Catalog No.: PC-38789Not For Human Use, Lab Use Only.
LL-00071210 is a potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 values of 24.6 nM and 9.4 nM in biochemical and cellular assays, respectively.
LL-00071210 is a potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 values of 24.6 nM and 9.4 nM in biochemical and cellular assays, respectively.
LL-00071210 demonstrated specific inhibitory action against PI3Kδ isoform with >100-fold selectivity over closely related PI3Kγ isoform.
LL-00071210 potently inhibited IL2 (A), TNF-α (B) and IFN-γ (C) secretion from human PBMC's on stimulation with anti-CD3/CD28.
LL-00071210 showed acceptable pharmacokinetic profile with good oral bioavailability in rodents.
In rodent arthritis model, treatment with LL-00071210 led to dosedependent inhibition of disease severity, along with histopathological
improvements in joint structure.
LL-00071210 also demonstrated good combination potential with methotrexate at sub-therapeutic doses.
