2416130-57-7

2416130-57-7 structure

Name: NRX-0492
Chemical Name: NRX-0492
CAS Number: 2416130-57-7
Molecular Formula: C₄₃H₅₁N₁₁O₆
Molecular Weight: 817.94
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Btk
Create Date: 2023-05-31 22:12:02
Modify Date: 2024-01-11 16:15:34
NRX-0492 is an orally active and potent degrader of BTK. NRX-0492 catalyzes ubiquitylation and proteasomal degradation of BTK with DC50≤0.2 nM and DC90≤0.5 nM, respectively. NRX-0492 inhibits B-cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion. Moreover, NRX-0492 also links a noncovalent BTK-binding domain to Cereblon. Cereblon is an adaptor protein of the E3 ubiquitin ligase complex[1].

Name	NRX-0492

Description	NRX-0492 is an orally active and potent degrader of BTK. NRX-0492 catalyzes ubiquitylation and proteasomal degradation of BTK with DC50≤0.2 nM and DC90≤0.5 nM, respectively. NRX-0492 inhibits B-cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion. Moreover, NRX-0492 also links a noncovalent BTK-binding domain to Cereblon. Cereblon is an adaptor protein of the E3 ubiquitin ligase complex[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk
References	[1]. Zhang D, et al. NRX-0492 degrades wild-type and C481 mutant BTK and demonstrates in vivo activity in CLL patient-derived xenografts. Blood. 2023 Mar 30;141(13):1584-1596.

Molecular Formula	C₄₃H₅₁N₁₁O₆
Molecular Weight	817.94