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TBK1 PROTAC® 3i

Cat. No. 7259 1 次引用 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent TANK-binding kinase 1 (TBK1) PROTAC®
化学名： (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
纯度： ≥98% (HPLC)
说明书
引用文献 (1)
评论
文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for TBK1 PROTAC® 3i

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.

技术数据 for TBK1 PROTAC® 3i

分子量 1093.19
公式 C53H74BrN9O9S
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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

溶解性数据 for TBK1 PROTAC® 3i

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 109.32 100

制备储备液 for TBK1 PROTAC® 3i

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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产品说明书 for TBK1 PROTAC® 3i

分析证书/产品说明书
化学品安全技术说明书

参考文献 for TBK1 PROTAC® 3i

参考文献是支持产品生物活性的出版物。

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.

按标靶查看相关产品

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

1 篇 TBK1 PROTAC® 3i 的引用文献

引用文献是使用了 Tocris 产品的出版物。 TBK1 PROTAC® 3i 的部分引用包括：

Sun et al (2023) Targeting TBK1 to overcome resistance to cancer immunotherapy. Nature 615 158 PMID: 36634707

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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。

TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia