Click Chemistry

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Boc-Val-Ala-OH is a cleavable ADC linker. The Val-Ala is effectively cleaved by lysosomal proteolytic enzymes while being highly stable in human plasma, making this a potentent stragy in ADC linker design. The Boc group can be deprotected under mild acidic conditions to form the free amine. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

Boc-Val-Ala-PAB is a cleavable ADC linker. The Val-Ala is effectively cleaved by lysosomal proteolytic enzymes while being highly stable in human plasma, making this a potentent stragy in ADC linker design. The t-butyl protected carboxyl group can be deprotected under acidic conditions. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

Boc-Val-Ala-PAB-PNP can be used to design cleavable ADC linkers. The Val-Ala, as shown in the ACD Zynlonta, is effectively cleaved by lysosomal proteolytic enzymes while being highly stable in human plasma. The t-butyl protected carboxyl group can be deprotected under acidic conditions. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

Alloc-Val-Ala-OH is a peptide linker with a terminal carboxylic acid group and an Alloc protecting group. The peptide chain can act as a cleavable linker in drug design, such as in antibody drug conjugates (ADC). The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond. The Alloc group is stable to treatment with piperidine and TFA, and can be removed in neutral conditions with catalytic amounts of Pd(PPh3)4 in the presence of PhSiH3. This allows the allyl system to work orthogonality with the most common protecting groups. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

Alloc-Val-Ala-PAB-OH is a peptide linker with a terminal Alloc protecting group. The peptide chain can act as a cleavable linker in drug design, such as in antibody drug conjugates (ADC). The Alloc group is stable to treatment with piperidine and TFA, and can be removed in neutral conditions with catalytic amounts of Pd(PPh3)4 in the presence of PhSiH3. This allows the allyl system to work orthogonality with the most common protecting groups. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

Alloc-Val-Ala-PAB-PNP is an ADC linker featuring an alloc-protected amine, a Val-Ala dipeptide, a PAB group, and a PNP carbonate. The PNP carbonate is highly activated towards attack from amines to form carbamate structures with a given payload, while the alloc protecting group can be removed by palladium catalysts to free the N-terminal amine to react with a wide variety of structures such as carboxylic acids. The Val-Ala dipeptide is cleaved by proteases to release a given drug payload via an elimination mechanism within the PAB group.