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Seletalisib

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

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

Seletalisib

Seletalisib

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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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$52In StockIn Stock
2 mg$74In StockIn Stock
5 mg$123In StockIn Stock
10 mg$198In StockIn Stock
25 mg$347In StockIn Stock
50 mg$496In StockIn Stock
100 mg$695-In Stock
1 mL x 10 mM (in DMSO)$128In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.81%
Appearance:Solid
Color:White
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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.
SynonymsUCB5857
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/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (165.68 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 3.3 mg/mL (6.83 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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