GSK2292767

Names

[ Name ]:
GSK2292767

[Synonym ]:
N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide
AZD 4547
QCR-89
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethylpiperazin-1-yl]benzamide
GSK2292767

Biological Activity

[Description]:

GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC50 of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease[1].

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

Research Areas >> Inflammation/Immunology

[Target]

PI3Kδ:10.1 (pIC50)

[In Vitro]

GSK2292767 exhibits high clearance (50 mL/min/kg) in vivo and low oral bioavailability (F < 2%) in a rat PK study[1]. GSK2292767 (0.01-1 μM) has no eﬀect on QT interval, Tp‑e, or QRS and no signiﬁcant risk of TdP arrhythmias in a rabbit cardiac ventricular wedge assay[1]. GSK2292767 protect against eosinophil recruitment with an ED50 of 35 μg/kg in the brown Norway rat acute OVA model of Th2 driven inﬂammation in the lungs of rats[1].

[References]

[1]. Down K, et, al. Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease. J Med Chem. 2015 Sep 24; 58(18): 7381-99.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₂₈N₆O₅S

[ Molecular Weight ]:
512.58100

[ Exact Mass ]:
512.18400

[ PSA ]:
143.85000

[ LogP ]:
4.36090

[ Storage condition ]:
-20℃