ABT-702 dihydrochloride

Name: ABT-702 dihydrochloride
Brand: MedChemExpress
SKU: HY-103161
Rating: 5.0 (3 reviews)

Cat. No.: HY-103161 Purity: 99.45%: Data Sheet
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ABT-702 dihydrochloride is a potent adenosine kinase (AK) inhibitor (IC₅₀=1.7 nM).

For research use only. We do not sell to patients.

CAS No. : 1188890-28-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of ABT-702 dihydrochloride:

ABT-702 In-stock
ABT-702 hydrochloride In-stock
ABT-702 dihydrochloride (Standard) Get quote

3 Publications Citing Use of MCE ABT-702 dihydrochloride

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

: 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.

: 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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Description

ABT-702 dihydrochloride is a potent adenosine kinase (AK) inhibitor (IC₅₀=1.7 nM).

IC₅₀ & Target

IC50: 1.7 nM (Adenosine kinase, AK)^[1]

In Vitro

ABT-702 is an orally effective adenosine kinase inhibitor that has several orders of magnitude selectivity over other sites of adenosine (ADO) interaction (A₁, A_2A, 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 (AK_long and AK_short), 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.

In Vivo

ABT-702 significantly reduces acute thermal nociception in a dose-dependent manner after both intraperitoneal (ED₅₀=8 μmol/kg i.p.) and oral (ED₅₀=65 μmol/kg p.o.) administration in the mouse hot-plate test. Consistent with its antinociceptive effects in the hot-plate assay, ABT-702 also produces dose-dependent antinociceptive effects (ED₅₀=2 μmol/kg i.p.) in the abdominal constriction assay. ABT-702 exhibits full efficacy in this model of persistent chemical pain^[1]. Rats are given an intraperitoneal injection of the adenosine A₁ receptor antagonist DPCPX (3 mg/kg), ABT-702 (3 mg/kg), or vehicle 10 minutes prior to an intravenous injection of 2-¹⁸F-fluorodeoxy-D-glucose (FDG) (FDG, 15.4±0.7 MBq per rat). Rats are then subjected to a 15 minute static positron emission tomography (PET) scan. Reconstructed images are normalized to FDG PET template for rats and standard uptake values (SUVs) are calculated. To examine the regional effect of active treatment compared to vehicle, statistical parametric mapping analysis is performed. Whole-brain FDG uptake is not affected by drug treatment. Significant regional hypometabolism is detected, particularly in cerebellum, of DPCPX and ABT-702 treated rats, relative to vehicle-treated rats. Thus, endogenous adenosine can affect FDG accumulation although this effect is modest in quiescent rats. Body weight (316.8±28.4 g; mean±SD) and blood glucose (5.5±1.7 mM) are not significantly different among three groups. Whole-brain PET SUV values are 1.6±0.4, 1.6±0.6, and 1.8±0.6 for vehicle, ABT-702, and DPCPX-treated rats, respectively (F(2,9)=0.298, P=0.75). statistical parametric mapping (SPM) analysis reveals significant regional hypometabolism in the cerebellum, mesencephalic region, and medulla in the ABT-702-treated rats compared to the vehicle-treated rats^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

536.25

Formula

C₂₂H₂₁BrCl₂N₆O

CAS No.

1188890-28-9

Appearance

Solid

Color

Yellow to orange

SMILES

NC1=C(C(C2=CC=CC(Br)=C2)=CC(C3=CC=C(N4CCOCC4)N=C3)=N5)C5=NC=N1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.45%

Select Batch:

Data Sheet (284 KB) SDS (394 KB)

COA (255 KB) HNMR (275 KB) LCMS (94 KB)

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]

Animal Administration
^[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

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