NRX-0492
Product Specifications
CAS Number
2416130-57-7
Target
BTK, Others, PROTACs
Related Pathways
Others, Tyrosine Kinase/Adaptors, PROTAC, Angiogenesis
Bioactivity
NRX-0492 is an orally administered compound that efficiently degrades Bruton's tyrosine kinase (BTK) by catalyzing its ubiquitylation and subsequent proteasomal degradation, achieving half-maximal degradation concentrations (DC50) of ≤0.2 nM and 90% degradation concentrations (DC90) of ≤0.5 nM. Additionally, NRX-0492 suppresses B-cell receptor (BCR) signaling, transcriptional activities, and chemokine production by linking a noncovalent BTK-binding domain to Cereblon, an adaptor protein within the E3 ubiquitin ligase complex [1].
Smiles
O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=C(C2)N4C[C@H](CN5CCC(CC5)C6=CC=C(NC7=NC(=CN=C7C(N)=O)N8C[C@@H](CCC8)N9CCN(C)C9=O)C=C6)CC4
Molecular Formula
C43H51N11O6
Molecular Weight
817.94
Shipping Conditions
Ice Packs
Storage Temperature
-20°C
Available Sizes
Frequently Asked Questions
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