ABT-702 dihydrochloride
Based on 5 publication(s) in Google Scholar
ABT-702 dihydrochloride is a potent adenosine kinase (AK) inhibitor (IC50=1.7 nM).
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 1188890-28-9
- Formula: C22H21BrCl2N6O
- Molecular Weight:536.25
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) ABT-702 dihydrochloride
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Cell Proliferation/Viability Assay
Biological Activity
IC50: 1.7 nM (Adenosine kinase, AK)[1]
ABT-702 is an orally effective adenosine kinase inhibitor that has several orders of magnitude selectivity over other sites of adenosine (ADO) interaction (A1, A2A, A3 receptors, ADO transporter, and ADO deaminase). ABT-702 is equipotent (IC50=1.5±0.3 nM) in inhibiting native human AK (placenta), two human recombinant isoforms (AKlong and AKshort), and AK from monkey, dog, rat, and mouse brain. ABT-702 potently inhibits the activity of rat brain cytosolic AK in a concentration-dependent manner with an IC50 value of 1.7 nM. ABT-702 also potently inhibits AK activity in intact cultured IMR-32 human neuroblastoma cells (IC50=51 nM), indicating that ABT-702 can penetrate the cell membrane and potently inhibit AK at its intracellular site[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1188890-28-9
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Appearance Solid
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Molecular Weight 536.25
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Formula C22H21BrCl2N6O
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Color Yellow to orange
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SMILES
NC1=C(C(C2=CC=CC(Br)=C2)=CC(C3=CC=C(N4CCOCC4)N=C3)=N5)C5=NC=N1.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell
Adenosine kinase and ADAL coordinate detoxification of modified adenosines to safeguard metabolism. [Abstract]2025 Oct 30;188(22):6151-6169.e24. PMID: 40840445 -
Cell Stem Cell
ENPP1 blockade with a humanized monoclonal antibody enhances renal repair after acute kidney injury. [Abstract]2026 Jun 16:S1934-5909(26)00203-1. PMID: 42302792 -
Cell Death Discov
5-Iodotubercidin sensitizes cells to RIPK1-dependent necroptosis by interfering with NFκB signaling. [Abstract]2023 Jul 26;9(1):262. PMID: 37495567
ABT-702 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2023 Jul 26;9(1):262. [Abstract]
MK2-deficient MEFs transduced with MK2 expression or control vector were treated with indicated small molecules (5 µM ABT-702 dihydrochloride, 100 nM gemcitabine, 5 µM etoposid, 5 µM doxorubicin and 5 µM staurosporine) in the presence or absence of TNF for 6 h and cell viability was assessed.
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Neurochem Res
2024 Nov 16;50(1):13. PMID: 39549173
ABT-702 dihydrochloride purchased from MedChemExpress. Usage Cited in: Neurochem Res. 2024 Nov 16;50(1):13. [Abstract]
Effects of inhibitors of adenosine metabolism on the utilization of adenosine for ATP restoration in glucose-fed astrocytes. Astrocyte cultures had been preincubated for 60 min in glucose-free IB with 1 µM of BAM15 to lower the cellular ATP content before the cells were incubated in glucose (5 mM)-containing IB without or with 30 µM adenosine in the absence or the presence of the adenosine kinase inhibitor ABT-702 dihydrochloride (ABT; 10 µM), the adenosine deaminase inhibitor DCF (1 µM) and/or the purine nucleoside phosphorylase inhibitor forodesine (Foro; 10 µM). After 60 min, the cellular ATP content was determined.
ABT-702 dihydrochloride purchased from MedChemExpress. Usage Cited in: Neurochem Res. 2024 Nov 16;50(1):13. [Abstract]
Effects of inhibitors of adenosine metabolism on the utilization of adenosine for ATP restoration in glucose-fed astrocytes. Astrocyte cultures had been preincubated for 60 min in glucose-free IB with 1 µM of BAM15 to lower the cellular ATP content before the cells were incubated in glucose (5 mM)-containing IB without or with 30 µM adenosine in the absence or the presence of the adenosine kinase inhibitor ABT-702 dihydrochloride (ABT; 10 µM), the adenosine deaminase inhibitor DCF (1 µM) and/or the purine nucleoside phosphorylase inhibitor forodesine (Foro; 10 µM). After 60 min, the extracellular LDH activity was determined.
ABT-702 dihydrochloride purchased from MedChemExpress. Usage Cited in: Neurochem Res. 2024 Nov 16;50(1):13. [Abstract]
Prevention of the exclusive utilization of adenosine for ATP restoration by inhibitors of adenosine metabolism. Astrocyte cultures had been preincubated for 60 min in glucose-free IB with 1 µM of BAM15 to lower the cellular ATP content before the cells were incubated in glucose-free IB with 100 µM adenosine in the absence or the presence of the adenosine kinase inhibitor ABT-702 dihydrochloride (ABT; 10 µM), the adenosine deaminase inhibitor DCF (1 µM) and/or the purine nucleoside phosphorylase inhibitor forodesine (Foro; 10 µM). After 60 min, the cellular ATP content and the extracellular LDH activity were determined.
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ESC Heart Fail
Inhibition of adenosine kinase alleviates hypertrophic cardiomyopathy by ameliorating coronary microvascular dysfunction. [Abstract]2026 May 5;13(3):xvag118. PMID: 42015547
Solvent & Solubility
DMSO : ≥ 33.33 mg/mL (62.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Rats[2]
Rats are fasted for 16 hours prior to use. At the beginning of the experiment, each rat is weighed, and then anesthetized using 5% isoflurane for induction and 2.5% for maintenance. A blood sample from tail vein is collected for a fasting blood glucose determination using a standard glucometer. Rats are then given an intraperitoneal (i.p.) injection of DPCPX (3 mg/kg, n=4), ABT-702 (3 mg/kg, n=4), or an equivalent volume of vehicle (15% dimethyl sulfoxide, 15% cremophor EL, 70% saline, n=4) to manipulate the effect of endogenous adenosine on neuronal activities. Ten minutes after i.p. injection, rats are administered FDG (15.4±0.7 MBq) in 0.3-0.5 mL saline by intravenous (i.v.) tail vein injection. Rats are allowed to recover from anesthesia after the FDG injection but are reanesthetized for 15-minute-static PET scan with the head in the center of the field of view. All images are reconstructed[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8648 mL | 9.3240 mL | 18.6480 mL | 46.6200 mL |
| 5 mM | 0.3730 mL | 1.8648 mL | 3.7296 mL | 9.3240 mL | |
| 10 mM | 0.1865 mL | 0.9324 mL | 1.8648 mL | 4.6620 mL | |
| 15 mM | 0.1243 mL | 0.6216 mL | 1.2432 mL | 3.1080 mL | |
| 20 mM | 0.0932 mL | 0.4662 mL | 0.9324 mL | 2.3310 mL | |
| 25 mM | 0.0746 mL | 0.3730 mL | 0.7459 mL | 1.8648 mL | |
| 30 mM | 0.0622 mL | 0.3108 mL | 0.6216 mL | 1.5540 mL | |
| 40 mM | 0.0466 mL | 0.2331 mL | 0.4662 mL | 1.1655 mL | |
| 50 mM | 0.0373 mL | 0.1865 mL | 0.3730 mL | 0.9324 mL | |
| 60 mM | 0.0311 mL | 0.1554 mL | 0.3108 mL | 0.7770 mL |
ABT-702 dihydrochloride Related Classifications
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