生物活性 | |||
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描述 | 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]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.27mL 0.25mL 0.13mL |
6.35mL 1.27mL 0.63mL |
12.69mL 2.54mL 1.27mL |
参考文献 |
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