1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. Nucleoside Antimetabolite/Analog Endogenous Metabolite
  3. 8-Azaguanine

8-Azaguanine is a purine analogue that shows antineoplastic activity. 8-Azaguanine functions as an antimetabolite and easily incorporates into ribonucleic acids, interfering with normal biosynthetic pathways, thus inhibiting cellular growth.

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

8-Azaguanine Chemical Structure

8-Azaguanine Chemical Structure

CAS No. : 134-58-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

8-Azaguanine is a purine analogue that shows antineoplastic activity. 8-Azaguanine functions as an antimetabolite and easily incorporates into ribonucleic acids, interfering with normal biosynthetic pathways, thus inhibiting cellular growth[1].

IC50 & Target

Human Endogenous Metabolite

 

In Vitro

8-Azaguanine induces a decrease in cell viability in a dose, time and cell type dependent manner with MOLT3 cells being the most sensitive to 8-Azaguanine citotoxic effects (24h IC50: 10 μM) when compared with CEM cells (24h IC50: 100 μM). MOLT3 cell treated with 8-Azaguanine shows an increase in CD26 expression (MIF) compared with that of CEM cell submitted to the same conditions (65.4 versus 18.7)[1].

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

Molecular Weight

152.11

Formula

C4H4N6O

CAS No.
Unlabeled CAS

Appearance

Solid

Color

White to yellow

SMILES

O=C1C(N=NN2)=C2N=C(N)N1

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (13.15 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C; 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 6.5742 mL 32.8709 mL 65.7419 mL
5 mM 1.3148 mL 6.5742 mL 13.1484 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: ≥ 0.24 mg/mL (1.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.24 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.4 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: ≥ 0.24 mg/mL (1.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.24 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.4 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: 99.84%

References
Cell Assay
[1]

Detection of apoptosis and necrosis is analyzed by Annexin V and propidium iodide staining. After incubation in the absence or in the presence of 8-Azaguanine, cells are washed (centrifuged at 300×g during 5 min) and incubated for 10 min at 4°C in 440 μL Annexin buffer, containing 5 μL Annexin V and 5 μL propidium iodide. Then cells are washed and re-suspended in phosphate buffered saline (PBS) until analysis[1].

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 6.5742 mL 32.8709 mL 65.7419 mL 164.3547 mL
5 mM 1.3148 mL 6.5742 mL 13.1484 mL 32.8709 mL
10 mM 0.6574 mL 3.2871 mL 6.5742 mL 16.4355 mL
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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.

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8-Azaguanine
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