SC239 is a cleavable 2-aminophenyl hemiasterlin agent-linker. SC239 can be as the agent-linker for ADC. SC239 is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
SC239 is composed of a tubulin-targeting 3-aminophenyl hemiasterlin warhead, SC209 , and a cleavable valine citrulline p-aminobenzyl carbamate linker functionalized with dibenzocyclooctyne (DBCO)[1].The SC239 drug-linker is conjugated via a cleavable valine citrulline p-aminobenzyl carbamate linker functionalized with dibenzocyclooctyne (DBCO)[1].SC239 conjugates exhibits better cytotoxic activity on Igrov1 cells which have lower expression levels of FolRα[1].
References:
[1]. Xiaofan Li, et al. Abstract 1782: Discovery and activity of STRO-002, a novel ADC targeting folate receptor alpha for ovarian and endometrial cancer. Cancer Res (2018) 78 (13_Supplement): 1782.