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Seletalisib (UCB5857) is a potent and selective PI3Kδ inhibitor, with IC50 of 12 nM. Seletalisib blocks human T-cell production of several cytokines from activated T-cells. Seletalisib inhibits T-cell differentiation to Th1, Th2, and Th17 subtypes. In human whole blood assays, Seletalisib inhibits CD69 expression upon B-cell activation and anti-IgE-mediated basophil degranulation. Seletalisib significantly inhibits IL-2 release following TCR stimulation in the rat.
| Cell Experiment | |
|---|---|
| Cell lines | Ramos B-cell line |
| Preparation method | Serially diluted seletalisib and goat anti-human F(ab)2 IgM in serum-free RPMI 1640 were added to Ramos cells plated in serum-free RPMI 1640. The plate was incubated for 10 minutes, chilled on ice, and the cells pelleted by centrifugation. Cellular phosphorylated AKT was detected by MSD assay. |
| Concentrations | 0.1 nM-10 μM |
| Incubation time | 10 min |
| Animal Experiment | |
|---|---|
| Animal models | Adult Lewis rats (male, 6-8 weeks of age) |
| Formulation | methylcellulose (0.5%, 400 cps) |
| Dosages | 0.1-10 mg/kg in 500 μL volume |
| Administration | oral gavage |
| Molecular Weight | 482.85 |
| Formula | C23H13ClF3N6O |
| CAS Number | 1362850-20-1 |
| Solubility (25°C) | DMSO 85 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
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