PI3Kγ inhibitor 4

Modify Date: 2024-01-16 07:44:51

PI3Kγ inhibitor 4 Structure
PI3Kγ inhibitor 4 structure
Common Name PI3Kγ inhibitor 4
CAS Number 1821038-80-5 Molecular Weight 416.49
Density N/A Boiling Point N/A
Molecular Formula C20H24N4O4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PI3Kγ inhibitor 4


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].

 Names

Name PI3Kγ inhibitor 4

 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
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
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.