2. PI3K/Akt/mTOR Stem Cell/Wnt
  3. GSK-3
  4. AZD1080

AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.

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

AZD1080 Chemical Structure

AZD1080 Chemical Structure

CAS No. : 612487-72-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 99 In-stock
10 mg USD 165 In-stock
50 mg USD 495 In-stock
100 mg USD 825 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

AZD1080 Related Antibodies

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GSK-3 GSK-3α GSK-3β

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.

IC50 & Target[1]

GSK-3α

8.2 (pKi)

GSK-3β

7.5 (pKi)

cdk5

6.4 (pKi)

cdk2

5.9 (pKi)

cdk1

5.7 (pKi)

In Vitro

AZD1080 shows selectivity against cdk2 (pKi=5.9; 1150 nM; 37-fold), cdk5 (pKi=6.4; 429 nM; 14-fold), cdk1 (pKi=5.7; 1980 nM; 64-fold) and Erk2 (pKi< 5; >10 μM; >323-fold). AZD1080 (at 10 μM) is also evaluated for pan-kinase selectivity and showed good overall selectivity versus 23 kinases, as well as against 65 different receptors, enzymes and ion channels in MDS Pharma screen (< 50% effect at 10 μM AZD1080). Concentration-dependent inhibition of tau phosphorylation is observed for AZD1080 (IC50=324 nM) and the non-selective reference GSK3 inhibitor LiCl (IC50=1.5 mM) indicating that AZD1080 is several orders of magnitude more potent than LiCl[1].

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

AZD1080 Related Antibodies
In Vivo

The pharmacokinetic analysis in blood after oral administration revealed that AZD1080 has a good oral bioavailability in rats (15-24%) with a half-life of 7.1 h, making AZD1080 attractive for further in vivo testing. The subchronic (3 days) oral treatment with AZD1080 at 4 or 15 μmol/kg significantly blocked the MK-801-induced memory deficit (AZD1080 vs. MK-801, p<0.05 at 4 μmol/kg and p<0.01 at 15 μmol/kg) in mice, raising the hypothesis that longer treatment may be required to prime the synapses to function effectively[1].

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

334.37

Formula

C19H18N4O2
CAS No.
Appearance

Solid

Color

Light yellow to orange

SMILES

OC(N1)=C(C2=CC=C(CN3CCOCC3)C=N2)C4=C1C=CC(C#N)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 21.35 mg/mL (63.85 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9907 mL 14.9535 mL 29.9070 mL
5 mM 0.5981 mL 2.9907 mL 5.9814 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. 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (7.48 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 (7.48 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
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: 99.46%

SDS (393 KB)

COA (257 KB) LCMS (110 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

The GSK3β, Cdk2, and Cdk5 Ki’s are determined using scintillation proximity assays and kinetic analyses. The GSK3α assay is performed for the GSK3β assay. The KM value of ATP used to calculate the Ki value for GSKα is 10 μM. Inhibition of Cdk1 is performed. The KM value of ATP used to calculate the Ki value is 51 μM. Erk2 activity is determined using an Ser/Thr kinase SPA kit, p42 MAPK kinase (20 U/well), and biotinylated MBP. The KM value of ATP used to calculate the Ki value is 71 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
A total of 161 male C57BL/6 mice, 8-12 weeks of age, are used. The animals are kept in conventional housing (3-5 mice per cage) and fed standard rodent chew and tap water ad libitum. Typically 9-12 mice are included in each experimental group and 2-4 mice in the satellite groups (for determination of compound exposure in plasma and brain, see below). AZD1080 (4.0 or 15 μmol/kg) or vehicle (water with 0.5% ascorbic acid, 0.01% EDTA, pH 2.0) is administered by oral gavage (10 mL/kg) acutely or subchronically (twice daily) for 3 days. The training trial is performed at 1.5, 3, or 5 h after final administration with AZD1080. To disrupt learning, the mice received subcutaneous administration of MK-801 (0.1 or 0.15 mg/kg; (+)-MK.801 hydrogen maleate) or vehicle (saline) 30 min before the training trial.
Rats[1]
A total of 71 adult male Sprague-Dawley rats (250-300 g) are used. The rats receive an acute dose of AZD1080 (1, 3 or 10 μmol/kg) or vehicle (water with 0.5% ascorbic acid, 0.01% EDTA, pH 2.0) via oral gavage (dosing volume 5 mL/kg). At 1, 2, 3, 6, or 24 h after administration the rats are anesthetized and blood, from abdominal aorta, is sampled in heparin micro tainer tubes. Peripheral blood mononuclear cells (PBMC) are isolated from the blood samples. Separate blood samples are obtained for plasma processing and subsequent bioanalysis.

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

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. 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 2.9907 mL 14.9535 mL 29.9070 mL 74.7675 mL
5 mM 0.5981 mL 2.9907 mL 5.9814 mL 14.9535 mL
10 mM 0.2991 mL 1.4953 mL 2.9907 mL 7.4767 mL
15 mM 0.1994 mL 0.9969 mL 1.9938 mL 4.9845 mL
20 mM 0.1495 mL 0.7477 mL 1.4953 mL 3.7384 mL
25 mM 0.1196 mL 0.5981 mL 1.1963 mL 2.9907 mL
30 mM 0.0997 mL 0.4984 mL 0.9969 mL 2.4922 mL
40 mM 0.0748 mL 0.3738 mL 0.7477 mL 1.8692 mL
50 mM 0.0598 mL 0.2991 mL 0.5981 mL 1.4953 mL
60 mM 0.0498 mL 0.2492 mL 0.4984 mL 1.2461 mL
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AZD1080 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD1080612487-72-6AZD 1080AZD-1080GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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