Fmoc-Val-Cit-PAB-PNP,863971-53

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Fmoc-Val-Cit-PAB-PNP

CAS No. : 863971-53-3

MCE 国际站：Fmoc-Val-Cit-PAB-PNP

产品活性：Fmoc-Val-Cit-PAB-PNP 是一种可降解 (cleavable) 的 ADC linker，可用于合成抗体偶联活性分子 (ADC)。 Fmoc-Val-Cit-PAB-PNP 的血浆稳定性优于不可降解连接剂。

研究领域：Antibody-drug Conjugate/ADC Related

作用靶点：ADC Linker

In Vitro: Fmoc-Val-Cit-PAB-PNP contains peptide sequence degradable by a lysosome enzyme.
Cathepsin B in the lysosome cleaves the peptide bond between Cit-PAB of dipeptide linkers containing Valine (Val)-citrulline (Cit) and p-aminobenzylalcohol (PAB). When PAB and a drug are binded covalently with carbamate bonds, the drug can be released by hydrolysis after cleavage of the peptide bond between Cit-PAB. Antibody-drug conjugates (ADCs) has been developed using this mechanism.

In Vivo: Fmoc-Val-Cit-PAB-PNP linker stabilization in the mouse is an essential prerequisite for designing successful efficacy and safety studies in rodents during preclinical stages of ADC programs.
Conjugation site plays an important role in determining VC-PABC linker stability in mouse plasma, and that the stability of the linker positively correlates with ADC cytotoxic potency both in vitro and in vivo.

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