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 | |
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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 | |
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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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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