Catalog No.: PC-22268Not For Human Use, Lab Use Only.
BIO-8169 is a highly potent, selective, brain-penetrant and oral bioavailable IRAK4 inhibitor with IC50 of 0.23 nM, potently inhibits R848 stimulated IL-1β production with IC50 of 246 nM in HWB assays.
BIO-8169 is a highly potent, selective, brain-penetrant and oral bioavailable IRAK4 inhibitor with IC50 of 0.23 nM, potently inhibits R848 stimulated IL-1β production with IC50 of 246 nM in HWB assays.
BIO-8169 displays high selectivity in a broad kinome panel (Eurofins: 468 kinases) at 1 uM, only three kinases in the panel shows greater than 80% inhibition (FLT3: 418 nM, TRKA: 752 nM, TRKB: 1155 nM).
BIO-8169 has an excellent PK profile, reduces the in vivo production of pro-inflammatory cytokines, and is tolerated in toxicity studies in rodents and dogs at margins.
BIO-8169 (30 mg/kg QD and 20 mg/kg BID) inhibited the development of EAE with concomitant reduction of number of inflammatory foci, T cell infiltrates, and activated microglial and macrophage density, in mouse model of human multiple sclerosis.
