Home / Active Degraders / DD 03-171

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
1 Image
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%

Product Details
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

DD 03-171 is a potent and selective BTK Degrader (PROTAC®) (IC50 = 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.

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

Reconstitution Calculator
Molarity Calculator

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Molarity Calculator

=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

FAQs

No product specific FAQs exist for this product, however you may

View all Small Molecule FAQs

Reviews for DD 03-171

There are currently no reviews for this product. Be the first to review DD 03-171 and earn rewards!

Have you used DD 03-171?

Submit a review and receive an Amazon gift card.

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review
Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.