| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
AZA1 targets Rac1 and Cdc42, two closely related members of the Rho family of small GTPases. These proteins act as molecular switches, cycling between an active GTP-bound state and an inactive GDP-bound state to regulate a wide array of cellular processes, including cytoskeletal dynamics, cell migration, proliferation, and survival. By inhibiting Rac1 and Cdc42, AZA1 disrupts these processes.
|
|---|---|
| ln Vitro |
Human prostate cancer cell 22Rv1 growth is inhibited by AZA1 (Rac1/Cdc42-IN-1) (2-10 μM; 72 hours) [1]. EGF-stimulated 22Rv1 prostate cancer cells exhibit reduced phosphorylation of PAK1, AKT, and BAD upon treatment with AZA1 (2-10 μM; 24 hours) [1]. AZA1 (10 μM; 24 hours) suppresses Rac1- and Cdc42-dependent cell cycle events in 22Rv1 prostate cancer cells [1]. AZA1 inhibits the migration of prostate cancer cells PC-3, DU 145, and 22Rv1 that is dependent on Rac1 and Cdc42 [1]. AZA1 suppresses Rac1 and Cdc42 activity through PAK1/2 phosphorylation, consequently altering cell motility and actin rearrangement of prostate cancer cells [1].
In vitro, AZA1 inhibits the migration of prostate cancer cells PC-3, DU 145, and 22Rv1 that is dependent on Rac1 and Cdc42. It induces apoptosis of prostate cancer cells and inhibits cell proliferation, migration, and invasion. The compound's ability to inhibit both Rac1 and Cdc42 makes it a valuable tool for studying the roles of these GTPases in cancer. |
| ln Vivo |
AZA1 (Rac1/Cdc42-IN-1) (100 μg; i.p.; once daily for two weeks) efficiently suppresses the growth of human 22Rv1 xenografts and enhances mouse survival [1].
Specific in vivo data for AZA1 are not detailed in the available literature. However, as a potent inhibitor of Rac1 and Cdc42, it is expected to have antitumor activity in vivo. It could be used in preclinical studies to investigate the role of Rac1 and Cdc42 in cancer progression and metastasis. |
| Enzyme Assay |
The activity of AZA1 can be assessed using cell-free assays to measure its binding to Rac1 and Cdc42. For example, surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) can be used to determine the binding affinity. The compound's ability to inhibit the GTPase activity of Rac1 and Cdc42 can be measured using GTPase activity assays.
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: 22Rv1 Prostate Cancer Cell Tested Concentrations: 2, 5, 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited the proliferation of 22Rv1 Prostate Cancer Cell in unstimulated and EGF-stimulated cancer cells in a dose-dependent manner. Western Blot Analysis[1] Cell Types: 22Rv1 prostate cancer cells (EGF stimulated) Tested Concentrations: 2, 5, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished phosphorylation of PAK1, AKT and BAD in EGF-stimulated 22Rv1 prostate cancer cells. To evaluate the cellular effects of AZA1, prostate cancer cells such as PC-3, DU 145, and 22Rv1 are treated with the compound. Cell proliferation, migration, and invasion are assessed using standard assays such as MTT, wound healing, and transwell assays. Apoptosis is measured using Annexin V/PI staining or caspase activity assays. The effects on Rac1 and Cdc42 signaling pathways are assessed by Western blotting. |
| Animal Protocol |
Animal/Disease Models: 5weeks old athymic nu/nu (nude) mice (carrying 22Rv1 prostate cancer cell xenografts) [1]
Doses: 100 μg in 100 µl 30% DMSO one time/day for 2 weeks Experimental Results: AZA1 The inhibitory effect on tumor growth is significant. In vivo studies with AZA1 would typically involve administration to tumor-bearing mice in xenograft models. The compound's effects on tumor growth, metastasis, and survival would be assessed. Biomarkers of Rac1 and Cdc42 activity would be measured in tumor tissue. |
| ADME/Pharmacokinetics |
AZA1 has a molecular weight of 368.43. Its CAS number is 1071098-42-4. The compound is a cell-permeable indolylpyrimidinediamine small molecule. It is soluble in DMSO and other organic solvents. The purity is typically >99%.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for AZA1 are not detailed in the available literature. However, its potent inhibition of Rac1 and Cdc42, which are essential for normal cellular functions, may lead to dose-dependent toxicity. As with all research compounds, standard safety precautions should be taken during handling.
|
| References |
|
| Additional Infomation |
It has antitumor activity; the structure is shown in the first source.
AZA1 (Rac1/Cdc42-IN-1) is a potent dual inhibitor of Rac1 and Cdc42 used in cancer research. It induces apoptosis of prostate cancer cells and inhibits cell proliferation, migration, and invasion. It is a valuable tool for studying the roles of Rac1 and Cdc42 in cancer progression and for developing targeted cancer therapies. It is not a clinically approved drug. |
| Molecular Formula |
C22H20N6
|
|---|---|
| Molecular Weight |
368.434403419495
|
| Exact Mass |
368.174
|
| CAS # |
1071098-42-4
|
| PubChem CID |
25104141
|
| Appearance |
Light brown to brown solid powder
|
| LogP |
5
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
28
|
| Complexity |
529
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N1C(C)=CC2C=C(C=CC1=2)NC1C=CN=C(N=1)NC1C=CC2=C(C=1)C=C(C)N2
|
| InChi Key |
SYWHWWKOIJCMKF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H20N6/c1-13-9-15-11-17(3-5-19(15)24-13)26-21-7-8-23-22(28-21)27-18-4-6-20-16(12-18)10-14(2)25-20/h3-12,24-25H,1-2H3,(H2,23,26,27,28)
|
| Chemical Name |
2-N,4-N-bis(2-methyl-1H-indol-5-yl)pyrimidine-2,4-diamine
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~135.71 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2714 mL | 1.3571 mL | 2.7142 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
