Overview
Cilengitide is a synthetic cyclic pentapeptide developed as an integrin antagonist, specifically targeting αvβ3 and αvβ5 integrins involved in tumor angiogenesis. Originally researched by Merck KGaA, it reached Phase III clinical trials for glioblastoma before development was discontinued in 2014. Despite this, it remains a valuable tool compound for studying integrin-mediated pathways in oncology and vascular biology research. The peptide's structure (Cyclo-RGDfNMeV) mimics the Arg-Gly-Asp (RGD) motif found in extracellular matrix proteins, enabling competitive inhibition of integrin binding. Its mechanism involves disrupting endothelial cell survival signals and tumor vasculature formation, making it a prototype for antiangiogenic drug design.
Physical and Chemical Properties
As a cyclic peptide, cilengitide exhibits greater metabolic stability than linear RGD peptides, with a plasma half-life of 3-4 hours in preclinical models. Its molecular weight (588.66 g/mol) and polar surface area (234 Ų) influence pharmacokinetics, requiring intravenous administration in clinical studies. The compound shows high water solubility (>10 mg/mL), facilitating formulation for injectable use. Characterization typically involves reversed-phase HPLC (≥98% purity) and mass spectrometry. The powder is hygroscopic, requiring desiccated storage. Thermal analysis shows decomposition above 200°C rather than a distinct melting point, consistent with peptide behavior.
Main Applications
Cilengitide's primary application has been in oncology research, particularly for glioblastoma multiforme (GBM). Phase II trials demonstrated its ability to cross the blood-brain barrier, with some evidence of prolonged progression-free survival when combined with temozolomide. Current non-clinical uses include: 1. Angiogenesis inhibition studies in cancer cell lines and xenograft models 2. Mechanistic research on integrin signaling pathways 3. Development of RGD-based drug delivery systems (e.g., nanoparticle targeting) 4. Vascular biology investigations in retinal and inflammatory diseases
Safety and Storage
As a research chemical, cilengitide requires handling with nitrile gloves and eye protection. Although not classified as acutely toxic, chronic exposure risks remain uncharacterized. Lyophilized powder should be stored at -20°C under inert gas, with reconstituted solutions used within 24 hours at 4°C. For bulk procurement, cold chain transport (2-8°C) with desiccant is recommended. Stability studies indicate ≤3% degradation after 12 months when stored properly. Waste disposal should follow institutional guidelines for peptide compounds.
B2B Procurement Guide
When sourcing cilengitide for research or development purposes, prioritize suppliers providing: - Certificate of Analysis (CoA) with HPLC purity ≥95% - Batch-specific MS and NMR characterization data - Documentation of endotoxin levels (<0.1 EU/mg for in vivo use) - Stability data under proposed storage conditions Lead times for custom synthesis typically range 4-8 weeks. For GMP-grade material (if available), expect 3-6 month production cycles. Consider ordering small test quantities to verify solubility and bioactivity before large purchases.
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