Chemical Structure : BIO-8169
CAS No.:
2792153-06-9
BIO-8169
(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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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449.51
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Formula
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C24H27N5O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(1-cyclopropyl-2-oxo-1,2-dihydropyridin-3-yl)-7-isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)imidazo[1,2-a]pyrimidine-6-carboxamide
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References
1. Pfaffenbach M, et al. J Med Chem. 2024 May 2. doi: 10.1021/acs.jmedchem.4c00560.
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