| Identification | Back Directory | [Name]
Benzenesulfonamide, 3-[6-amino-5-(2-methyl-5-oxazolyl)-3-pyridinyl]-N-(2-hydroxy-2-methylpropyl)-4-methyl- | [CAS]
1821038-80-5 | [Synonyms]
PI3Kγ inhibitor 4
Benzenesulfonamide, 3-[6-amino-5-(2-methyl-5-oxazolyl)-3-pyridinyl]-N-(2-hydroxy-2-methylpropyl)-4-methyl- | [Molecular Formula]
C20H24N4O4S | [MOL File]
1821038-80-5.mol | [Molecular Weight]
416.49 |
| Hazard Information | Back Directory | [Uses]
PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC50 of 40 nM. PI3Kγ inhibitor 4 shows ～7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation[1]. | [in vivo]
PI3Kγ inhibitor 4 (10-20 mg/kg; a single p.o.) dose dependently inhibits the amplitude of the enhanced pause (ΔPenh) response to ovalbumin in a model of airway inflammation[1].
PI3Kγ inhibitor 4 (a single p.o.) exhibits high oral bioavailability (72, 94 and 122%) and Cmax (1.53, 12.2 and 25.2 μM) following oral administration (10, 100 and 300 mg/kg) in rats[1]. | [IC 50]
PI3Kγ: 40 nM (IC50); PI3Kα: 300 nM (IC50) | [References]
[1] Bellenie BR, et, al. Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ. J Med Chem. 2021 Aug 26;64(16):12304-12321. DOI:10.1021/acs.jmedchem.1c00986 |
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