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).

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).
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]
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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
Formula

C26H28N6O

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

In vivo Formulation Calculator (Clear solution)

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03398421 Completed Drug: Nemiralisib|Drug: Itraconazole Pulmonary Disease Chronic Obstructive GlaxoSmithKline January 17 2018 Phase 1
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

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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