Bioactivity | 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]. |
In Vivo | 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 protects 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]. |
Name | GSK2292767 |
CAS | 1254036-66-2 |
Formula | C24H28N6O5S |
Molar Mass | 512.58 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |