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MedKoo Cat#: 205260 | Name: Eflornithine free base
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Description:

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

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

Eflornithine free base
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: 182.0867

Molecular Weight: 182.17

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 650.00 2 weeks
200mg USD 950.00 2 weeks
500mg USD 1,950.00 2 weeks
1g USD 2,950.00 2 weeks
2g USD 3,950.00 2 weeks
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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).      

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
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.

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DBCO-NH-Boc

DBCO-NH-Boc

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