Nemiralisib

SKU: orb1707242

Description

Nemiralisib

Research Area

Signal Transduction

Key Properties

• CAS Number: 1254036-71-9
• MW: 440.54
• Purity: 99.91%
• Formula: C₂₆H₂₈N₆O
• SMILES: CC(C)N1CCN(Cc2cnc(o2)-c2cc(cc3[nH]ncc23)-c2cccc3[nH]ccc23)CC1
• Target: PI3K
• Solubility: DMSO:29 mg/mL (65.83 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.54 mM)

Bioactivity

• Target IC50:
  PI3Kα:5.3 (pic50)|PI3Kβ:5.8 (pic50)|PI3Kγ:5.2 (pic50)|PI3Kδ:9.9 (pki)
• 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).
• 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).

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Nemiralisib, GSK 2269557, GSK2269557, GSK-2269557, PI3Kδ, PI3Kγ, PI3Kβ, PI3Kα

Compound Identifiers

PubChem CID

49784002