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DD 03-171

Cat. No. 7160 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for DD 03-171

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.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Technical Data for DD 03-171

M. Wt 991.16
Formula C55H62N10O8
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2366132-45-6
PubChem ID 138059681
InChI Key QBPVFCNYKUENHU-UHFFFAOYSA-N
Smiles CN1C=C(N=C(NC2=CC=C(C=C2)C(=O)N2CCN(CCCCCCNC(=O)CNC3=C4C(=O)N(C5CCC(=O)NC5=O)C(=O)C4=CC=C3)CC2)C1=O)C1=C(C)C(NC(=O)C2=CC=C(C=C2)C(C)(C)C)=CC=C1

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.

Solubility Data for DD 03-171

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.56 50

Preparing Stock Solutions for DD 03-171

The following data is based on the product molecular weight 991.16. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 2.02 mL 10.09 mL 20.18 mL
2.5 mM 0.4 mL 2.02 mL 4.04 mL
5 mM 0.2 mL 1.01 mL 2.02 mL
25 mM 0.04 mL 0.2 mL 0.4 mL

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References for DD 03-171

References are publications that support the biological activity of the product.

Dobrovolsky et al (2019) Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. Blood 133 952 PMID: 30545835

If you know of a relevant reference for DD 03-171, please let us know.

View Related Products by Target

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Citations for DD 03-171

Citations are publications that use Tocris products.

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Literature in this Area

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia