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Gandotinib (LY2784544) is a small molecule selective mutant JAK2 kinase inhibitor with an IC50 of 68 nM. In the in vitro tests using Ba/F3 cells expressing either wild type or V617F mutant JAK2, Gandotinib (LY2784544) 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, Gandotinib (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.
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Source | Mol Cancer Ther (2015). Figure 3. LY2784544 |
| Method | Viral knockdown | |
| Cell Lines | MCF10A cells | |
| Concentrations | 1.25 μmol/L | |
| 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. |
| Molecular Weight | 469.94 |
| Formula | C23H25ClFN7O |
| CAS Number | 1229236-86-5 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Constantine S Tam, et al. Investigational Janus kinase inhibitors
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