Eflornithine - CAS 70052-12-9
Catalog number: 70052-12-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
Others
Description:
Eflornithine is a difluoromethylated ornithine compound with antineoplastic activity. Eflornithine irreversibly inhibits ornithine decarboxylase, an enzyme required for polyamine biosynthesis, thereby inhibiting the formation and proliferation of tumor cells. Polyamines are involved in nucleosome oligomerization and DNA conformation, creating a chromatin environment that stimulates neoplastic transformation of cells. This agent has been shown to induce apoptosis in leiomyoma cells.
Publictions citing BOC Sciences Products
  • >> More
Synonyms:
CPP-1X, 2-difluoromethylornithine; alpha-difluoromethylornithine; difluromethylornithine;
MSDS:
Inquire
Current Developer:
Cancer Prevention Pharmaceuticals.
1.Translational development of difluoromethylornithine (DFMO) for the treatment of neuroblastoma.
Bassiri H1, Benavides A1, Haber M1, Gilmour SK1, Norris MD1, Hogarty MD1. Transl Pediatr. 2015 Jul;4(3):226-38. doi: 10.3978/j.issn.2224-4336.2015.04.06.
Neuroblastoma is a childhood tumor in which MYC oncogenes are commonly activated to drive tumor progression. Survival for children with high-risk neuroblastoma remains poor despite treatment that incorporates high-dose chemotherapy, stem cell support, surgery, radiation therapy and immunotherapy. More effective and less toxic treatments are sought and one approach under clinical development involves re-purposing the anti-protozoan drug difluoromethylornithine (DFMO; Eflornithine) as a neuroblastoma therapeutic. DFMO is an irreversible inhibitor of ornithine decarboxylase (Odc), a MYC target gene, bona fide oncogene, and the rate-limiting enzyme in polyamine synthesis. DFMO is approved for the treatment of Trypanosoma brucei gambiense encephalitis ("African sleeping sickness") since polyamines are essential for the proliferation of these protozoa. However, polyamines are also critical for mammalian cell proliferation and the finding that MYC coordinately regulates all aspects of polyamine metabolism suggests polyamines may be required to support cancer promotion by MYC.
2.Input estimation for drug discovery using optimal control and Markov chain Monte Carlo approaches.
Trägårdh M1,2, Chappell MJ3, Ahnmark A4, Lindén D4, Evans ND3, Gennemark P5. J Pharmacokinet Pharmacodyn. 2016 Apr;43(2):207-21. doi: 10.1007/s10928-016-9467-z. Epub 2016 Mar 1.
Input estimation is employed in cases where it is desirable to recover the form of an input function which cannot be directly observed and for which there is no model for the generating process. In pharmacokinetic and pharmacodynamic modelling, input estimation in linear systems (deconvolution) is well established, while the nonlinear case is largely unexplored. In this paper, a rigorous definition of the input-estimation problem is given, and the choices involved in terms of modelling assumptions and estimation algorithms are discussed. In particular, the paper covers Maximum a Posteriori estimates using techniques from optimal control theory, and full Bayesian estimation using Markov Chain Monte Carlo (MCMC) approaches. These techniques are implemented using the optimisation software CasADi, and applied to two example problems: one where the oral absorption rate and bioavailability of the drug eflornithine are estimated using pharmacokinetic data from rats, and one where energy intake is estimated from body-mass measurements of mice exposed to monoclonal antibodies targeting the fibroblast growth factor receptor (FGFR) 1c.
3.Quilamine HQ1-44, an iron chelator vectorized toward tumor cells by the polyamine transport system, inhibits HCT116 tumor growth without adverse effect.
Renaud S1, Corcé V2, Cannie I3, Ropert M4, Lepage S5, Loréal O3, Deniaud D6, Gaboriau F7. Biochem Pharmacol. 2015 Aug 1;96(3):179-89. doi: 10.1016/j.bcp.2015.06.001. Epub 2015 Jun 10.
Tumor cell growth requires large iron quantities and the deprivation of this metal induced by synthetic metal chelators is therefore an attractive method for limiting the cancer cell proliferation. The antiproliferative effect of the Quilamine HQ1-44, a new iron chelator vectorized toward tumor cells by a polyamine chain, is related to its high selectivity for the Polyamine Transport System (PTS), allowing its preferential uptake by tumoral cells. The difference in PTS activation between healthy cells and tumor cells enables tumor cells to be targeted, whereas the strong dependence of these cells on iron ensures a secondary targeting. Here, we demonstrated in vitro that HQ1-44 inhibits DNA synthesis and cell proliferation of HCT116 cells by modulating the intracellular metabolism of both iron and polyamines. Moreover, in vivo, in xenografted athymic nude mice, we found that HQ1-44 was as effective as cis-platin in reducing HCT116 tumor growth, without its side effects.
4.Suppression of ornithine decarboxylase promotes osteogenic differentiation of human bone marrow-derived mesenchymal stem cells.
Tsai YH1, Lin KL1, Huang YP2, Hsu YC3, Chen CH4, Chen Y5, Sie MH1, Wang GJ6, Lee MJ7. FEBS Lett. 2015 Jul 22;589(16):2058-65. doi: 10.1016/j.febslet.2015.06.023. Epub 2015 Jun 30.
Ornithine decarboxylase (ODC) is the rate-limiting enzyme for polyamine biosynthesis. Suppression of ODC by its irreversible inhibitor, α-difluoromethylornithine (DFMO), or by RNA interference through siRNA, enhanced osteogenic gene expression and alkaline phosphatase activity, and accelerated matrix mineralization of human bone marrow-derived mesenchymal stem cells (hBMSCs). Besides, adipogenic gene expression and lipid accumulation was attenuated, indicating that the enhanced osteogenesis was accompanied by down-regulation of adipogenesis when ODC was suppressed. A decrease in the intracellular polyamine content of hBMSCs during osteogenic induction was observed, suggesting that the level of endogenous polyamines is regulated during differentiation of hBMSCs. This study elucidates the role of polyamine metabolism in the lineage commitment of stem cells and provides a potential new indication for DFMO as bone-stimulating drug.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Products


CAS 16506-27-7 Bendamustine

Bendamustine
(CAS: 16506-27-7)

Bendamustine, a lbenzimidazol derivative, has been found to be an alkylating agent that acts through restraining DNA synthesis so that could be useful as an ant...

