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Purity: ≥98%
Namodenoson (2-Cl-IB-MECA; CF102; CF-102) is a novel, potent, orally bioavailable, and highly selective adenosine A3 receptor (A3AR) agonist with potential anticancer activity. The agonist of the adenosine A3 receptor CF102 specifically binds to and activates the A3AR expressed on the cell surface. This deregulation of Wnt and NF-kB signal transduction pathways may lead to the apoptosis of tumor cells that express A3AR. Hepatocellular carcinoma (HCC) cells are among the solid tumor cell types that have high expression levels of A3AR, a G protein-coupled receptor that is crucial to cellular proliferation.
| Targets |
A3 adenosine receptor ( Ki = 0.33 nM )
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|---|---|
| ln Vitro |
Namodenoson (2-Cl-IB-MECA) 100 nM significantly reorganized the cytoskeleton in human ADF cells of the astroglial lineage, resulting in the appearance of stress fibers and multiple cell protrusions. High Namodenoson (2-Cl-IB-MECA) concentrations directly result in a Ca2+ influx[2].
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| ln Vivo |
After receiving 200 μg/kg of Namodenoson (2-Cl-IB-MECA) intravenously, there was a brief drop in blood pressure and a 50–100 fold increase in plasma histamine levels. Hemodynamic effects were absent when Namodenoson (2-Cl-IB-MECA) was administered in two doses[1].
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| Cell Assay |
The indicated drug concentrations were applied to the cells for a duration of 48 hours.
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| References | |
| Additional Infomation |
Namodenoson has been used in trials studying the treatment of Chronic Hepatitis C and Hepatocellular Carcinoma.
Namodenoson is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. Namodenoson selectively binds to and activates the cell surface-expressed A3AR, deregulating Wnt and NF-kB signal transduction pathways downstream, which may result in apoptosis of A3AR-expressing tumor cells. A3AR, a G protein-coupled receptor, is highly expressed on the cell surfaces of various solid tumor cell types, including hepatocellular carcinoma (HCC) cells, and plays an important role in cellular proliferation. |
| Molecular Formula |
C18H18CLIN6O4
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|---|---|
| Molecular Weight |
544.7308
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| Exact Mass |
544.012
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| Elemental Analysis |
C, 39.69; H, 3.33; Cl, 6.51; I, 23.30; N, 15.43; O, 11.75
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| CAS # |
163042-96-4
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| PubChem CID |
3035850
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| Appearance |
Solid powder
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| Density |
2.0±0.1 g/cm3
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| Melting Point |
209 °C
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| Index of Refraction |
1.814
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| LogP |
3.14
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
623
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| Defined Atom Stereocenter Count |
4
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| SMILES |
IC1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])N([H])C1=C2C(=NC(=N1)Cl)N(C([H])=N2)[C@@]1([H])[C@@]([H])([C@@]([H])([C@@]([H])(C(N([H])C([H])([H])[H])=O)O1)O[H])O[H]
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| InChi Key |
IPSYPUKKXMNCNQ-PFHKOEEOSA-N
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| InChi Code |
InChI=1S/C18H18ClIN6O4/c1-21-16(29)13-11(27)12(28)17(30-13)26-7-23-10-14(24-18(19)25-15(10)26)22-6-8-3-2-4-9(20)5-8/h2-5,7,11-13,17,27-28H,6H2,1H3,(H,21,29)(H,22,24,25)/t11-,12+,13-,17+/m0/s1
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| Chemical Name |
(2S,3S,4R,5R)-5-[2-chloro-6-[(3-iodophenyl)methylamino]purin-9-yl]-3,4-dihydroxy-N-methyloxolane-2-carboxamide
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| Synonyms |
CF102; Cl-IB-MECA; CF-102; 2-Cl-IB-MECA; CF 102; Namodenoson; Chloro-IB-MECA
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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 |
| 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: ~100 mg/mL (~183.6 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.82 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 20.8 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: 2.08 mg/mL (3.82 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8358 mL | 9.1789 mL | 18.3577 mL | |
| 5 mM | 0.3672 mL | 1.8358 mL | 3.6715 mL | |
| 10 mM | 0.1836 mL | 0.9179 mL | 1.8358 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04697810 | Recruiting | Drug: Namodenoson Drug: Placebo |
NASH - Nonalcoholic Steatohepatitis |
Can-Fite BioPharma | December 10, 2021 | Phase 2 |
| NCT05201404 | Recruiting | Drug: Namodenoson Drug: Placebo |
Hepatocellular Carcinoma Cirrhosis |
Can-Fite BioPharma | March 15, 2023 | Phase 3 |
| NCT02927314 | Completed | Drug: CF102 Drug: Placebo |
Non-alcoholic Steatohepatitis (NASH) |
Can-Fite BioPharma | November 27, 2017 | Phase 2 |
| NCT00790673 | Completed | Drug: CF102 Drug: Placebo |
Chronic Hepatitis C | Can-Fite BioPharma | July 2009 | Phase 1 Phase 2 |
| NCT00790218 | Completed | Drug: CF102 | Hepatocellular Carcinoma | Can-Fite BioPharma | February 2009 | Phase 1 Phase 2 |
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