Home PI3K/Akt/mTOR PI3K inhibitor Nemiralisib For research use only.

Nemiralisib

Synonyms: GSK2269557

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

Nemiralisib Chemical Structure

Nemiralisib Chemical Structure

CAS No. 1254036-71-9

Purity & Quality Control

Batch: S793701 DMSO]88 mg/mL]false]Ethanol]8 mg/mL]false]Water]Insoluble]false Purity: 99.99%
99.99

Nemiralisib Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

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
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 Animal Models Sprague Dawley male rats
Dosages oral:3 mg/kg; IV:1 mg/kg
Administration oral/i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03398421 Completed
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 January 17 2018 Phase 1
NCT03189589 Completed
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 June 15 2017 Phase 1
NCT02972905 Completed
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 October 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 440.54 Formula

C26H28N6O
CAS No. 1254036-71-9 SDF Download Nemiralisib SDF
Smiles CC(C)N1CCN(CC1)CC2=CN=C(O2)C3=C4C=NNC4=CC(=C3)C5=C6C=CNC6=CC=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (199.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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.

Handling Instructions

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