LY2228820 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.
|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 20 mg/mL
Water 100 mg/mL
|Source||Oncotarget (2016). Figure 3. LY2228820|
|Cell Lines||MDA-MB-231 cells|
|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|
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