Product Data Sheet

NRX-0492

Catalog No. A24841

main product photo
NRX-0492 is an orally active PROTAC BTK degrader that promotes the ubiquitination and proteasomal degradation of Bruton's tyrosine kinase (BTK) with DC50 values as low as 0.2 nM. This compound effectively inhibits B cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion, demonstrating significant antitumor activity against chronic lymphocytic leukemia. NRX-0492 comprises a BTK inhibitor, an E3 ligase ligand derived from Thalidomide, and a PROTAC linker, making it a valuable tool for studying BTK-related pathways and therapies.
Chemical Information
Catalog NumA24841
M. Wt817.94
FormulaC43H51N11O6
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.2416130-57-7
Synonyms
SMILESNC(C1=C(N=C(N2CCC[C@@H](N3CCN(C)C3=O)C2)C=N1)NC(C=C4)=CC=C4C(CC5)CCN5C[C@@H](C6)CCN6C7=CC=C(C(C(N8C9C(NC(CC9)=O)=O)=O)=C7)C8=O)=O
Biological Activity
DescriptionNRX-0492 is an orally active PROTAC BTK degrader that promotes the ubiquitination and proteasomal degradation of Bruton's tyrosine kinase (BTK) with DC50 values as low as 0.2 nM. This compound effectively inhibits B cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion, demonstrating significant antitumor activity against chronic lymphocytic leukemia. NRX-0492 comprises a BTK inhibitor, an E3 ligase ligand derived from Thalidomide, and a PROTAC linker, making it a valuable tool for studying BTK-related pathways and therapies.
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SHIPPING AND STORAGE
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