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GSK2269557

Cat. No. M5231
GSK2269557 Structure
Synonym:

Nemiralisib; GSK-2269557

Size Price Availability Quantity
5mg USD 137  USD137 In stock
10mg USD 237  USD237 In stock
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Quality Control & Documentation
Biological 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.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Sprague Dawley male rats
Formulation DMSO/PEG200/water (5:45:50 v/v/v)
Dosages 3 mg/kg; IV:1 mg/kg
Administration oral/i.v.
Chemical Information
Molecular Weight 440.54
Formula C26H28N6O
CAS Number 1254036-71-9
Solubility (25°C) 88 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Down K, et al. J Med Chem. Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.

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Keywords: GSK2269557, Nemiralisib; GSK-2269557 supplier, PI3K, inhibitors, activators


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