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Chemical Structure| 1362850-20-1 Chemical Structure| 1362850-20-1

Structure of Seletalisib
CAS No.: 1362850-20-1

Chemical Structure| 1362850-20-1

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Seletalisib is a potent and selective PI3 kinase inhibitor, which may be useful for the treatment of immune-inflammatory diseases, such as psoriasis amd primary Sjogren's syndrome.

Synonyms: UCB5857

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Product Details of Seletalisib

CAS No. :1362850-20-1
Formula : C23H14ClF3N6O
M.W : 482.85
SMILES Code : FC(F)(F)[C@@H](C1=CC2=CC=CC(Cl)=C2N=C1C3=C[N+]([O-])=CC=C3)NC4=C5C(C=CC=N5)=NC=N4
Synonyms :
UCB5857
MDL No. :MFCD28963973
InChI Key :LNLJHGXOFYUARS-OAQYLSRUSA-N
Pubchem ID :56928390

Safety of Seletalisib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of Seletalisib

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, IC50:282 nM

  • p110δ

    PI3Kδ, IC50:12 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human keratinocytes 1 µM 1-hour pretreatment followed by stimulation for 6-24 hours To evaluate the impact of seletalisib on PI3K-dependent pathways activated by IL-22 and TNF-α in human keratinocytes. Results showed that seletalisib inhibited PI3Kδ activity, significantly reducing PDK1 phosphorylation and inhibiting AKT Thr308 and Ser473 phosphorylation at 6 and 24 hours post IL-22 stimulation. Additionally, seletalisib completely abrogated S6 phosphorylation, not only in IL-22-treated cells but also in untreated cells, suggesting a role for PI3Kδ in cellular homeostasis. Cells. 2021 Oct 2;10(10):2636
MDA PCa 2b cells 0-100 µM 48 hours Evaluate the effect of Seletalisib on MDA PCa 2b cell viability, showing an IC50 value of 53.1 μM Cancers (Basel). 2023 Feb 20;15(4):1337.
LNCaP cells 0-100 µM 48 hours Evaluate the effect of Seletalisib on LNCaP cell viability, showing an IC50 value of 3.7 μM Cancers (Basel). 2023 Feb 20;15(4):1337.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/cJ mice Imiquimod-induced psoriasis-like dermatitis model Topical administration 1 mM Once daily for 5 days To evaluate the therapeutic effects of seletalisib in the imiquimod-induced psoriasis-like dermatitis model. Results showed that seletalisib ameliorated the histological psoriasiform manifestations, with a reduction of ~50% in acanthosis and consequent scale thickness, and a substantial decrease in inflammatory cell infiltration (~35% reduction). Additionally, seletalisib reduced the expression of PI3Kδ and phosphorylation of AKT Thr308 and Ser473. Cells. 2021 Oct 2;10(10):2636
C57BL/6 mice Adenovirus-induced sialoadenitis model Oral gavage 10 mg/kg Once daily, starting from day 0, 3, 5, or 8 To evaluate the effect of Seletalisib on lymphocyte infiltration and autoantibody production in a sialoadenitis model. Results showed that Seletalisib significantly reduced the numbers of CD45+, CD3+, and CD19+ cells, decreased autoantibody production, and improved saliva flow. Ann Rheum Dis. 2019 Feb;78(2):249-260

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.36mL

2.07mL

1.04mL

20.71mL

4.14mL

2.07mL

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