NRX-0492

Overview

NRX-0492 is an orally active BTK PROTAC degrader, with a binding IC 50 of 1.2 nM for both wild-type BTK and BTK T474I , and 2.7 nM for BTK C481S , and exhibits cellular DC 50 values of 0.1 nM and 0.2 nM against wild-type BTK and BTK C481S , respectively. NRX-0492 catalyzes the ubiquitination and proteasomal degradation of wild-type and drug-resistant mutant BTK by recruiting the CRBN E3 ubiquitin ligase complex. NRX-0492 inhibits the BCR signaling pathway and its downstream NF-κB/MYC transcriptional program, achieves rapid and sustained degradation in primary CLL cells, and exhibits extremely low cytotoxicity. NRX-0492 degrades BTK , inhibits tumor cell proliferation and activation, and significantly suppresses tumor growth in xenograft models. NRX-0492 can be used in research related to chronic lymphocytic leukemia and diffuse large B-cell lymphoma. (Pink: Btk ligand ( HY-49421 ); Blue: Cereblon ligand ( HY-W087383 ); Black: linker ( HY-60263 )).

Application

Products | Products > Disease Areas > Cancer | Products > Disease Areas > Inflammation or Immune System Disease | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Leukemia/Lymphoma/Myeloma | Products > Disease Areas > Blood Disease | Products > Disease Areas > Autoimmune Disease | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > NF-κB | Products > Research Areas > Inflammation/Immunology | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Immunotherapy | Products > Research Areas > Cancer > Cancer Drug Resistance | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > Btk | Products > Signaling Pathways > c-Myc | Products > Signaling Pathways > NF-κB

Product Information

• Catalog No.: HY-153357
• CAS No.: 2416130-57-7
• Molecular Formula: C43H51N11O6
• Molecular Weight: 817.94
• Purity: 98.30%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Availability: In-stock

Source

Original product source