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NX 2127

Cat. No. 8951 Submit a Review Datasheet / COA / SDS
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Description: Potent BTK Degrader (PROTAC®)
Chemical Name: 3-[[4-[1-[[(3R)-1-[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)-2-pyrazinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for NX 2127

NX 2127 is a potent BTK Degrader (PROTAC®) (DC50 = 4.5 nM and Dmax = 94%). It comprises a BTK binding moiety joined by a linker to a cereblon (CRBN) ligand. NX 2127 also degrades the transcription factors IKZF1 and IKZF3 (DC50 = 57 and 36 nM, respectively). In vivo, NX 2127 possesses potent target degradation activity across species and demonstrates efficacy in preclinical oncology models. NX 2127 is orally bioavailable.

Licensing Information

Sold under license from Nurix Therapeutics

Technical Data for NX 2127

M. Wt 719.85
Formula C39H45N9O5
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 3024312-52-2
PubChem ID 167282486
InChI Key XLWJWCMQMBVNSG-LZDHLTRGSA-N
Smiles O=C1C2=CC(N3C[C@H](CC3)CN4CCC(C5=CC=C(C=C5)NC6=NC(N7CCCCC7)=CN=C6C(N)=O)CC4)=CC=C2C(N1C8C(NC(CC8)=O)=O)=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 2127

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.99 50

Preparing Stock Solutions for NX 2127

The following data is based on the product molecular weight 719.85. 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.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 2.78 mL 13.89 mL 27.78 mL
2.5 mM 0.56 mL 2.78 mL 5.56 mL
5 mM 0.28 mL 1.39 mL 2.78 mL
25 mM 0.06 mL 0.28 mL 0.56 mL

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Product Datasheets for NX 2127

Certificate of Analysis is currently unavailable on-line.
Please contact Customer Service
Safety Datasheet

References for NX 2127

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

Robbins et al (2024) Discovery and preclinical pharmacology of NX-2127, an orally bioavailable Degrader of Bruton's tyrosine kinase with immunomodulatory activity for the treatment of patients with B cell malignancies. J.Med.Chem. 67 2321 PMID: 38300987

If you know of a relevant reference for NX 2127, please let us know.

View Related Products by Target

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Citations for NX 2127

Citations are publications that use Tocris products.

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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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

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