L-Eflornithine
L-Eflornithine (L-DFMO) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min-1.
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- CAS. Nr.: 66640-93-5
- Formel: C6H12F2N2O2
- Molecular Weight:182.17
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
KD:1.3±0.3 µM (Ornithine decarboxylase, ODC)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | CC50 |
>100 μM
Compound: Eflornithine
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Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTT assay
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[PMID: 29885575] |
| HepG2 | CC50 |
>100 μM
Compound: Eflornithine
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 30092366] |
In Vitro
Eflornithine (D/L-DFMO) is an inhibitor of ODC, the first enzyme in eukaryotic polyamine biosynthesis. Both enantiomers of Eflornithine (DFMO) irreversibly inactivate ODC. Both Eflornithine enantiomers (L-Eflornithine and D-Eflornithine) suppress ODC activity in a time- and concentration-dependent manner. The inhibitor dissociation constant (KD) values for the formation of enzyme-inhibitor complexes are 28.3±3.4, 1.3±0.3 and 2.2±0.4 µM respectively for D-Eflornithine, L-Eflornithine and Eflornithine. The inhibitor inactivation constants (Kinact) for the irreversible step were 0.25±0.03, 0.15±0.03 and 0.15±0.03 min-1 respectively for D-Eflornithine, L-Eflornithine and Eflornithine. Treatment of human colon tumour-derived HCT116 cells with either L-Eflornithine or D- Eflornithine decreases the cellular polyamine contents in a concentration-dependent manner[1]. The enantiomers display different potencies in vitro, with the L-enantiomer having up to a 20-fold higher affinity for the target enzyme ornithine decarboxylase[2].
The L-Eflornithine also appears to be more potent in cultured T.brucei gambiense parasites[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 66640-93-5
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Molecular Weight 182.17
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Formel C6H12F2N2O2
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SMILES
N[C@](CCCN)(C(F)F)C(O)=O
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Synonyms
L-DFMO; L-RMI71782; L-α-difluoromethylornithine
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Qu N, et al. Inhibition of human ornithine decarboxylase activity by enantiomers of difluoromethylornithine. Biochem J. 2003 Oct 15;375(Pt 2):465-70. [Content Brief]
[2]. Jansson-Löfmark R, et al. Enantiospecific reassessment of the pharmacokinetics and pharmacodynamics of oral eflornithine against late-stage Trypanosoma brucei gambiense sleeping sickness. Antimicrob Agents Chemother. 2015 Feb;59(2):1299-307. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
L-Eflornithine Related Classifications
HY-B0744C Related Classifications
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