1254036-66-2

1254036-66-2 structure

Name: GSK2292767
Chemical Name: N-{5-[4-(5-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-1,3-oxazo l-2-yl)-1H-indazol-6-yl]-2-methoxy-3-pyridinyl}methanesulfonamide
CAS Number: 1254036-66-2
Molecular Formula: C₂₄H₂₈N₆O₅S
Molecular Weight: 512.58100
Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
Create Date: 2016-01-19 08:51:13
Modify Date: 2024-01-02 17:54:35
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].

Name	N-{5-[4-(5-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-1,3-oxazo l-2-yl)-1H-indazol-6-yl]-2-methoxy-3-pyridinyl}methanesulfonamide
Synonyms	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

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.