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 uM for JAK2 V617F vs. 2.26 uM for WT JAK2). Similarly in the proliferation assay, LY2784544 selectively inhibited the JAK2 V617F-driven cell proliferation (IC50= 0.068 uM). Inhibition of JAK2 V617F signaling correlated well with the induction of apoptosis (EC50= 0.113 uM) in Ba/F3 cell model.
|Source||Mol Cancer Ther (2015). Figure 3. LY2784544|
|Cell Lines||MCF10A cells|
|Incubation Time||48 h|
|Results||Using the xCELLigence system to monitor cell growth in real time, LY2784544 had only a modest effect on MCF10A cells at 0.32, 0.63, and 1.25 μmol/L concentrations; however, the cell proliferation index was reduced in the CDH1-/- cells in a concentration-dependent manner.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 90 mg/mL|
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