Fmoc-Val-Cit-OH
Fmoc-Val-Cit-OH is a high-purity dipeptide linker composed of valine and citrulline, featuring an Fmoc-protected N-terminus for orthogonal conjugation and a free carboxylic acid for further functionalization. This cleavable linker is widely used in antibody–drug conjugates (ADCs) due to its stability in circulation and efficient cleavage by cathepsin B inside target cells. Its balanced hydrophilicity and stability make it ideal for controlled drug release, precision linker design, and advanced bioconjugation strategies.
Key Features and Benefits
-
Fmoc-Protected Amine: Enables orthogonal, controlled deprotection for stepwise conjugation.
-
Val-Cit Cleavable Linker: Stable in systemic circulation and selectively cleaved by cathepsin B in target cells.
-
Free Carboxylic Acid: Allows further coupling to amines, alcohols, or other reactive groups.
-
Proven in ADC Development: Commonly used for targeted drug delivery with predictable release profiles.
-
High Purity: Supplied at >95% purity for consistent, reproducible results.
Applications
-
Antibody–Drug Conjugates (ADCs): Incorporate as a cleavable linker for targeted drug release.
-
Peptide–Drug Conjugates: Enable site-specific drug release via enzymatic cleavage.
-
Nanoparticle Functionalization: Introduce cleavable linkers for controlled payload delivery.
-
Prodrug Development: Build linkers that activate in disease-specific environments.
-
Diagnostic Agents: Create targeted imaging probes with controlled release mechanisms.
Storage and Handling
-
Storage: Store at –20 °C, dry, and protected from light.
-
Handling: Use anhydrous solvents; avoid prolonged exposure to moisture to maintain integrity.
Fmoc-Val-Cit-OH offers a proven cleavable linker system with orthogonal reactivity, high stability, and selective enzymatic cleavage, making it an especially versatile tool in ADC development, targeted delivery systems, and controlled-release bioconjugates.
AxisPharm offers 5000+ PEG Linkers with high purity. Different kinds of PEG Reagents may be available by custom synthesis.
