Click Chemistry

H-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 potent strategy in ADC linker design.

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 potent strategy in ADC linker design. The Boc group can be deprotected under mild acidic conditions to form the free amine.

Boc-Val-Ala-PAB is a cleavable ADC linker. The Val-Ala peptide will specifically be cleaved by Cathepsin B. The Boc group can be removed under acidic conditions.

Boc-Val-Ala-PAB-PNB is a cleavable peptide ADC linker. The Val-Ala will specifically be cleaved by Cathepsin B. Since this enzyme is only present in the lysosome, the ADC payload will be released only in the cell. PNP can be substituted by amine-bearing molecules.

Alloc-Val-Ala-OH is a building block in the synthesis of Tesirine, a clinical antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. The Val-Ala will specifically be cleaved by Cathepsin B. The Alloc group is stable to treatment with piperidine and TFA, but can be easily removed under mild conditions by palladium catalyzed allyl transfer.

Alloc-Val-Ala-PAB is a peptide cleavable linker used in the synthesis of antibody-drug conjugates (ADCs). The Val-Ala will specifically be cleaved by Cathepsin B. The Alloc group is stable to treatment with piperidine and TFA, but can be easily removed under mild conditions by palladium catalyzed allyl transfer.

Alloc-Val-Ala-PAB is a peptide cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). The Val-Ala will specifically be cleaved by Cathepsin B. The Alloc group is stable to treatment with piperidine and TFA, but can be easily removed under mild conditions by palladium catalyzed allyl transfer. PNP is a good leaving group.

Fmoc-Val-Ala-PAB is a peptide cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). The Val-Ala will specifically be cleaved by Cathepsin B. The Fmoc group can be deprotected under basic conditions to obtain the free amine which can be used for further conjugations.

Fmoc-Val-Ala-PAB-PNP is a peptide cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). The Val-Ala will specifically be cleaved by Cathepsin B. The Fmoc group can be deprotected under basic conditions to obtain the free amine which can be used for further conjugations. PNP is a good leaving group.