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Furamidine 2HCl, the dihydrochloride salt of Furamidine, is an abisbenzamidine analog and an antiparasite agent. It actis as an inhibitor of protein arginine methyltransferase 1 (PRMT1). Furamidine is also a competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor.
| ln Vitro |
Nitrofuranzidine dihydrochloride (Compound 1; 20 μM; 72 hours; white cell lines) suppresses the proliferation of most white cell lines [1], with the exception of JAK2V617F HEL cells. The expression level of methylated GFP-ALY protein in 293T cells was considerably lowered after 15 hours of treatment with nitrofuranzidine (20 μM) dihydrochloride [1]. It is also possible to inject furosidine hydrochloride in between the GC base pairs of double-stranded DNA. Therefore, TDP and other enzymes involved in DNA processing may be affected by nitrofuranzidine hydrochloride.
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| ln Vivo |
Nitrofuranzidine (1 mg/kg; i.p.; three times weekly, every 4 weeks; for 34 weeks; female NZB/NZW mice) dihydrochloride and irinotecan, when combined, decreased proteinuria. Prolonged NZB/combination treatment does not change anti-dsDNA antibody levels in lupus-prone persons [3].
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: Meg-01, K562, HL-60, NB4, MOLM13, HEL, CMK, CMY, CMS and CHRF Cell Tested Concentrations: 20 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited cell growth of most leukemia cell lines, except HEL cells with JAK2V617F mutation. Western Blot Analysis [1] Cell Types: 293T cells Tested Concentrations: 20 μM Incubation Duration: 15 hrs (hours) Experimental Results: The expression level of methylated GFP-ALY protein was Dramatically diminished. |
| Animal Protocol |
Animal/Disease Models: Female NZB/NZW mice (6 weeks old) treated with irinotecan (1 mg/kg)[3]
Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection; 3 times a week, repeated every 4 weeks ; Lasts 34 weeks Experimental Results: Combination with irinotecan suppresses proteinuria and extends survival in lupus-prone NZB/NZW mice. |
| References |
[1]. Yan L, et al. Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J Med Chem. 2014 Mar 27;57(6):2611-22.
[2]. Antony S, et al. Novel high-throughput electrochemiluminescent assay for identification of human tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors and characterization of furamidine (NSC 305831) as an inhibitor of Tdp1. Nucleic Acids Res. 2007;35(13):4474-84. [3]. Keil A, et al. The Topoisomerase I Inhibitor Irinotecan and the Tyrosyl-DNA Phosphodiesterase 1 Inhibitor Furamidine Synergistically Suppress Murine Lupus Nephritis. Arthritis Rheumatol. 2015 Jul;67(7):1858-67. |
| Molecular Formula |
C18H16N4O
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|---|---|
| Molecular Weight |
304.34584
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| Exact Mass |
340.109
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| CAS # |
55368-40-6
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| Related CAS # |
Furamidine;73819-26-8
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| PubChem CID |
126437
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.583
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
396
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C2=CC=C(O2)C3=CC=C(C=C3)C(=N)N)C(=N)N.Cl.Cl
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| InChi Key |
ZJHZBDRZEZEDGB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16N4O/c19-17(20)13-5-1-11(2-6-13)15-9-10-16(23-15)12-3-7-14(8-4-12)18(21)22/h1-10H,(H3,19,20)(H3,21,22)
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| Chemical Name |
4-[5-(4-carbamimidoylphenyl)furan-2-yl]benzenecarboximidamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~33.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2857 mL | 16.4285 mL | 32.8569 mL | |
| 5 mM | 0.6571 mL | 3.2857 mL | 6.5714 mL | |
| 10 mM | 0.3286 mL | 1.6428 mL | 3.2857 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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