CAS · 159858-22-7
Product Overview
FMOC-VAL-CIT-PAB is a high-purity nucleosides-nucleotides supplied for industrial and specialty chemical applications. Contact our team for specifications, packaging options and lead times.
Product Specifications
| Appearance | White to faint yellow powder, free from visible foreign matter |
|---|---|
| Appearance of 0.2M Solution | Report color and clarity of a 0.2M amidate solution in acetonitrile |
| Molecular Weight by MS | 721 to 723 Da (M+) or 743 to 745 Da (M+ Na+) |
| 1H NMR | To conform structure |
| 31P NMR | 98% min |
| RP-HPLC | 98% min |
| GC Standard Solvent Panel | 5% max |
| Moisture | 1% max |
Applications
FMOC-VAL-CIT-PAB (CAS 159858-22-7) is a specialized peptide-based linker widely used in the design and synthesis of antibody–drug conjugates (ADCs) and other targeted drug delivery systems. It consists of a dipeptide sequence (valine–citrulline) and a para-aminobenzyl (PAB) self-immolative spacer, capped with a fluorenylmethyloxycarbonyl (FMOC) protecting group. Its primary application lies in controlled drug release, where the valine–citrulline sequence is cleaved by cathepsin enzymes in tumor cells, triggering the PAB spacer to self-eliminate and release the active drug payload. In addition to oncology-focused ADCs, it is employed in medicinal chemistry for the preparation of enzyme-sensitive prodrugs and in the development of novel bioconjugates for targeted therapeutics. Researchers also use this linker in proof-of-concept studies for precision drug delivery systems.
Benefits
The benefits of FMOC-VAL-CIT-PAB are centered on its efficiency, selectivity, and reliability as a cleavable linker. Its enzyme-specific cleavage ensures that drug payloads are released preferentially within target cells, improving therapeutic index and minimizing systemic toxicity. The self-immolative PAB spacer allows rapid and complete drug release after cleavage, preventing partial activation or accumulation of inactive intermediates. The FMOC group provides convenient protection during synthesis, facilitating straightforward incorporation into complex drug conjugates. This combination of controlled release, chemical stability, and synthetic accessibility makes it a gold-standard linker system in ADC technology and a valuable tool for advancing targeted therapies.
Conclusion
In summary, FMOC-VAL-CIT-PAB is a highly functional linker that plays a crucial role in modern targeted drug delivery, especially in antibody–drug conjugates. Its applications include oncology therapeutics, prodrug development, and advanced bioconjugation strategies, while its benefits lie in enzyme-specific release, stability, and synthetic practicality. As precision medicine continues to expand, this compound remains a cornerstone in the design of safer and more effective therapeutic systems.
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