Seletalisib

SKU: orb1296248

Description

Seletalisib (UCB5857) is a highly selective PI3Kδ inhibitor with an IC50 of 12 nM. It is a valuable research tool for studying B-cell and immune cell signaling in vitro and has demonstrated efficacy in models of inflammatory and autoimmune diseases in vivo.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1362850-20-1
• MW: 482.85
• Purity: 99.81% (May vary between batches)
• Formula: C₂₃H₁₄ClF₃N₆O
• SMILES: [O-][n+]1cccc(c1)-c1nc2c(Cl)cccc2cc1[C@@H](Nc1ncnc2cccnc12)C(F)(F)F
• Target: PI3K
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (6.83 mM);DMSO:80 mg/mL (165.68 mM)

Bioactivity

• Target IC50:
  PI3Kδ:12 nM
• In Vivo:
  Seletalisib markedly reduces IL-2 release in response to TCR stimulation in rats, achieving near-total suppression at doses ≥1 mg/kg. This compound demonstrates strong in vivo activity, with an estimated IC50 value of <10 nM across all tested concentrations.
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• In Vitro:
  Seletalisib is able to block AKT phosphorylation following activation of the BCR in a B-cell line. No indications of cytotoxicity are observed in PBMCs or other cell types treated with Seletalisib. Seletalisib blocks human T-cell production of several cytokines from activated T-cells. Seletalisib inhibits T-cell differentiation to Th1, Th2, and Th17 subtypes. Additionally, Seletalisib inhibits B-cell proliferation and cytokine release. In human whole blood assays, Seletalisib inhibits CD69 expression upon B-cell activation and anti-IgE-mediated basophil degranulation.
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• Cell Research:
  Seletalisib is dissolved 1 mM solution in DMSO, and tested in a concentration-response, to explore the effects of PI3Kδ-specific inhibition compared with complete inhibition of class I PI3K signaling. In addition, seletalisib is tested in the BioMap BT cell system at concentrations of 1000, 100, 10, and 1 nM. An activity profile is generated based on the effect of the compounds on the levels of cellular readouts, including cytokines, growth factors, adhesion molecules, and proliferation endpoints.
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• Animal Research:
  Rats are dosed with Seletalisib (0.1-10 mg/kg in 500 μL volume) or vehicle via oral gavage 30 min prior to i.v. administration of anti- CD3 antibody administered in a 200 μL dose volume. The vehicle is methylcellulose or saline for oral and i.v. administration, respectively. Seletalisib levels and IL-2 levels are measured.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, PI3K, PI3Kδ, Phosphoinositide 3-kinase, Seletalisib, UCB5857, UCB-5857, UCB 5857

Compound Identifiers

PubChem CID

56928390