CAS · 644981-35-1
Product Overview
Val-Cit-PAB-MMAE is a high-purity amino-acids supplied for industrial and specialty chemical applications. Contact our team for specifications, packaging options and lead times.
Product Specifications
| Appearance: | White to off-white solid |
|---|---|
| Identification: | HPLC: the retention time of major peak confirms |
| Purity (by HPLC): | 98% min |
| Total impurity: | 2% max |
Applications
Val-Cit-PAB-MMAE is primarily used in the development and production of antibody-drug conjugates, a class of biopharmaceuticals that combine the specificity of monoclonal antibodies with the high potency of cytotoxic drugs. The Val-Cit dipeptide linker is cleavable by cathepsin B, an enzyme overexpressed in tumor cells, ensuring that the MMAE payload is released selectively inside malignant tissues. The PAB spacer promotes efficient self-immolation after enzymatic cleavage, releasing free MMAE in its active form. MMAE acts as a microtubule inhibitor, preventing cell division and inducing apoptosis in cancer cells. This conjugate framework has been applied in several FDA-approved ADCs and continues to serve as a benchmark in new therapeutic designs targeting solid and hematologic malignancies.
Benefits
The benefits of Val-Cit-PAB-MMAE stem from its precision, potency, and modularity. The enzymatically cleavable linker provides targeted drug release, thereby reducing off-target cytotoxicity and enhancing the therapeutic index of ADCs. The stability of the linker under physiological conditions ensures minimal premature drug release during systemic circulation, while the efficient intracellular cleavage mechanism guarantees high activity within tumor cells. MMAE itself is an extremely potent cytotoxin, active at sub-nanomolar concentrations, which allows for effective tumor killing even when only a small fraction of the conjugated drug reaches the target tissue. Furthermore, the modular structure of Val-Cit-PAB-MMAE allows it to be adapted to different antibodies and cancer targets, offering flexibility in ADC design.
Conclusion
In summary, Val-Cit-PAB-MMAE is a cornerstone linker-payload system in modern oncology therapeutics, enabling the targeted and controlled delivery of highly potent cytotoxic agents. Its intelligent combination of stability, selectivity, and bioactivity makes it ideal for use in antibody-drug conjugates that require precise intracellular activation. Through its integration into several successful anticancer drugs, Val-Cit-PAB-MMAE continues to play a vital role in advancing targeted chemotherapy and improving outcomes in cancer treatment.
Previous
Estradiol Undecylate丨CAS 3571-53-7
Next