Gandotinib, also known as LY2784544, is a potent and selective JAK inhibitor. LY2784544 in vitro selectivity for JAK2 was found to be equal or superior to known JAK2 inhibitors. LY2784544 effectively inhibited JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55 nM, respectively). In vivo, LY2784544 effectively inhibited STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP ascitic tumor cells (TED50=12.7 mg/kg) and significantly reduced (P<0.05) Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model (TED50=13.7 mg/kg, twice daily).
JAK Inhibitors Related Products:
Ruxolitinib; Ruxolitinib phosphate; Tofacitinib; AZD1480; Momelotinib; AZ960; Pacritinib; XL019; Upadacitinib; Decernotinib; Filgotinib; GLPG0634 analogue; FLLL32; AG-490 (Tyrphostin B42); NSC-42834; Itacitinib; Go6976; Baricitinib; Oclacitinib; Oclacitinib maleate; WP1066