Nemiralisib (GSK2269557)

For research use only.

Catalog No.S7937 Synonyms: Nemiralisib

1 publication

Nemiralisib (GSK2269557) Chemical Structure

CAS No. 1254036-71-9

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

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Selleck's Nemiralisib (GSK2269557) has been cited by 1 publication

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Biological Activity

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


Animal Research:[1]
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  • Animal Models: Sprague Dawley male rats
  • 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


CAS No. 1254036-71-9
Storage powder
in solvent
Synonyms Nemiralisib
Smiles CC(C)N1CCN(CC1)CC2=CN=C(O2)C3=C4C=NNC4=CC(=C3)C5=C6C=CNC6=CC=C5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03189589 Completed Drug: GSK2269557 500 µg|Drug: GSK2269557 750 µg Pulmonary Disease Chronic Obstructive GlaxoSmithKline June 15 2017 Phase 1
NCT02972905 Completed Drug: GSK2269557 ELLIPTA DPI|Drug: Placebo ELLIPTA DPI Pulmonary Disease Chronic Obstructive GlaxoSmithKline October 2016 Phase 1
NCT02593539 Completed Drug: GSK2269557 DPI 500 mcg Activated PI3K-delta Syndrome GlaxoSmithKline July 22 2016 Phase 2

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID