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Seletalisib

Cat. No. M10157
Seletalisib Structure
Synonym:

UCB5857

Size Price Availability Quantity
5mg USD 200  USD200 In stock
10mg USD 320  USD320 In stock
25mg USD 600  USD600 In stock
50mg USD 1020  USD1020 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Rodger A Allen, et al. J Pharmacol Exp Ther. Seletalisib: Characterization of a Novel, Potent, and Selective Inhibitor of PI3K δ

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Keywords: Seletalisib, UCB5857 supplier, PI3K, inhibitors, activators


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