Eflornithine free base
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205260

CAS#: 70052-12-9 (free base)

Description: Eflornithine, also known as Difluoromethylornithine, 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.


Chemical Structure

img
Eflornithine free base
CAS# 70052-12-9 (free base)

Theoretical Analysis

MedKoo Cat#: 205260
Name: Eflornithine free base
CAS#: 70052-12-9 (free base)
Chemical Formula: C6H12F2N2O2
Exact Mass: 182.09
Molecular Weight: 182.168
Elemental Analysis: C, 39.56; H, 6.64; F, 20.86; N, 15.38; O, 17.57

Price and Availability

Size Price Availability Quantity
100mg USD 650 2 weeks
200mg USD 950 2 weeks
500mg USD 1950 2 weeks
1g USD 2950 2 weeks
2g USD 3950 2 weeks
Bulk inquiry

Related CAS #: 70052-12-9 (free base)   96020-91-6 (HCl hydrate)   68278-23-9 (HCl)   69955-42-6 (S-isomer)   70050-55-4 (R-isomer)   66640-93-5 (L-isomer),  

Synonym: CPP-1X; DFMO; MDL 71782; MDL-71782; MDL71782; RMI71782; RMI-71782; RMI 71782; Difluoromethylornithine; Eflornithine

IUPAC/Chemical Name: 2,5-diamino-2-(difluoromethyl)pentanoic acid.

InChi Key: VLCYCQAOQCDTCN-UHFFFAOYSA-N

InChi Code: InChI=1S/C6H12F2N2O2/c7-4(8)6(10,5(11)12)2-1-3-9/h4H,1-3,9-10H2,(H,11,12)

SMILES Code: O=C(O)C(C(F)F)(N)CCCN

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Eflornithine (α-difluoromethylornithine or DFMO) is a drug found to be effective in the treatment of facial hirsutism  (excessive hair growth) as well as in African trypanosomiasis (sleeping sickness). Eflornithine hydrochloride cream, which is for topical administration in women suffering from facial hirsutism, is marketed under the brand name Vaniqa by Almirall in Europe, CSL in Australia, Triton in Canada, Medison in Israel and SkinMedica in the USA.  Eflornithine for injection against sleeping sickness is manufactured by Sanofi Aventis and sold under the brand name Ornidyl in the USA. Both are prescription drugs.  Eflornithine was initially developed for cancer treatment at Merrell Dow Research Institute in the late 1970s, but, while having little use in treating malignancies, it was found to be highly effective in reducing hair growth, as well as in treatment of African trypanosomiasis (sleeping sickness), especially the West African form (Trypanosoma brucei gambiense). (source: http://en.wikipedia.org/wiki/Eflornithine).      

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 182.17 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Jobanputra KS, Rajpal AV, Nagpur NG. Eflornithine. Indian J Dermatol Venereol Leprol. 2007 Sep-Oct;73(5):365-6. doi: 10.4103/0378-6323.35752. PMID: 17921631.


2: Balfour JA, McClellan K. Topical eflornithine. Am J Clin Dermatol. 2001;2(3):197-201; discussion 202. doi: 10.2165/00128071-200102030-00009. PMID: 11705097.


3: Kang CN, Shah M, Lynde C, Fleming P. Hair Removal Practices: A Literature Review. Skin Therapy Lett. 2021 Sep;26(5):6-11. PMID: 34524781.


4: Eflornithine. Am J Health Syst Pharm. 2001 Dec 1;58(23):2244. doi: 10.1093/ajhp/58.23.2244. PMID: 11763800.


5: Van Bogaert I, Haemers A. Eflornithine. A new drug in the treatment of sleeping sickness. Pharm Weekbl Sci. 1989 Jun 23;11(3):69-75. doi: 10.1007/BF02110252. PMID: 2505225.


6: Does eflornithine help women face hirsutism? Drug Ther Bull. 2007 Aug;45(8):62-4. doi: 10.1136/dtb.2007.45862. PMID: 17718095.


7: Burri C, Brun R. Eflornithine for the treatment of human African trypanosomiasis. Parasitol Res. 2003 Jun;90 Supp 1:S49-52. doi: 10.1007/s00436-002-0766-5. Epub 2002 Dec 10. PMID: 12811548.


8: Levin VA, Ictech SE, Hess KR. Clinical importance of eflornithine (α-difluoromethylornithine) for the treatment of malignant gliomas. CNS Oncol. 2018 Apr;7(2):CNS16. doi: 10.2217/cns-2017-0031. Epub 2018 Jan 30. PMID: 29378419; PMCID: PMC5977277.


