Uses
Mc-Val-Ala-PAB-PNP is a cleavable ADC linker for the synthesis of antibody-drug conjugates (ADCs). Cryptophycin-55 (CR55) can be conjugated to the model antibody trastuzumab (an anti-HER2 antibody drug approved by the FDA for the treatment of breast cancer) through the linker of Mc-NHS and Mc-Val-Cit-PAB-PNP to prepare trastuzumab-CR55 conjugates. These conjugates exhibit potent cytotoxicity in HER2-positive tumor cell lines, with IC50 values at low nanomolar levels (0.58-1.19 nM)
[1].
Biological Activity
MC-Val-Ala-PAB-PNP is a cleavable ADC linker that can be used to synthesize antibody-drug conjugates (ADCs).
in vitro
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.
References
[1] QINHUAI LAI . Cryptophycin-55/52 based antibody-drug conjugates: Synthesis, efficacy, and mode of action studies[J]. European Journal of Medicinal Chemistry, 2020. DOI:10.1016/j.ejmech.2020.112364.
