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NAMPT PROTAC® A7

Cat. No. 7842 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 and selective nicotinamide phosphoribosyl transferase (NAMPT) Degrader (PROTAC®)
化学名： (2S,4R)-1-((S)-18-(tert-Butyl)-1,16-dioxo-1-(4-((4-((4-(3-(pyridin-3-ylmethyl)thioureido)phenyl)sulfonyl)piperazin-1-yl)methyl)phenyl)-5,8,11,14-tetraoxa-2,17-diazanonadecan-19-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
纯度： ≥98% (HPLC)
说明书
引用文献
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 NAMPT PROTAC® A7

NAMPT PROTAC A7 is a potent and selective intracellular nicotinamide phosphoribosyl transferase (iNAMPT) Degrader (PROTAC®) (IC50 of 9.5 nM against the enzymatic activity of NAMPT). Comprises a potent NAMPT inhibitor joined by a linker to a ligand for Von Hippel-Lindau (VHL) protein. Proteomic analysis of global protein level changes confirms selectivity. NAMPT PROTAC A7 decreases iNAMPT level and the secretion of extracellular NAMPT (eNAMPT) in CT26 or MC38 cells. In CT26 tumor bearing BALB/c mice, the compound degrades tumoral NAMPT, and boosts antitumor immunity by inhibiting tumor infiltrating myeloid-derived suppressive cells.

Antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF4335 and MAB40441.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

技术数据 for NAMPT PROTAC® A7

分子量 1185.49
公式 C58H76N10O11S3
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2484876-94-8
InChI Key WJRWRYBOCSUYIN-IWIXZVHYSA-N
Smiles O=C(C1=CC=C(C=C1)CN2CCN(CC2)S(=O)(C3=CC=C(C=C3)NC(NCC4=CN=CC=C4)=S)=O)NCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(N=CS7)C)C=C6)C)=O)=O)=O

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 NAMPT PROTAC® A7

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 23.71 20

制备储备液 for NAMPT PROTAC® A7

以下数据基于产品分子量 1185.49。 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
0.2 mM 4.22 mL 21.09 mL 42.18 mL
1 mM 0.84 mL 4.22 mL 8.44 mL
2 mM 0.42 mL 2.11 mL 4.22 mL
10 mM 0.08 mL 0.42 mL 0.84 mL

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产品说明书 for NAMPT PROTAC® A7

分析证书/产品说明书
化学品安全技术说明书

参考文献 for NAMPT PROTAC® A7

参考文献是支持产品生物活性的出版物。

Wu et al (2022) NAMPT-targeting PROTAC promotes antitumor immunity via suppressing myeloid-derived suppressor cell expansion. Acta.Pharm.Sin.B 12 2859 PMID: 35755293

If you know of a relevant reference for NAMPT PROTAC® A7, please let us know.

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关键词: NAMPT PROTAC® A7, NAMPT PROTAC® A7 supplier, protacs, active, degraders, potent, selective, nicotinamide, phosphoribosyl, transferase, NAMPT, Degrader, antitumor, immunity, Other, Degraders, 7842, Tocris Bioscience

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该领域的文献

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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