DD 03-171
Tocris Bioscience, part of Bio-Techne | Catalog # 7160
Potent and selective BTK Degrader (PROTAC®)
Key Product Details
Description
Potent and selective BTK Degrader (PROTAC®)
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 InstituteProduct Specifications
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for DD 03-171
For research use only
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