TBK1 PROTAC® 3i
Tocris Bioscience, part of Bio-Techne | Catalog # 7259
Potent TANK-binding kinase 1 (TBK1) PROTAC®
Key Product Details
Description
Potent TANK-binding kinase 1 (TBK1) PROTAC®
Product Description
TBK1 PROTAC® 3i is a potent TANK-binding kinase 1 (TBK1) PROTAC® Degrader (DC50 = 12 nM, Dmax = 96%). Exhibits >50-fold selectivity for TBK1 over the closely related IKKε. Comprises a ligand for von-Hippel Lindau (VHL) protein joined by a linker to a TBK1-targeting moiety. Brings about near complete degradation of TBK1 in mutant K-Ras and wild-type cancer cell lines with no significant effect of proliferation.Negative control TBK1 control PROTAC® 4 (Cat. No. 7260) and TBK1 antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF9934 and NB100-56705.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Product Specifications
Molecular Weight
1093.19
Formula
C53H74BrN9O9S
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(2S,4R)-1-((S)-18-(4-((5-Bromo-4-((3-(N-methylcyclobutanecarboxamido)propyl)amino)pyrimidin-2-yl)amino)phenoxy)-2-(tert-butyl)-4-oxo-6,10,15-trioxa-3-azaoctadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
CAS Number
2052306-13-3
PubChem ID
124108661
InChI Key
QMGHHBHPDDAGGO-IIWOMYBWSA-N
SMILES
CN(C(C1CCC1)=O)CCCNC2=NC(NC3=CC=C(C=C3)OCCCOCCCCOCCCOCC(N[C@@H](C(C)(C)C)C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)O)=O)=O)=NC=C2Br
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 | 109.32 | 100 |
Preparing Stock Solutions
for TBK1 PROTAC® 3i
The following data is based on the product molecular weight 1093.19
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 |
|---|---|---|---|
| 1 mM | 0.91 mL | 4.57 mL | 9.15 mL |
| 5 mM | 0.18 mL | 0.91 mL | 1.83 mL |
| 10 mM | 0.09 mL | 0.46 mL | 0.91 mL |
| 50 mM | 0.02 mL | 0.09 mL | 0.18 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Crew Identification and characterization of Von Hippel-Lindau-recruiting proteolysis targeting chimeras (PROTACs) of TANK-binding kinase 1. J.Med.Chem. 2018 PMID: 28692295
Product Specific Notices for TBK1 PROTAC® 3i
For research use only
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