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DD 03-171

Catalog #: 7160 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7160/5
DD 03-171 | CAS No. 2366132-45-6 | Active Degraders
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Description: Potent and selective BTK Degrader (PROTAC®)

Chemical Name: 4-(1,1-Dimethylethyl)-N-[3-[6-[[4-[[4-[6-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]acetyl]amino]hexyl]-1-piperazinyl]carbonyl]phenyl]amino]-4,5-dihydro-4-methyl-5-oxo-2-pyrazinyl]-2-methylphenyl]benzamide

Purity: ≥98%

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Biological Activity

DD 03-171 is a potent and selective BTK Degrader (PROTAC®) (DC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.

BTK antibodies validated for Western Blot also available: Catalog # MAB5807 and NBP2-02472.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data

M.Wt:
991.16
Formula:
C55H62N10O8
Solubility:
Soluble to 50 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2366132-45-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold under license from Dana-Farber Cancer Institute

Background References

  1. Bruton tyrosine kinase degradation as a therapeutic strategy for cancer.
    Dobrovolsky et al.
    Blood, 2019;133:952

Product Datasheets

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