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| 5mg |
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| 25mg |
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Piclidenoson, formerly known as CF101, is a specific agonist to the A3 adenosine receptor, which inhibits the development of colon carcinoma growth in cell cultures and xenograft murine models. It has been demonstrated that CF101 suppresses the expression of the PKB/Akt and NF-κB proteins. Drug resistance is avoided by CF101, which increases the cytotoxic effect of 5-FU. The development of CF101 as a 5-FU adjunct treatment is suggested by its myeloprotective effect.
| Targets |
A3AR
|
|---|---|
| ln Vitro |
Piclidenoson can reduce the amount of cAMP stimulated by forskolin, with EC50 values in OVCAR-3 cells of 0.82 μM and in Caov-4 cells of 1.2 μM, respectively [2].
Piclidenoson (0.0001-100 μM; 48 hours) dramatically lowers human ovarian line cell viability in a dose-dependent manner; for OVCAR-3 and Caov-4 cells, the IC50s are 32.14 μM and 45.37 μM, respectively [2]. Piclidenoson (0.001-100 μM; 48 hours) through the caspase pathway. |
| ln Vivo |
Piclidenoson (105 μg/kg; IP) improvement γ The survival rate of irradiated mice [3].
|
| Cell Assay |
Cell Line: OVCAR-3 cells, Caov-4 cells
Concentration: 0.0001-100 μM Incubation Time: 48 hours Result: Resulted in a dose-dependent reduction in the cell viability. |
| Animal Protocol |
B10CBAF1 male mice aged 3 months (average 30 g)
105 μg/kg Intraperitoneal injection, 0.5 h after irradiation |
| References |
|
| Molecular Formula |
C18H19IN6O4
|
|---|---|
| Molecular Weight |
510.28
|
| Exact Mass |
510.05
|
| Elemental Analysis |
C, 42.37; H, 3.75; I, 24.87; N, 16.47; O, 12.54
|
| CAS # |
152918-18-8
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| Related CAS # |
152918-18-8
|
| Appearance |
Solid powder
|
| SMILES |
O=C([C@H]1O[C@@H](N2C=NC3=C(NCC4=CC=CC(I)=C4)N=CN=C23)[C@H](O)[C@@H]1O)NC
|
| InChi Key |
HUJXGQILHAUCCV-MOROJQBDSA-N
|
| InChi Code |
InChI=1S/C18H19IN6O4/c1-20-17(28)14-12(26)13(27)18(29-14)25-8-24-11-15(22-7-23-16(11)25)21-6-9-3-2-4-10(19)5-9/h2-5,7-8,12-14,18,26-27H,6H2,1H3,(H,20,28)(H,21,22,23)/t12-,13+,14-,18+/m0/s1
|
| Chemical Name |
(2S,3S,4R,5R)-3,4-dihydroxy-5-(6-(3-iodobenzylamino)-9H-purin-9-yl)-N-methyltetrahydrofuran-2-carboxamide
|
| Synonyms |
ALB-7208; ALB 7208; CF101; CF-101; CF 101; ALB7208; IB MECA; Piclidenoson
|
| 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 (In Vitro) |
DMSO: ≥ 45 mg/mL (~88.2 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.90 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 25.0 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: ≥ 2.5 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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: ≥ 2.5 mg/mL (4.90 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 | 1.9597 mL | 9.7985 mL | 19.5971 mL | |
| 5 mM | 0.3919 mL | 1.9597 mL | 3.9194 mL | |
| 10 mM | 0.1960 mL | 0.9799 mL | 1.9597 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 |
| NCT04333472 | Completed | Drug: Piclidenoson Drug: Placebo |
COVID-19 Coronavirus Infection |
Can-Fite BioPharma | January 6, 2021 | Phase 2 |
| NCT00349466 | Completed | Drug: CF101 Drug: Placebo |
Keratoconjunctivitis Sicca | Can-Fite BioPharma | January 2007 | Phase 2 |
| NCT01034306 | Completed | Drug: CF101 Drug: Placebo control |
Rheumatoid Arthritis | University of Alberta | October 2010 | Phase 2 |
| NCT03168256 | Active Recruiting |
Drug: CF101 2mg Biological: Plerixafor |
Sickle Cell Disease | Sangamo Therapeutics | March 6, 2019 | Phase 1 Phase 2 |
| NCT02570542 | Active Recruiting |
Drug: Plerixafor Drug: CF101 3mg |
Can-Fite BioPharma | University of Chicago | September 15, 2018 | Phase 3 |
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