Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Seletalisib (UCB5857) (UCB5857) is a potent and specific PI3Kδ inhibitor (IC50: 12 nM).
説明 | Seletalisib (UCB5857) (UCB5857) is a potent and specific PI3Kδ inhibitor (IC50: 12 nM). |
ターゲット&IC50 | PI3Kδ:12 nM |
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. |
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. |
細胞研究 | 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. |
動物実験 | 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. |
別名 | UCB5857 |
分子量 | 482.85 |
分子式 | C23H14ClF3N6O |
CAS No. | 1362850-20-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 80 mg/mL (165.69 mM)
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Seletalisib 1362850-20-1 PI3K/Akt/mTOR signaling PI3K Inhibitor Phosphoinositide 3-kinase UCB5857 inhibit UCB-5857 UCB 5857 inhibitor