SJF620是一种PROTACBTK降解剂,DC50为7.9nM。SJF620含有Lenalidomide类似物,可募集CRBN。
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SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN[1].
SJF620 is a PROTAC that retains potent degradation of BTK in cellular assays with a DC50 of 7.9 nM in Burkitt lymphoma cell line NAMALWA[1].
SJF620 has a super pharmacokinetic profile in mice (1 mg/kg; i.v.) with half life (t1/2) of 1.64 h. SJF620 exhibits a significantly better pharmacokinetic profile than MT802[1].
[1]. Jaime-Figueroa S, et al. Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties. 2020 Feb 1;30(3):126877.
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