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Tocris Bioscience™ NX 5948
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.
Specifications
Specifications
| Chemical Name or Material | 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 | 2649400-34-8 |
| Quantity | 5 mg |
| Target | Active Degraders |
| Molecular Formula | C42H54N12O5 |
| Purity | 98% |
Product Title
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