NX 2127
Tocris Bioscience, part of Bio-Techne | Catalog # 8951
Potent BTK Degrader (PROTAC®)
Product Description
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.PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Licensing Information
Sold under license from Nurix TherapeuticsProduct Specifications
Molecular Weight
719.85
Formula
C39H45N9O5
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
Product Specific Notices for NX 2127
For research use only
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