product name GSK2269557
Description: GSK-2269557, also known as Nemiralisib, is a potent and selective PI3Kδ inhibitor(pKi = 9.9). It is active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation. PI3Kδ is highly enriched in leukocytes, making it an attractive target for the treatment of inflammatory conditions, such as asthma,6 chronic obstructive pulmonary disease (COPD), and autoimmune diseases. GSK-2269557 is is currently in clinical trials for the treatment of respiratory diseases such as asthma and COPD.
References: J Med Chem. 2015 Sep 24;58(18):7381-99.
440.54
Formula
C26H28N6O
CAS No.
1254036-71-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 88 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 8 mg/mL (18.2 mM)
Solubility (In vivo)
Synonyms
Nemiralisib
other peoduct :
| In Vitro |
In vitro activity: GSK-2269557 has low oral bioavailability (F=2%) and in vivo clearance of 28 mL/min/kg but has a high volume of distribution of 6.3 L/kg. GSK-2269557 induces concentration-dependent increases in QT interval and Tp-e at 0.3 and 1 μM (1 and 0.5 Hz) and an increase in QRS at 1 μM (2 Hz), however, no treatment-related torsades de pointes (TdP) arrhythmias are observed. In a disease relevant brown Norway rat acute OVA model of Th2 driven lung inflammation, GSK-2269557 is shown to protect against eosinophil recruitment with an ED50 of 67 μg/kg and dose-dependently reduces recruitment of all leukocyte subpopulations and IL-13 in the lungs. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Sprague Dawley male rats |
| Animal model | Formulated in DMSO/PEG200/water (5:45:50 v/v/v); oral:3 mg/kg; IV:1 mg/kg; oral and i.v. |
| Formulation & Dosage | |
| References | J Med Chem. 2015 Sep 24;58(18):7381-99. |
