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NX 5948

Cat. No. 8856 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 BTK Degrader (PROTAC®)
化学名： 3-[[4-[1-[[1-[6-[[[(3S)-2,6-Dioxo-3-piperidinyl]amino]carbonyl]-3-pyridinyl]-4-piperidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-[(3R)-3-(3-methyl-2-oxo-1-imidazolidinyl)-1-piperidinyl]-2-pyrazinecarboxamide
纯度： ≥98% (HPLC)
说明书
引用文献
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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 NX 5948

NX 5948 is a potent and selective Bruton's tyrosine kinase (BTK) Degrader (PROTAC®) (DC50 = <1 nM; Dmax = 98%). Comprises a BTK binding moiety joined by a linker to cereblon (CRBN) ligand. In vitro, NX-5948 very potently, rapidly and completely degrades BTK in primary human B cells (DC50 = 0.034 nM). NX 5948 degrades BTK, inhibits tumor growth and increases survival in TMD8 xenograft mouse models of brain maligancy. Reduces inflammation and symptom severity in a mouse model of collagen-induced arthritis. NX 5948 is orally bioavailable and blood brain barrier penetrant.

许可信息

Sold under license from Nurix Therapeutics

技术数据 for NX 5948

分子量 806.97
公式 C42H54N12O5
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2649400-34-8
PubChem ID 156464216
InChI Key HPTPDBYCFHFWJG-CWTKIQHKSA-N
Smiles NC(C1=C(N=C(N2C[C@H](N3C(N(CC3)C)=O)CCC2)C=N1)NC4=CC=C(C5CCN(CC5)CC6CCN(C7=CN=C(C(N[C@@H]8C(NC(CC8)=O)=O)=O)C=C7)CC6)C=C4)=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 NX 5948

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 40.35 50

制备储备液 for NX 5948

以下数据基于产品分子量 806.97。 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
0.5 mM 2.48 mL 12.39 mL 24.78 mL
2.5 mM 0.5 mL 2.48 mL 4.96 mL
5 mM 0.25 mL 1.24 mL 2.48 mL
25 mM 0.05 mL 0.25 mL 0.5 mL

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参考文献 for NX 5948

参考文献是支持产品生物活性的出版物。

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关键词: NX 5948, NX 5948 supplier, NX5948, Potent, selective, active, degraders, degrades, Bruton, tyrosine, kinase, cereblon, CRBN, PROTAC, PROTACs, proteolysis, targeting, chimeras, targeted, protein, degradation, tpd, Brutons, Tyrosine, Kinase, BTK, in, vivo, BBB, penetrant, orally, bioavailable, brain, malignancies, Degraders, (BTK), 8856, Tocris Bioscience

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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!

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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