DD 03-171

Name: DD 03-171
Brand: Tocris Bioscience
SKU: 7160

Tocris Bioscience, part of Bio-Techne | Catalog # 7160

Citations (2)

COA / SDS

Potent and selective BTK Degrader (PROTAC®)

Key Product Details

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)
Molecular Weight:	991.16

View Full Technical Details for DD 03-171

Technical Data
Citations

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 for DD 03-171

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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

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References for DD 03-171

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

Dobrovolsky Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. Blood 2019 PMID: 30545835