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Chemical Structure : MT-802
CAS No.: 2231744-29-7
Catalog No.: PC-35213Not For Human Use, Lab Use Only.
MT-802 (MT802) is a potent BTK PROTAC degrader that induces degradation of both wild-type and C481S mutant BTK (DC50=9.1 nM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $598 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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MT-802 (MT802) is a potent BTK PROTAC degrader 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。
MT-802 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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| Chemical Name/SMILES |
2-(2-(2-(4-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)ethoxy)ethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)acetamide |
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1. Buhimschi AD, et al. Biochemistry. 2018 Jun 14. doi: 10.1021/acs.biochem.8b00391.
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