PRN371 is a novel potent, selective JAK3 inhibitor with IC50 of 0.5 nM, displays >250-fold selectivity over JAK1, JAK2, and TYK2.
PRN371 effectively inhibits IL-2 induces JAK1/3-STAT5 phosphorylation in PBMCs with IC50 of 99 nM, effectively blocks JAK3-mediated signaling in JAK3-driven cancer cells.
PRN371 effectively inhibits the growth of NKTL cells via suppressing the JAK3-STAT pathway, and exhibits a more durable inhibition on JAK3 compared to tofacitinib in vitro.
PRN371 significantly inhibits tumor growth in NKTL xenograft model harboring JAK3 activating mutation.
