FmocEVCit-PAB
This product is a high-purity cleavable linker composed of glutamic acid–valine–citrulline (EVCit) and a para-aminobenzyl (PAB) self-immolative spacer, featuring an Fmoc-protected amine for orthogonal conjugation, widely used in antibody–drug conjugates (ADCs) and other targeted therapeutics, specifically where the EVCit sequence is selectively cleaved by cathepsin B inside target cells, triggering the PAB spacer to release the attached payload. The design specifically ensures stability in circulation and efficient intracellular drug release.
Key Features and Benefits
-
Fmoc-Protected Amine: Enables orthogonal, controlled deprotection for sequential conjugation.
-
EVCit Cleavable Linker: Stable in systemic circulation and selectively cleaved by cathepsin B in lysosomes.
-
PAB Self-Immolative Spacer: Facilitates rapid and complete release of payload after enzymatic cleavage.
-
Proven in ADC Development: Widely used for targeted delivery of cytotoxic agents.
-
High Purity: Supplied at >95% purity for consistent, reproducible performance.
Applications
-
Antibody–Drug Conjugates (ADCs): Link antibodies to cytotoxic drugs for targeted cancer therapy.
-
Peptide–Drug Conjugates: Enable site-specific, enzyme-triggered drug release.
-
Nanoparticle Functionalization: Introduce cleavable linkers for controlled payload delivery.
-
Prodrug Development: Build activation linkers responsive to disease-specific enzymes.
-
Diagnostic Imaging Agents: Create targeted 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 reactivity.
FmocEVCit-PAB combines a cathepsin B–cleavable EVCit linker with a PAB self-immolative spacer for efficient intracellular payload release, making it especially ideal for ADCs and other targeted delivery systems requiring stability in circulation and controlled activation inside cells.
AxisPharm offers 5000+ PEG Linkers with high purity. Different kinds of PEG Reagents may be available by custom synthesis.
