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Purity: ≥98%
ABT-702 dihydrochloride is a novel and potent non-nucleoside adenosine kinase (AK) inhibitor with IC50 of 1.7 nM. ABT 702 Dihydrochloride is selective over other sites of adenosine interaction like A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase. It displays oral activity in animal models of pain and inflammation.
| ln Vitro |
Across multiple orders of magnitude, ABT-702 is an oral active adenosine kinase inhibitor that has significant selectivity over other adenosine (ADO) interaction sites, including A1, A2A, A3 receptors, ADO transporters, and ADO deaminase. ABT-702 exhibits comparable inhibitory effects on native human placental AK, two human recombinant isoforms (AKlong and AKshort), as well as AK derived from the brains of monkeys, dogs, rats, and mice (IC50=1.5±0.3 nM). With an IC50 value of 1.7 nM, ABT-702 efficiently suppresses cytosolic AK activity in the rat brain in a concentration-dependent manner. ABT-702 can efficiently inhibit AK at its intracellular location by penetrating the cell membrane, as demonstrated by its ability to significantly reduce AK activity in intact cultured IMR-32 human neuroblastoma cells (IC50=51 nM) [1].
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| ln Vivo |
In the mouse hot plate test, ABT-702 was administered intraperitoneally (ED50=8 μmol/kg ip) and orally (ED50=65 μmol/kg po) and dramatically reduced acute thermal nociception in a dose-dependent manner. ABT-702 had a dose-dependent antinociceptive effect in the abdominal contraction test (ED50=2 μmol/kg ip), which was in line with the antinociceptive effect observed in the hot plate test. In this paradigm of persistent chemical pain, ABT-702 showed sufficient effectiveness [1]. ABT-702 (3 mg/kg), DPCPX (3 mg/kg), or a vehicle were delivered intraperitoneally into rats 10 minutes before to the intravenous injection of 2-18F-fluorodeoxy-D-glucose. FDG) (15.4±0.7 MBq/rat for FDG). After that, the rats had a static positron emission tomography (PET) scan for 15 minutes. The standardized uptake value (SUV) was computed after the reconstructed pictures were normalized to the rat FDG PET template. A statistical parametric mapping analysis was carried out in order to investigate the regional impacts of active therapy in comparison with the vehicle. Therapy did not alter the absorption of FDG over the whole brain. Rats treated with DPCPX and ABT-702 showed significant local hypometabolism compared to rats treated with vehicle, especially in the cerebellum. As a result, endogenous adenosine can influence the accumulation of FDG, albeit slightly in rats that are at rest. Between the three groups, there were no appreciable variations in blood glucose levels (5.5±1.7 mM) or body weight (316.8±28.4 g; mean±SD). Whole-brain PET SUV values for rats treated with vehicle, ABT-702, and DPCPX were 1.6±0.4, 1.6±0.6, and 1.8±0.6, respectively (F(2,9)=0.298, P=0.75). Comparing ABT-702-treated rats with vehicle-treated rats, statistical parametric map (SPM) analysis showed a substantial regional hypometabolism in the cerebellum, midbrain regions, and medulla oblongata [2].
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| References |
[1]. Jarvis MF, et al. ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse. J Pharmacol Exp Ther. 2000 Dec;295(3):1156-64.
[2]. Parkinson FE, et al. The Effect of Endogenous Adenosine on Neuronal Activity in Rats: An FDG PET Study. J Neuroimaging. 2016 Jul;26(4):403-5 |
| Molecular Formula |
C22H21BRCL2N6O
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|---|---|
| Molecular Weight |
536.251741170883
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| CAS # |
1188890-28-9
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| Related CAS # |
214697-26-4;1188890-28-9 (HCl);
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| SMILES |
BrC1=CC(C2=CC(C3=CC=C(N4CCOCC4)N=C3)=NC5=NC=NC(N)=C52)=CC=C1.[H]Cl.[H]Cl
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| InChi Key |
OOXNYFKPOPJIOT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H19BrN6O.2ClH/c23-16-3-1-2-14(10-16)17-11-18(28-22-20(17)21(24)26-13-27-22)15-4-5-19(25-12-15)29-6-8-30-9-7-29;;/h1-5,10-13H,6-9H2,(H2,24,26,27,28);2*1H
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| Chemical Name |
5-(3-Bromophenyl)-7-[6-(4-morpholinyl)-3-pyrido[2,3-d]byrimidin-4-amine dihydrochloride
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| Synonyms |
ABT 702 Dihydrochloride; ABT 702 Dihydrochloride; ABT-702; ABT702;
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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 : ≥ 33.33 mg/mL (~62.15 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.66 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 (4.66 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 (4.66 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 | 1.8648 mL | 9.3240 mL | 18.6480 mL | |
| 5 mM | 0.3730 mL | 1.8648 mL | 3.7296 mL | |
| 10 mM | 0.1865 mL | 0.9324 mL | 1.8648 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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