1821038-80-5

1821038-80-5 structure
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
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