GSK-2292767( GSK2292767 | GSK-2292767 | GSK 2292767 )

Catalog No. M11026 CAS No. 1254036-66-2

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GSK-2292767
Note

Research use only, not for human use.
Brief Description

GSK-2269557 is a highly potent and selective inhibitor of PI3Kδ (pKi=10.1).
Description

GSK-2269557 is a highly potent and selective inhibitor of PI3Kδ (pKi=10.1); displays >1,000 fold selectivity versus others PI3K isoforms; inhibits both IFNγ and IL-2 production in a concentration-dependent manner, with pIC50 values of 8.7 and 8.5, respectively, in a human lung parenchyma assay; shows activity in rat acute OVA model of Th2-driven lung inflammation (ED50=35 ug/kg).COPD Phase 1 Clinical.
In Vitro

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In Vivo

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

GSK2292767 | GSK-2292767 | GSK 2292767
Pathway

PI3K/Akt/mTOR signaling
Target

PI3K
Recptor

PI3Kδ
Research Area

Inflammation/Immunology
Indication

COPD

CAS Number

1254036-66-2
Formula Weight

512.58
Molecular Formula

C24H28N6O5S
Purity

>98% (HPLC)
Solubility

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SMILES

CS(=O)(NC1=CC(C2=CC3=C(C(C4=NC=C(CN5C[C@@H](C)O[C@@H](C)C5)O4)=C2)C=NN3)=CN=C1OC)=O
Chemical Name

N-(5-(4-(5-(((2R,6S)-2,6-dimethylmorpholino)methyl)oxazol-2-yl)-1H-indazol-6-yl)-2-methoxypyridin-3-yl)methanesulfonamide

1. Down K, et al. J Med Chem. 2015 Sep 24;58(18):7381-99.

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