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Nemiralisib

Nemiralisib
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Purity:99.91%
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Nemiralisib

Catalog No. T15431Cas No. 1254036-71-9
Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease.
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Pack SizePriceAvailabilityQuantity
1 mg$40In Stock
2 mg$56In Stock
5 mg$91In Stock
10 mg$147In Stock
25 mg$297In Stock
50 mg$476In Stock
1 mL x 10 mM (in DMSO)$100In Stock
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Product Introduction

Bioactivity
Description
Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease.
Targets&IC50
PI3Kδ:9.9 (pki), PI3Kγ:5.2 (pic50), PI3Kβ:5.8 (pic50), PI3Kα:5.3 (pic50)
In vitro
Nemiralisib inhibits IFNγ in the peripheral blood mononuclear (PBMC) (pIC50: 9.7). Nemiralisib is highly selective for PI3Kδ. It has >1000-fold selectivity over the closely related isoforms PI3Kα (pIC50: 5.3), PI3Kβ (pIC50: 5.8), and PI3Kγ (pIC50: 5.2).[1]
In vivo
Nemiralisib is active in a disease-relevant brown Norway rat acute OVA model of Type 2 helper T-cells (Th2)-driven lung inflammation. Pharmacokinetic data from Sprague Dawley male rats are obtained to assess the suitability of the series for inhaled delivery clearance data in rat microsomes and subsequently in vivo. Compounds (e.g., Nemiralisib) are administered by the oral or intravenous routes, at a dose level of 3 and 1mg/kg respectively (n=2 rats/route).[1]
AliasGSK2269557 (free base), GSK2269557
Chemical Properties
Molecular Weight440.54
FormulaC26H28N6O
Cas No.1254036-71-9
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 29 mg/mL (65.83 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2699 mL11.3497 mL22.6994 mL113.4971 mL
5 mM0.4540 mL2.2699 mL4.5399 mL22.6994 mL
10 mM0.2270 mL1.1350 mL2.2699 mL11.3497 mL
20 mM0.1135 mL0.5675 mL1.1350 mL5.6749 mL
50 mM0.0454 mL0.2270 mL0.4540 mL2.2699 mL

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