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Chemical Structure : BIO-8169
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.
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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.
| M.Wt | 449.51 | |
| Formula | C24H27N5O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Pfaffenbach M, et al. J Med Chem. 2024 May 2. doi: 10.1021/acs.jmedchem.4c00560.
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