1. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  2. Ras Apoptosis
  3. AZA1

AZA1  (Synonyms: Rac1/Cdc42-IN-1)

Cat. No.: HY-136383 Purity: 98.07%
COA Handling Instructions

AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.

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

AZA1 Chemical Structure

AZA1 Chemical Structure

CAS No. : 1071098-42-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 480 In-stock
50 mg USD 1350 In-stock
100 mg USD 1950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion[1][2].

In Vitro

AZA1 (Rac1/Cdc42-IN-1) (2-10 μM; 72 hours) blocks the proliferation of human prostate cancer cells 22Rv1 prostate cancer cells[1].
AZA1 (2-10 μM; 24 hours) reduces phosphorylation of PAK1, AKT and BAD in EGF-stimulated 22Rv1 prostate cancer cells[1].
AZA1 (10 μM; 24 hours) blocks Rac1 and Cdc42-dependent cell cycle events in 22Rv1 prostate cancer cells[1].
AZA1 blocks Rac1 and Cdc42-dependent migration of 22Rv1, DU 145 and PC-3 prostate cancer cells[1].
AZA1 affects cell motility and actin rearrangement in prostate cancer cells by suppressing Rac1 and Cdc42 activity via PAK1/2 phosphorylation[1].

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

Cell Proliferation Assay[1]

Cell Line: 22Rv1 prostate cancer cells
Concentration: 2, 5, 10 μM
Incubation Time: 72 hours
Result: Suppressed 22Rv1 prostate cancer cell proliferation in both unstimulated and EGF-stimulated cancer cells in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: 22Rv1 prostate cancer cells (EGF-stimulated)
Concentration: 2, 5, 10 μM
Incubation Time: 24 hours
Result: Reduced phosphorylation of PAK1, AKT and BAD in EGF-stimulated 22Rv1 prostate cancer cells.
In Vivo

AZA1 (Rac1/Cdc42-IN-1) (100 μg; i.p.; daily for 2 weeks) is potent in suppressing human 22Rv1 xenograft growth in mice and improving survival[1].

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

Animal Model: 5 week-old athymic nu/nu (nude) mice (bearing 22Rv1 prostate cancer cell xenografts)[1]
Dosage: 100 μg in 100 µl 30% DMSO
Administration: I.p.; daily for 2 weeks
Result: The suppressive effect of AZA1 on tumor growth was significant.
Molecular Weight

368.43

Formula

C22H20N6

CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

CC(N1)=CC2=C1C=CC(NC3=NC(NC4=CC5=C(NC(C)=C5)C=C4)=NC=C3)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (135.71 mM; Need ultrasonic; 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 2.7142 mL 13.5711 mL 27.1422 mL
5 mM 0.5428 mL 2.7142 mL 5.4284 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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 (6.79 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 (6.79 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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7142 mL 13.5711 mL 27.1422 mL 67.8555 mL
5 mM 0.5428 mL 2.7142 mL 5.4284 mL 13.5711 mL
10 mM 0.2714 mL 1.3571 mL 2.7142 mL 6.7855 mL
15 mM 0.1809 mL 0.9047 mL 1.8095 mL 4.5237 mL
20 mM 0.1357 mL 0.6786 mL 1.3571 mL 3.3928 mL
25 mM 0.1086 mL 0.5428 mL 1.0857 mL 2.7142 mL
30 mM 0.0905 mL 0.4524 mL 0.9047 mL 2.2618 mL
40 mM 0.0679 mL 0.3393 mL 0.6786 mL 1.6964 mL
50 mM 0.0543 mL 0.2714 mL 0.5428 mL 1.3571 mL
60 mM 0.0452 mL 0.2262 mL 0.4524 mL 1.1309 mL
80 mM 0.0339 mL 0.1696 mL 0.3393 mL 0.8482 mL
100 mM 0.0271 mL 0.1357 mL 0.2714 mL 0.6786 mL
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AZA1 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.

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