ARQ 531
ARQ-531 is a potent and orally active BTK inhibitor with potential antineoplastic activity. ARQ 531 is a reversible non-covalent inhibitor of Bruton's Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases. In GCB-DLBCL cell lines (SUDHL-4 and DOHH-2), ARQ 531 potently suppressed expression of anti-apoptotic c-Myc and BCL6 oncoproteins in a dose-dependent fashion, and concomitantly induced apoptotic cleavage of PARP protein.
| Supplier | BOC Sciences |
|---|---|
| Product # | 2095393-15-8 |
| Pricing | Inquire |
| Cas | 2095393-15-8 |
| Molecular Weight | 478.93 |
| Molecular Formula | C25H23ClN4O4 |
| Canonical SMILES | O=C(C1=CC=C(OC2=CC=CC=C2)C=C1Cl)C3=CNC4=NC=NC(N[C@H]5CO[C@H](CO)CC5)=C43 |