GSK2292767

• CAT Number: M015632
• CAS Number: 1254036-66-2
• Molecular Formula: C24H28N6O5S
• Molecular Weight: 512.58
• Purity: ≥95%
• Synonyms: N-[5-[4-[5-[[(2S,6R)-2,6-dimethylmorpholin-4-yl]methyl]-1,3-oxazol-2-yl]-1H-indazol-6-yl]-2-methoxypyridin-3-yl]methanesulfonamide
• InChI: InChI=1S/C24H28N6O5S/c1-14-11-30(12-15(2)34-14)13-18-9-26-23(35-18)19-5-16(6-21-20(19)10-27-28-21)17-7-22(29-36(4,31)32)24(33-3)25-8-17/h5-10,14-15,29H,11-13H2,1-4H3,(H,27,28)/t14-,15+
• InChIKey: NLUPPCTVKHDVIQ-GASCZTMLSA-N
• SMILES: CC1CN(CC(O1)C)CC2=CN=C(O2)C3=C4C=NNC4=CC(=C3)C5=CC(=C(N=C5)OC)NS(=O)(=O)C

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].
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].

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.
 [Content Brief]