Namodenoson (2 Cl-IB-MECA; CF102)

Alias: CF102; Cl-IB-MECA; CF-102; 2-Cl-IB-MECA; CF 102; Namodenoson; Chloro-IB-MECA

Cat No.:V17958 Purity: ≥98%

COA Product Data Instructions for use SDS

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.

Namodenoson (2 Cl-IB-MECA; CF102) Chemical Structure CAS No.: 163042-96-4
Product category: Adenosine Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

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Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

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.

Biological Activity I Assay Protocols (From Reference)

Targets	A3 adenosine receptor ( Ki = 0.33 nM )
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].
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].
Cell Assay	The indicated drug concentrations were applied to the cells for a duration of 48 hours.
References	[1]. Hemodynamic effects and histamine release elicited by the selective adenosine A3 receptor agonist 2-Cl-IB-MECA in conscious rats. Eur J Pharmacol. 1996 Jul 25;308(3):311-4. [2]. Adenosine A3 receptors: novel ligands and paradoxical effects. Trends Pharmacol Sci. 1998 May;19(5):184-91.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C18H18CLIN6O4
Molecular Weight	544.7308
Exact Mass	544.01
Elemental Analysis	C, 39.69; H, 3.33; Cl, 6.51; I, 23.30; N, 15.43; O, 11.75
CAS #	163042-96-4
Appearance	Solid powder
SMILES	CNC(=O)[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=C(N=C32)Cl)NCC4=CC(=CC=C4)I)O)O
InChi Key	IPSYPUKKXMNCNQ-PFHKOEEOSA-N
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
Chemical Name	(2S,3S,4R,5R)-5-[2-chloro-6-[(3-iodophenyl)methylamino]purin-9-yl]-3,4-dihydroxy-N-methyloxolane-2-carboxamide
Synonyms	CF102; Cl-IB-MECA; CF-102; 2-Cl-IB-MECA; CF 102; Namodenoson; Chloro-IB-MECA
HS Tariff Code	2934.99.9001
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)

Solubility Data

Solubility (In Vitro)	DMSO: ~100 mg/mL (~183.6 mM)
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. 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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO: ~100 mg/mL (~183.6 mM)

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.
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 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	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.

Calculator

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
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The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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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.

Note： (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.

Clinical Trial Information

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

Biological Data

Averaged time profiles of mean arterial pressure (upper panel) and heart rate (lower panel); conscious rats received two subsequent i.v. infusions of 200 μg/kg 2-Cl-IB-MECA in 15 min (●) or vehicle in 15 min (▲); the filled bars represent the two infusion periods; data are presented as mean ± S.E. (n = 6). Eur J Pharmacol . 1996 Jul 25;308(3):311-4.

Plasma histamine concentration vs. time profile for rats which received two subsequent i.v. infusions of 200 μg/kg 2-Cl-IB-MECA in 15 min; the filled bars represent the two infusion periods. Eur J Pharmacol . 1996 Jul 25;308(3):311-4.

Cardioprotection elicited by the selective A₃ adenosine receptor agonists, N⁶-(3-iodobenzyl)-adenosine-5′-N-methyluronamide (IB-MECA) and Cl-IB-MECA, during prolonged ischaemia (modified from Ref. 16). Trends Pharmacol Sci . 1998 May;19(5):184-91.