DD 03-171

Tocris Bioscience | Catalog # 7160

Potent and selective BTK Degrader (PROTAC®)
Tocris Bioscience

Key Product Details

Description

Potent and selective BTK Degrader (PROTAC®)
View all Active Degraders »

Product Description

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

Product Specifications for DD 03-171

Molecular Weight

991.16

Formula

C55H62N10O8

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

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 all 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 0.40 mL 2.02 mL 4.04 mL
5 mM 0.20 mL 1.01 mL 2.02 mL
25 mM 0.04 mL 0.20 mL 0.40 mL

Calculators

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Background References

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

Product Documents for DD 03-171

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for DD 03-171

For research use only

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