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PI3Kγ inhibitor 4

Names

[ CAS No. ]:
1821038-80-5

[ Name ]:
PI3Kγ inhibitor 4

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K
Research Areas >> Inflammation/Immunology

[Target]

PI3Kγ:40 nM (IC50)

PI3Kα:300 nM (IC50)


[In Vitro]

PI3Kγ inhibitor 4 inhibits PI3Kγ and PI3Kα in U937 cells, with IC50s of 120 nM and 6250 nM, respectively[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].

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H24N4O4S

[ Molecular Weight ]:
416.49

Related Compounds