CAS 770691-21-9 Gadobutrol

Gadobutrol
(CAS: 770691-21-9)

Gadobutrol is a nonionic, paramagnetic contrast agent developed for tissue contrast enhancement in magnetic resonance imaging (MRI). It has a macrocyclic framew...

CAS 152378-30-8 (-)-Epibatidine dihydrochloride

(-)-Epibatidine dihydrochloride
(CAS: 152378-30-8)

(-)-Epibatidine dihydrochloride is a highly potent nicotinic agonist and (-)-Enantiomer of (±)-Epibatidine dihydrochloride.

R 428 dihydrochloride

R 428 dihydrochloride is a potent and selective inhibitor of Axl receptor tyrosine kinases (IC50 = 14 nM). R428 inhibits Axl kinase and Axl-dependent events, in...

CAS 53760-19-3 Cytochalasin H

Cytochalasin H
(CAS: 53760-19-3)

Cytochalasin H, a biologically active metabolite was found in crude extracts of an unidentified species of phomopsis isolated from wccvil-damaged pecans, beside...

CAS 101387-97-7 Ro18-5362

Ro18-5362
(CAS: 101387-97-7)

Ro18-5362 is the less active prodrug of Ro 18-5364 which is an extremely potent and rapid inhibitor of the gastric mucosal (H+ + K+)-ATPase.

CAS 452342-37-9 GW-6604

GW-6604
(CAS: 452342-37-9)

GW6604 is a potent and selective ALK-5 inhibitor with an IC(50) of 140 nM and in a cellular assay inhibited TGF-beta-induced transcription of PAI-1 (IC(50): 500...

CAS 374675-21-5 Kisspeptin-10

Kisspeptin-10
(CAS: 374675-21-5)

Kisspeptin-10, also called as Metastin (45-54), is a potent vasoconstrictor and a potent endogenous ligand for the Kisspeptin receptor (KISS1, GPR54).

CAS 22839-47-0 Aspartame

Aspartame
(CAS: 22839-47-0)

Aspartame is an artificial, non-saccharide sweetener used as a sugar substitute in some foods and beverages.

CAS 251994-14-6 CAM-IN-1

CAM-IN-1
(CAS: 251994-14-6)

A potent and selective inhibitor of E-selectin (IC50= 7 nM) and ICAM-1 (IC50= 5 nM)

CAS 611-75-6 Bromhexine Hydrochloride

Bromhexine Hydrochloride
(CAS: 611-75-6)

Bromhexine is a mucolytic (expectorant) agent used in the treatment of respiratory disorders associated with viscid or excessive mucus. In addition, bromhexine ...

CAS 391610-37-0 MCHr1 antagonist 1

MCHr1 antagonist 1
(CAS: 391610-37-0)

A selective antagonist of melanin concentrating hormone-1 (MCH1) receptor

CAS 121-32-4 Ethyl vanillin

Ethyl vanillin
(CAS: 121-32-4)

Ethyl vanillin, a kind of flavorant, could be commonly used in the production of food like chocolate. FEMA No: 2464.

CAS 1916571-90-8 NCT-503

NCT-503
(CAS: 1916571-90-8)

NCT-503 is a non-competitive phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50= 2.5 µM), reducing the production of glucose-derived serine in cells and sup...

CAS 538-71-6 Domiphen Bromide

Domiphen Bromide
(CAS: 538-71-6)

Domiphen bromide is a quaternary ammonium antiseptic with actions as a cationic surfactant.

2'-Cyano-2'-deoxyarabinofuranosylcytosin
(CAS: 134665-72-8)

This compound is a bio-active molecular, but no detailed information has been published yet.

CAS 739-71-9 trimipramine

trimipramine
(CAS: 739-71-9)

Trimipramine is a tricyclic antidepressant. It is serotonin and norepinephrine transport inhibitor with antipsychotic and sedative properties.

Monohydroxy Netupitant
(CAS: 910808-12-7)

Monohydroxy Netupitant is the metabolite of Netupitant which is a potent and selective neurokinin-1 receptor (NK1) receptor antagonist. It is achiral and orally...

CAS 6066-49-5 Butylphthalide <b>(Natural)</b>

Butylphthalide <b>(Natural)</b>
(CAS: 6066-49-5)

Butylphthalide is an anti-cerebral-ischemia drug, which is first isolated from the seeds of celery, showed efficacy in animal models of stroke. It alleviates ox...

CAS 18059-10-4 Peiminine

Peiminine
(CAS: 18059-10-4)

Peiminine and DXS significantly reduced alveolar inflammation and pulmonary interstitial inflammation in rats with bleomycin-induced lung injury. peiminine inhi...

Chemical Structure

CAS 70052-12-9 Eflornithine

Quick Inquiry

Verification code

Featured Items