GSK2269557

Catalog No.S7937 Synonyms: Nemiralisib

GSK2269557 Chemical Structure

Molecular Weight(MW): 440.54

Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).

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Biological Activity

Description Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).
Targets
PI3Kδ [1]
(Cell-free assay)
9.9(pKi)
In vivo 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[1].

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Sprague Dawley male rats
  • Formulation: DMSO/PEG200/water (5:45:50 v/v/v)
  • Dosages: oral:3 mg/kg; IV:1 mg/kg
  • Administration: oral/i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (199.75 mM)
Ethanol 8 mg/mL (18.15 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 440.54
Formula

C26H28N6O

CAS No. 1254036-71-9
Storage powder
in solvent
Synonyms Nemiralisib

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID