MT-802 (MT802) is a potentBTK PROTAC that induces degradation of both wild-type and C481S mutantBTK (DC50=9.1 nM); MT-802 recruitsBTK to the cereblon E3 ubiquitin ligase complex to triggerBTK ubiquitination and degradation via the proteasome; MT-802 binds fewer off-target kinases than ibrutinib does and retains an equivalent potency (>99% degradation at nanomolar concentrations) against wild-type and C481S BTK, elicits completeBTK knockdown at 250 nM; reduces the pool of active, phosphorylatedBTK in cells isolated from CLL patients with the C481S mutation, whereas ibrutinib cannot.
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MT-802 is a potent BTK PROTAC that induces degradation of both wild-type and C481S mutant BTK (DC50=9.1 nM). MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. MT-802 binds fewer off-target kinases than ibrutinib does and retains an equivalent potency (>99% degradation at nanomolar concentrations) against wild-type and C481S BTK. In cells isolated from CLL (chronic lymphocytic leukemia) patients with the C481S mutation, MT-802 is able to reduce the pool of active, phosphorylated BTK whereas ibrutinib cannot[1].
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