NRX-0492

CAT: 0931-MF-0155152-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0931-MF-0155152-01Size:5 mg
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AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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
Cool pack
Storage Temperature
-20°C

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