MT-802( MT802 )

Catalog No. M13579 CAS No. 2231744-29-7

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

MT-802
Note

Research use only, not for human use.
Brief Description

MT-802 (MT802) is a potent BTK PROTAC that induces degradation of both wild-type and C481S mutant BTK (DC50=9.1 nM).
Description

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.
In Vitro

MT-802 degrades BTK with a DC50 of 9.1 nM with maximal degradation being observed by 250 nM.
In Vivo

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Synonyms

MT802
Pathway

PROTACs
Target

PROTAC
Recptor

PROTAC
Research Area

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Indication

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CAS Number

2231744-29-7
Formula Weight

787.834
Molecular Formula

C41H41N9O8
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 100 mg/mL (126.93 mM)
SMILES

O=C(NC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1)COCCOCCN4CCC(N5N=C(C6=CC=C(OC7=CC=CC=C7)C=C6)C8=C(N)N=CN=C85)CC4
Chemical Name

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

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

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