GGFG-amino-CH₂O-acetyl Exatecan (CAS 1599440-12-6), also known as Exatecan-2-(aminomethoxy)acetamide-Gly-Phe-Gly-Gly, is a hexacyclic derivative of camptothecin. It acts as a potent DNA topoisomerase I inhibitor and is widely used in antibody-drug conjugate (ADC) research.
Key Features:
- Molecular Formula: C₄₂H₄₅FN₈O₁₀
- Molecular Weight: 840.85 g/mol
- Mechanism: Inhibits DNA topoisomerase I, causing DNA damage and cancer cell death.
- Peptide Linker: Includes a cleavable Gly-Phe-Gly-Gly (GGFG) linker for controlled drug release.
Applications:
- Antibody-Drug Conjugates (ADCs):
- Serves as a cytotoxic payload for targeted cancer therapy.
- The GGFG linker enables drug release within lysosomes of target cells.
- Cancer Research:
- Evaluates the efficacy of topoisomerase I inhibitors in various cancer models.
- Studies drug resistance mechanisms and therapeutic outcomes.
- Drug Development:
- Supports the design of chemotherapeutic agents.
- Assesses combination therapies for enhanced anticancer effects.
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