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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $40 | In Stock | |
2 mg | $56 | In Stock | |
5 mg | $91 | In Stock | |
10 mg | $147 | In Stock | |
25 mg | $297 | In Stock | |
50 mg | $476 | In Stock | |
1 mL x 10 mM (in DMSO) | $100 | In Stock |
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), PI3Kβ:5.8 (pic50), PI3Kγ:5.2 (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] |
Alias | GSK2269557 |
Molecular Weight | 440.54 |
Formula | C26H28N6O |
Cas No. | 1254036-71-9 |
Smiles | CC(C)N1CCN(Cc2cnc(o2)-c2cc(cc3[nH]ncc23)-c2cccc3[nH]ccc23)CC1 |
Relative Density. | 1.281 g/cm3 (Predicted) |
Storage | store 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
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