TBK1 PROTAC® 3i

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Cat.No. 7259 - TBK1 PROTAC® 3i | C53H74BrN9O9S | CAS No. 2052306-13-3
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
评论
文献 (4)

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) also available.

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

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.

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, Active, TANK, binding, (TBK), 7259, Tocris Bioscience

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