MT-802 是基于PROTAC技术的、BTK 的降解剂,DC50 值为 1 nM。MT-802具有治疗C481S突变型慢性淋巴细胞白血病(CLL)的潜力。
CAS:2231744-29-7
分子式:C41H41N9O8
分子量:787.82
纯度:98%
存储:Store at -20°C
Background:
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.