Catalog No.: PC-43343Not For Human Use, Lab Use Only.
LY2784544 (Gandotinib) is a potent, selective and ATP-competitive inhibitor of JAK2 V617F, effectively inhibits JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55 nM, respectively).
LY2784544 (Gandotinib) is a potent, selective and ATP-competitive inhibitor of JAK2 V617F, effectively inhibits JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55 nM, respectively).
LY2784544 inhibits JAK2 and JAK3 in biochemical assays with IC50 of 3 nM and 48 nM, respectively.
LY2784544 is much less potent at inhibiting IL-3-stimulated wild-type JAK2-mediated signaling and cell proliferation (IC50=1183 and 1309 nM, respectively).
LY2784544 effectively inhibits STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP ascitic tumor cells (TED50=12.7 mg/kg) and significantly reduces Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model.
LY2784544 also is a potent GPR39 agonist with pEC50 of 9.36 (at 316 uM ZnCl2).
