AZA197

SKU: orb1702521

Description

AZA197 is a selective small molecule inhibitor of Cdc42. It has demonstrated efficacy in preclinical research, suppressing primary colon tumor growth in mouse xenograft models and extending survival through the downregulation of PAK1 activity. This compound is a useful research tool for studying Rho GTPase signaling in cancer biology, both in vitro and in vivo.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1249398-09-1
• MW: 408.58
• Purity: >99.99% (May vary between batches)
• Formula: C₂₄H₃₆N₆
• SMILES: C(CNC1=NC(NC(CCCN(CC)CC)C)=NC(C)=C1)C=2C=3C(NC2)=CC=CC3
• Target: Apoptosis,PAK,CDK,Ras,ERK
• Solubility: DMSO:Slightly soluble

Bioactivity

• In Vivo:
  Systemic AZA197(i.p. injections with 100 μg) treatment reduced tumor growth in vivo and significantly increased mouse survival in SW620 tumor xenografts. Ki-67 staining and tissue TUNEL assays showed that both inhibition of cell proliferation and induction of apoptosis associated with reduced PAK/ERK activation contributed to the AZA197-induced therapeutic effects in vivo.
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• In Vitro:
  In SW620 and HT-29 human colon cancer cells, AZA197(1, 2, 5 and 10 μM; 24 h) demonstrated selectivity for Cdc42 without inhibition of Rac1 or RhoA GTPases from the same family. AZA197 suppressed colon cancer cell proliferation, cell migration and invasion and increased apoptosis associated with down-regulation of the PAK1 and ERK signaling pathways in vitro.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cdc42, AZA 197, AZA197, AZA-197

Compound Identifiers

PubChem CID

46938132