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Ralimetinib dimesylate (LY2228820 dimesylate) is a novel and potent p38MAPK inhibitor. In vitro kinase enzyme activity showed that the IC50 for p38αMAPK and p38βMAPK of LY2228820 were 7 nM and 3 nM, respectively. Phosphorylation of MAPKAPK2 and/or HSP27, down stream targets of p38MAPK, was significantly inhibited by LY in both MM cell lines and LT-BMSCs.
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Source | Oncotarget (2016). Figure 3. LY2228820 |
| Method | colony assays | |
| Cell Lines | MDA-MB-231 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 72 h | |
| Results | The triple combination significantly retarded shortterm proliferation of MDA-MB-231 cells compared to vehicle and single drug controls (p<0.001), as well as the two-agent combinations |
| Molecular Weight | 612.74 |
| Formula | C24H29FN6.2CH4O3S |
| CAS Number | 862507-23-1 |
| Solubility (25°C) | DMSO 30 mg/mL Water 33 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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