Biochem/physiol Actions

AS1517499 is a potent STAT6 (signal transducer and activator of transcription 6) inhibitor (IC₅₀ = 21 nM against IL-4-dependent reporter activity) that selectively prevents anti-CD3- & IL-4-induced T-helper cell 2 (Th2) differentiation of mouse spleen T cells (IC₅₀ = 2.3 nM), without affecting anti-CD3- & IL-12-induced Th1 differentiation. AS1517499 in vivo effecicacy is demonstrated in various animal models of immunological disorders, including the autoimmune Graves’; disease, antigen-induced bronchial hypercontractility (10 mg/kg i.p.). AS1517499 treatment (10 mg/kg/day i.p.) following early gliomagenesis blockage by a CSF-1R inhibitor is also shown to greatly prolong the survival rate when compared with CSF-1R inhibition alone in a murine model of PDGF-driven glioma (PDG).

AS1517499 moderately inhibits the expression of RhoA (ras homolog family member A). Overexpression of RhoA protein is associated with allergic bronchial asthma.

Packaging

5, 25 mg in glass bottle