1362850-20-1
1362850-20-1 structure
- Name: Seletalisib
- Chemical Name: Seletalisib
- CAS Number: 1362850-20-1
- Molecular Formula: C23H14ClF3N6O
- Molecular Weight: 482.845
- Catalog: Research Areas Inflammation/Immunology
- Create Date: 2018-10-09 14:48:32
- Modify Date: 2024-01-03 16:04:47
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Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.
| Name | Seletalisib |
|---|---|
| Synonyms |
Seletalisib
UNII-64CW205BDD 64CW205BDD N-{(1R)-1-[8-Chloro-2-(1-oxido-3-pyridinyl)-3-quinolinyl]-2,2,2-trifluoroethyl}pyrido[3,2-d]pyrimidin-4-amine Pyrido[3,2-d]pyrimidin-4-amine, N-[(1R)-1-[8-chloro-2-(1-oxido-3-pyridinyl)-3-quinolinyl]-2,2,2-trifluoroethyl]- |
| Description | Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM. |
|---|---|
| Related Catalog | |
| Target |
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]. |
| 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]. |
| Kinase Assay | 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]. |
| Animal Admin | 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]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 710.8±60.0 °C at 760 mmHg |
| Molecular Formula | C23H14ClF3N6O |
| Molecular Weight | 482.845 |
| Flash Point | 383.7±32.9 °C |
| Exact Mass | 482.086975 |
| LogP | 2.21 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.692 |
| Storage condition | -20℃ |