MT-802 is a potent BTK degrader based on PROTAC technology, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL)[1]. DC50: 1 nM (BTK)[1].
MT-802 degrades BTK with a DC50 of 9.1 nM with maximal degradation being observed by 250 nM[1].
[1]. Buhimschi AD, et al. Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation. Biochemistry. 2018 Jul 3;57(26):3564-3575.
















