2. PI3K/Akt/mTOR
  3. PI3K
  4. Seletalisib

Seletalisib  (Synonyms: UCB5857)

Cat. No.: HY-16754 Purity: 98.88%
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Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.

For research use only. We do not sell to patients.

Seletalisib Chemical Structure

Seletalisib Chemical Structure

CAS No. : 1362850-20-1

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 159 In-stock
Solution
10 mM * 1 mL in DMSO USD 159 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 420 In-stock
50 mg USD 600 In-stock
100 mg USD 840 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Seletalisib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Seletalisib

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.

IC50 & Target[1]

PI3Kδ

12 nM (IC50)

In Vitro

Seletalisib is a potent, ATP-competitive and highly selective PI3Kδ inhibitor able to block AKT phosphorylation following activation of the BCR in a B-cell line. Seletalisib inhibits N-formyl peptides (fMLP)-stimulated but not phorbol myristate acetate (PMA)-stimulated superoxide release from human neutrophils consistent with a PI3Kδ-specific activity. 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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Seletalisib Related Antibodies
In Vivo

Seletalisib significantly inhibits IL-2 release following TCR stimulation in the rat. The inhibition is observed at all tested doses of seletalisib with almost complete inhibition reached at dose levels ≥1 mg/kg. Seletalisib has potent in vivo effects with an estimated IC50 value of <10 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

482.85

Formula

C23H14ClF3N6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)[C@H](NC1=C2C(C=CC=N2)=NC=N1)C3=CC4=CC=CC(Cl)=C4N=C3C5=CC=C[N+]([O-])=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.3 mg/mL (172.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0710 mL 10.3552 mL 20.7104 mL
5 mM 0.4142 mL 2.0710 mL 4.1421 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

Seletalisib is dissolved 1 mM solution in DMSO, and tested in a concentration response (seletalisib), 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats: 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0710 mL 10.3552 mL 20.7104 mL 51.7759 mL
5 mM 0.4142 mL 2.0710 mL 4.1421 mL 10.3552 mL
10 mM 0.2071 mL 1.0355 mL 2.0710 mL 5.1776 mL
15 mM 0.1381 mL 0.6903 mL 1.3807 mL 3.4517 mL
20 mM 0.1036 mL 0.5178 mL 1.0355 mL 2.5888 mL
25 mM 0.0828 mL 0.4142 mL 0.8284 mL 2.0710 mL
30 mM 0.0690 mL 0.3452 mL 0.6903 mL 1.7259 mL
40 mM 0.0518 mL 0.2589 mL 0.5178 mL 1.2944 mL
50 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0355 mL
60 mM 0.0345 mL 0.1726 mL 0.3452 mL 0.8629 mL
80 mM 0.0259 mL 0.1294 mL 0.2589 mL 0.6472 mL
100 mM 0.0207 mL 0.1036 mL 0.2071 mL 0.5178 mL
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Seletalisib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Seletalisib1362850-20-1UCB5857UCB 5857UCB-5857PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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