p27(Kip1) phosphorylation at residues Ser10 and Thr198[5].
Eflornithine (1% w/v in the drinking water; 48-72 h) alone markedly increases survival of pancreatic tumor-bearing mice in contrast with GW5074 across multiple dosing and tumor seeding strategies [6]. The Kras(G12D/+) mice fed Eflornithine at 0.1% and 0.2% in the diet showed a significant inhibition of pancreatic ductal adenocarcinoma (PDAC) incidence compared with mice fed control diet [7].
References:
[1]. Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006-. Eflornithine. 2021 Dec 20. PMID: 29999676.
[2]. Kang CN, Shah M, et,al. Hair Removal Practices: A Literature Review. Skin Therapy Lett. 2021 Sep;26(5):6-11. PMID: 34524781.
[3]. El Naggar O, Doyle B, et,al. Difluoromethylornithine (DFMO) Enhances the Cytotoxicity of PARP Inhibition in Ovarian Cancer Cells. Med Sci (Basel). 2022 May 26;10(2):28. doi: 10.3390/medsci10020028. PMID: 35736348; PMCID: PMC9230675.
[4]. Alhosin M, Razvi SSI, et,al. Thymoquinone and Difluoromethylornithine (DFMO) Synergistically Induce Apoptosis of Human Acute T Lymphoblastic Leukemia Jurkat Cells Through the Modulation of Epigenetic Pathways. Technol Cancer Res Treat. 2020 Jan-Dec;19:1533033820947489. doi: 10.1177/1533033820947489. PMID: 32912061; PMCID: PMC7488875.
[5]. Koomoa DL, Geerts D, et,al. DFMO/eflornithine inhibits migration and invasion downstream of MYCN and involves p27Kip1 activity in neuroblastoma. Int J Oncol. 2013 Apr;42(4):1219-28. doi: 10.3892/ijo.2013.1835. Epub 2013 Feb 21. PMID: 23440295; PMCID: PMC3622674.
[6]. Nakkina SP, Gitto SB, et,al. DFMO Improves Survival and Increases Immune Cell Infiltration in Association with MYC Downregulation in the Pancreatic Tumor Microenvironment. Int J Mol Sci. 2021 Dec 7;22(24):13175. doi: 10.3390/ijms222413175. PMID: 34947972; PMCID: PMC8706739.
[7]. Mohammed A, Janakiram NB, et,al. Eflornithine (DFMO) prevents progression of pancreatic cancer by modulating ornithine decarboxylase signaling. Cancer Prev Res (Phila). 2014 Dec;7(12):1198-209. doi: 10.1158/1940-6207.CAPR-14-0176. Epub 2014 Sep 23. PMID: 25248858; PMCID: PMC4310684.
Cas No. | 70052-12-9 | SDF | |
Canonical SMILES | NC(CCCN)(C(F)F)C(O)=O | ||
Formula | C6H12F2N2O2 | M.Wt | 182.17 |
Löslichkeit | Soluble in H2O | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 5.4894 mL | 27.4469 mL | 54.8938 mL |
5 mM | 1.0979 mL | 5.4894 mL | 10.9788 mL |
10 mM | 0.5489 mL | 2.7447 mL | 5.4894 mL |
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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