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Synthesis of unnatural amino acids and other blocks
Fmoc-Val-Cit-PABC-PNP
Name
Fmoc-Val-Cit-PABC-PNP
Molecular structural formula
Purity
≥95%
CAS Number
863971-53-3
MW
766.80
Target
ADC Linker
InChIKey
USMYACISHVPTHK-PXLJZGITSA-N
Solubility in DMSO
≥ 40 mg/mL
References
[1]. Dubowchik GM, et al. Cathepsin B-labile dipeptide linkers for lysosomal release of doxorubicin from internalizing immunoconjugates: model studies of enzymatic drug release and antigen-specific in vitro anticancer activity. Bioconjug Chem. 2002 Jul-Aug;13(4):855-69. [2]. Yoneda Y, et al. A cell-penetrating peptidic GRP78 ligand for tumor cell-specific prodrug therapy. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1632-6. [3]. Dorywalska M, et al. Effect of attachment site on stability of cleavable antibody drug conjugates. Bioconjug Chem. 2015 Apr 15;26(4):650-9.
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Fmoc-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Val-Cit-PAB-PNP has superior plasma stability comparable to that of non-cleavable linkers.