Seletalisib Inhibitor

Solid. Powder

99.81%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

482.85

DMSO: 80mg/mL (165.69mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

C23H13ClF3N6O

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

1362850-20-1

Seletalisib is dissolved 1mM solution in DMSO, and tested in a concentration-response, to explore the effects of PI3Kdelta-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 1nM. 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.

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.

PI3K/Akt/mTOR signaling; PI3K