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Seletalisib

Cat. No. M10157
Seletalisib Structure
Synonym:

UCB5857

Size Price Availability
5mg USD 278  USD278 4-7 Days
10mg USD 408  USD408 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 482.85
Formula C23H13ClF3N6O
CAS Number 1362850-20-1
Purity >99%
Solubility DMSO 85 mg/mL
Storage at -20°C
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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  Catalog
Abmole Inhibitor Catalog




Keywords: Seletalisib, UCB5857 supplier, PI3K, inhibitors

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