9: Boberg M, Cal M, Kaiser M, Jansson-Löfmark R, Mäser P, Ashton M. Enantiospecific antitrypanosomal in vitro activity of eflornithine. PLoS Negl Trop Dis. 2021 Jul 12;15(7):e0009583. doi: 10.1371/journal.pntd.0009583. PMID: 34252098; PMCID: PMC8297939.


10: Burke CA, Dekker E, Lynch P, Samadder NJ, Balaguer F, Hüneburg R, Burn J, Castells A, Gallinger S, Lim R, Stoffel EM, Gupta S, Henderson A, Kallenberg FG, Kanth P, Roos VH, Ginsberg GG, Sinicrope FA, Strassburg CP, Van Cutsem E, Church J, Lalloo F, Willingham FF, Wise PE, Grady WM, Ford M, Weiss JM, Gryfe R, Rustgi AK, Syngal S, Cohen A. Eflornithine plus Sulindac for Prevention of Progression in Familial Adenomatous Polyposis. N Engl J Med. 2020 Sep 10;383(11):1028-1039. doi: 10.1056/NEJMoa1916063. PMID: 32905675.


11: Sahai J, Berry AJ. Eflornithine for the treatment of Pneumocystis carinii pneumonia in patients with the acquired immunodeficiency syndrome: a preliminary review. Pharmacotherapy. 1989;9(1):29-33. doi: 10.1002/j.1875-9114.1989.tb04100.x. PMID: 2493638.


12: Shapiro J, Lui H. Vaniqa--eflornithine 13.9% cream. Skin Therapy Lett. 2001 Apr;6(7):1-3, 5. Erratum in: Skin Therapy Lett 2001 May;6(8):5. PMID: 11376395.


13: Coyne PE Jr. The eflornithine story. J Am Acad Dermatol. 2001 Nov;45(5):784-6. doi: 10.1067/mjd.2001.117853. PMID: 11606936.


14: Amilon C, Boberg M, Tarning J, Äbelö A, Ashton M, Jansson-Löfmark R. Population Pharmacodynamic Modeling of Eflornithine-Based Treatments Against Late-Stage Gambiense Human African Trypanosomiasis and Efficacy Predictions of L-eflornithine-Based Therapy. AAPS J. 2022 Mar 25;24(3):48. doi: 10.1208/s12248-022-00693-2. PMID: 35338410.


15: Louis FJ, Keiser J, Simarro PP, Schmid C, Jannin J. L'éflornithine dans le traitement de la maladie du sommeil [Eflornithine in the treatment of African trypanosomiasis]. Med Trop (Mars). 2003;63(6):559-63. French. PMID: 15077414.


16: Rajasekaran S, Bupp CP, Leimanis-Laurens M, Shukla A, Russell C, Junewick J, Gleason E, VanSickle EA, Edgerly Y, Wittmann BM, Prokop JW, Bachmann AS. Repurposing eflornithine to treat a patient with a rare ODC1 gain-of-function variant disease. Elife. 2021 Jul 20;10:e67097. doi: 10.7554/eLife.67097. PMID: 34282722; PMCID: PMC8291972.


17: Priotto G, Kasparian S, Ngouama D, Ghorashian S, Arnold U, Ghabri S, Karunakara U. Nifurtimox-eflornithine combination therapy for second-stage Trypanosoma brucei gambiense sleeping sickness: a randomized clinical trial in Congo. Clin Infect Dis. 2007 Dec 1;45(11):1435-42. doi: 10.1086/522982. Epub 2007 Oct 22. PMID: 17990225.


18: Smith SR, Piacquadio DJ, Beger B, Littler C. Eflornithine cream combined with laser therapy in the management of unwanted facial hair growth in women: a randomized trial. Dermatol Surg. 2006 Oct;32(10):1237-43. doi: 10.1111/j.1524-4725.2006.32282.x. PMID: 17034372.


19: Priotto G, Kasparian S, Mutombo W, Ngouama D, Ghorashian S, Arnold U, Ghabri S, Baudin E, Buard V, Kazadi-Kyanza S, Ilunga M, Mutangala W, Pohlig G, Schmid C, Karunakara U, Torreele E, Kande V. Nifurtimox-eflornithine combination therapy for second-stage African Trypanosoma brucei gambiense trypanosomiasis: a multicentre, randomised, phase III, non-inferiority trial. Lancet. 2009 Jul 4;374(9683):56-64. doi: 10.1016/S0140-6736(09)61117-X. Epub 2009 Jun 24. PMID: 19559476.


20: Kumar A, Naguib YW, Shi YC, Cui Z. A method to improve the efficacy of topical eflornithine hydrochloride cream. Drug Deliv. 2016 Jun;23(5):1495-501. doi: 10.3109/10717544.2014.951746. Epub 2014 Sep 3. PMID: 25182303; PMCID: PMC4348346.