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NX 5948

Cat. No. 8856 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective BTK Degrader (PROTAC®)
Chemical Name: 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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity 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.

Licensing Information

Sold under license from Nurix Therapeutics

Technical Data for NX 5948

M. Wt 806.97
Formula C42H54N12O5
Storage Store at -20°C
Purity ≥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

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 for NX 5948

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.35 50

Preparing Stock Solutions for NX 5948

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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References for NX 5948

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

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Citations for NX 5948

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Literature in this Area

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