AZA197
Based on 1 Customer Validation
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.71%
- CAS 番号: 1249398-09-1
- 分子式: C24H36N6
- 分子量:408.58
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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.
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Cell Line:SW620 cells
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Concentration:2, 5 and 10 μM
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Incubation Time:24 h
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Result:Increased the number of apoptotic cells (sub G0/G1 peak, M1) in a dose-dependent manner.
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Cell Line:SW620 cells
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Concentration:2, 5 and 10 μM
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Incubation Time:24 h
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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.
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Cell Line:SW620 and HT-29 cells
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Concentration:1, 2 and 5 μM
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Incubation Time:24 h
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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.
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Cell Line:SW620 and HT-29 cells
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Concentration:1, 2 and 5 μM
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Incubation Time:24 h
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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%.
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Cell Line:SW620 and HT-29 cells
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Concentration:2, 5 and 10 μM
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Incubation Time:24 h
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Result:Caused the cells to become round, the filamentous pseudopodia to completely disappear, and the actin cytoskeleton to undergo reorganization.
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Cell Line:SW620 and HT-29 cells
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Concentration:2, 5 and 10 μM
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Incubation Time:24 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SW620 xenograft model established in Balb/c nude, female mice[1]
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Dosage:100 μg, dissolved in 100 μL of 30% DMSO
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Administration:Intraperitoneal injection (i.p.), once daily for 2 weeks or 100 days
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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.
化学情報
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CAS 番号 1249398-09-1
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性状 Solid
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分子量 408.58
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分子式 C24H36N6
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Color Off-white to light yellow
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SMILES
CC1=NC(NC(CCCN(CC)CC)C)=NC(NCCC2=CNC3=C2C=CC=C3)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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取扱説明書 (2659 KB)
参考文献
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 |