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Seletalisib

🥰Excellent
Catalog No. TQ0044Cas No. 1362850-20-1
Alias UCB5857

Seletalisib (UCB5857) (UCB5857) is a potent and specific PI3Kδ inhibitor (IC50: 12 nM).

Seletalisib

Seletalisib

🥰Excellent
Purity: 99.81%
Catalog No. TQ0044Alias UCB5857Cas No. 1362850-20-1
Seletalisib (UCB5857) (UCB5857) is a potent and specific PI3Kδ inhibitor (IC50: 12 nM).
Pack SizePriceAvailabilityQuantity
1 mg$52In Stock
2 mg$74In Stock
5 mg$123In Stock
10 mg$198In Stock
25 mg$347In Stock
50 mg$496In Stock
100 mg$695In Stock
1 mL x 10 mM (in DMSO)$128In Stock
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Purity:99.81%
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Product Introduction

Bioactivity
Description
Seletalisib (UCB5857) (UCB5857) is a potent and specific PI3Kδ inhibitor (IC50: 12 nM).
Targets&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.
Cell Research
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.
Animal Research
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.
AliasUCB5857
Chemical Properties
Molecular Weight482.85
FormulaC23H14ClF3N6O
Cas No.1362850-20-1
Smiles[O-][n+]1cccc(c1)-c1nc2c(Cl)cccc2cc1[C@@H](Nc1ncnc2cccnc12)C(F)(F)F
Relative Density.1.53 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 80 mg/mL (165.69 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0710 mL10.3552 mL20.7104 mL103.5518 mL
5 mM0.4142 mL2.0710 mL4.1421 mL20.7104 mL
10 mM0.2071 mL1.0355 mL2.0710 mL10.3552 mL
20 mM0.1036 mL0.5178 mL1.0355 mL5.1776 mL
50 mM0.0414 mL0.2071 mL0.4142 mL2.0710 mL
100 mM0.0207 mL0.1036 mL0.2071 mL1.0355 mL

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