LY2784544 英文名称: LY2784544 |
型号:null 产品货号: S2179 |
价格:请致电:010-57128832,18610462672 |
品牌: 美国 试剂级别: 超纯级 |
LY2784544 is a small molecule selective mutant JAK2 kinase inhibitor with an IC50 of 68 nM. The antiproliferative activity of LY2784544 and its ability to induce apoptosis were examined by Celltiter-Glo Cell Viability and Caspase-Glo 3/7 Apoptosis Assays, respectively. In the in vitro tests using Ba/F3 cells expressing either wild type or V617F mutant JAK2, it potently inhibited the JAK2 V617F-STAT5 signaling at a concentration that was 41-fold lower than that required to inhibit IL-3-activated wild type JAK2-STAT5 signaling (IC50 = 0.055 µM for JAK2 V617F vs. 2.26 µM for WT JAK2). Similarly in the proliferation assay, LY2784544 selectively inhibited the JAK2 V617F-driven cell proliferation (IC50= 0.068 µM). Inhibition of JAK2 V617F signaling correlated well with the induction of apoptosis (EC50= 0.113 µM) in Ba/F3 cell model. |