2. GPCR/G Protein Cell Cycle/DNA Damage Apoptosis Stem Cell/Wnt MAPK/ERK Pathway Cytoskeleton
  3. PAK Apoptosis Ras ERK
  4. AZA197

AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts. AZA197 can be used for the study of colon cancer.

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AZA197

AZA197 Chemical Structure

CAS No. : 1249398-09-1

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Based on 1 publication(s) in Google Scholar

AZA197 Related Antibodies

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Description

AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts. AZA197 can be used for the study of colon cancer[1].

In Vitro

AZA197 (1-100 μM, 24 h) promotes LDH release and inhibits Cdc42 activation in SW620 colon cancer cells[1].
AZA197 (1-10 μM, 24-72 h) significantly inhibits the proliferation of SW620 and HT-29 cells in a dose- and time-dependent manner[1].
AZA197 (2-10 μM, 24 h) induces SW620 cell apoptosis and causes cell cycle arrest[1].
AZA197 (1-5 μM, 24 h) dose-dependently significantly inhibits the migration and invasion abilities of SW620 and HT-29 cells[1].
AZA197 (2-10 μM, 24 h) inhibits Cdc42, thereby disrupting its crucial functions in regulating cell morphology and movement in SW620 and HT-29 cells[1].
AZA197 (2-10 μM, 24 h) inhibits Cdc42, thereby suppressing the downstream PAK-ERK signaling axis in SW620 and HT-29 cells[1].

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

AZA197 Related Antibodies

Apoptosis Analysis[1]

Cell Line: SW620 cells
Concentration: 2, 5 and 10 μM
Incubation Time: 24 h
Result: Increased the number of apoptotic cells (sub G0/G1 peak, M1) in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: SW620 cells
Concentration: 2, 5 and 10 μM
Incubation Time: 24 h
Result: led to an increase in the proportion of Sub G0/G1 phase and a decrease in the proportions of cells in S phase and G2/M phase.

Cell Migration Assay [1]

Cell Line: SW620 and HT-29 cells
Concentration: 1, 2 and 5 μM
Incubation Time: 24 h
Result: Significantly reduced cancer cell migration by 47.4% and 43.5%, respectively at 2 and 5 μM in SW620 cells.
Significantly reduced cancer cell migration in a dose-dependent manner up to 77.1% in HT-29 colon cancer cells.

Cell Migration Assay [1]

Cell Line: SW620 and HT-29 cells
Concentration: 1, 2 and 5 μM
Incubation Time: 24 h
Result: Significantly decreased SW620 invasion by 61.3%, 71.0% and 83.9%.
Significantly decreased invasion of HT-29 cells at corresponding concentrations up to 84.6%.

Immunofluorescence[1]

Cell Line: SW620 and HT-29 cells
Concentration: 2, 5 and 10 μM
Incubation Time: 24 h
Result: Caused the cells to become round, the filamentous pseudopodia to completely disappear, and the actin cytoskeleton to undergo reorganization.

Western Blot Analysis[1]

Cell Line: SW620 and HT-29 cells
Concentration: 2, 5 and 10 μM
Incubation Time: 24 h
Result: Significantly and dose-dependently reduced the levels of phosphorylated PAK (p-PAK) and phosphorylated ERK (p-ERK).
Did not affect the protein expression levels of Cdc42, total PAK, and total ERK.
Significantly reduced the protein expression level of Cyclin D1.
In Vivo

AZA197 (100 μg, dissolved in 100 μL of 30% DMSO (HY-Y0320C), i.p., once daily for 2 weeks or 100 days) significantly inhibits tumor growth and significantly prolonged the survival time of tumor-bearing mice in a colon cancer xenograft model[1].

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

Animal Model: SW620 xenograft model established in Balb/c nude, female mice[1]
Dosage: 100 μg, dissolved in 100 μL of 30% DMSO
Administration: Intraperitoneal injection (i.p.), once daily for 2 weeks or 100 days
Result: Significantly inhibited tumor growth.
Significantly prolonged the survival period of tumor-bearing mice.
Inhibited the proliferation of tumor cells and induced cell apoptosis within the body.
Reduced the levels of p-PAK and p-ERK in the tumor tissue.
Molecular Weight

408.58

Formula

C24H36N6
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=NC(NC(CCCN(CC)CC)C)=NC(NCCC2=CNC3=C2C=CC=C3)=C1
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 : 4.5 mg/mL (11.01 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 2.4475 mL 12.2375 mL 24.4750 mL
5 mM 0.4895 mL 2.4475 mL 4.8950 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.

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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, 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 2.4475 mL 12.2375 mL 24.4750 mL 61.1875 mL
5 mM 0.4895 mL 2.4475 mL 4.8950 mL 12.2375 mL
10 mM 0.2448 mL 1.2238 mL 2.4475 mL 6.1188 mL
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AZA197 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:

AZA1971249398-09-1AZA 197AZA-197PAKApoptosisRasERKp21 activated kinasesExtracellular signal regulated kinasesCdc42 InhibitorXenograft modelColon cancerInhibitorinhibitorinhibit

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