NX 5948

Tocris Bioscience | Catalog # 8856

Potent and selective BTK Degrader (PROTAC®)
Tocris Bioscience
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Key Product Details

Description

Potent and selective BTK Degrader (PROTAC®)

Product Description

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.

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

Licensing Information

Sold under license from Nurix Therapeutics

Product Specifications for NX 5948

Molecular Weight

806.97

Formula

C42H54N12O5

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

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Solubility

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 all 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 0.50 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 0.50 mL

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Background References

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

There are currently no references for this product.

Product Documents for NX 5948

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for NX 5948

For research use only

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