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Chemical Structure : MT-802
Catalog No.: PC-35213Not For Human Use, Lab Use Only.
MT-802 (MT802) is a potent BTK PROTAC that induces degradation of both wild-type and C481S mutant BTK (DC50=9.1 nM).
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MT-802 (MT802) 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, elicits complete BTK knockdown at 250 nM; reduces the pool of active, phosphorylated BTK in cells isolated from CLL patients with the C481S mutation, whereas ibrutinib cannot.
| M.Wt | 787.834 | |
| Formula | C41H41N9O8 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Buhimschi AD, et al. Biochemistry. 2018 Jun 14. doi: 10.1021/acs.biochem.8b00391.
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