MT-802 | BTK PROTAC | Probechem Biochemicals

Chemical Structure : MT-802

CAS No.: 2231744-29-7

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MT-802 (MT802)

货号: 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).

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5 mg	￥2580	In stock
10 mg	￥3980	In stock
25 mg	￥5980	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	787.834
分子式	C41H41N9O8
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
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

参考文献

1. Buhimschi AD, et al. Biochemistry. 2018 Jun 14. doi: 10.1021/acs.biochem.8b00391.

MT-802 (MT802)

生物&药学活性

物理化学性质&存储条件

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MT-802 (MT802)

生物&药学活性

物理化学性质&存储条件

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