1821038-80-5

1821038-80-5 structure

Name: PI3Kγ inhibitor 4
Chemical Name: PI3Kγ inhibitor 4
CAS Number: 1821038-80-5
Molecular Formula: C₂₀H₂₄N₄O₄S
Molecular Weight: 416.49
Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
Create Date: 2021-10-07 20:02:25
Modify Date: 2024-01-16 07:44:51
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].

Name	PI3Kγ inhibitor 4

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.

Molecular Formula	C₂₀H₂₄N₄O₄S
Molecular Weight	416.49