TBK1 PROTAC® 3i

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Cat.No. 7259 - TBK1 PROTAC® 3i | C53H74BrN9O9S | CAS No. 2052306-13-3
Description: Potent TANK-binding kinase 1 (TBK1) Degrader
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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

Potent TANK-binding kinase 1 (TBK1) 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) also available.

Technical Data

M. Wt 1093.19
Formula C53H74BrN9O9S
Storage Store at -20°C
Purity ≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 109.32 100

Preparing Stock Solutions

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 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
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

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References

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

Crew et al (2018) Identification and characterization of Von Hippel-Lindau-recruiting proteolysis targeting chimeras (PROTACs) of TANK-binding kinase 1. J.Med.Chem. 61 583 PMID: 28692295


If you know of a relevant reference for TBK1 PROTAC® 3i, please let us know.

Keywords: TBK1 PROTAC® 3i, TBK1 PROTAC® 3i supplier, TANK-binding, kinase, 1, TBK1, potent, Degrader, Degraders, PROTACs, targeted, protein, degradation, TPD, von, Hippel, Lindau, VHL, E3, ligase, Active, TANK, binding, (TBK), 7259, Tocris Bioscience

Citations for TBK1 PROTAC® 3i

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Literature in this Area

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Epigenetics in Cancer Poster

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Targeted Protein Degradation Poster

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