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In vitro: Y2409881 inhibited constitutively activated NF-κB, and caused concentration- and time-dependent growth inhibition and apoptosis in lymphoma cells. Pretreatment of LY10 with 10 umol/L of LY2409881 prevented the formation of phosphorylated IkB in samples treated with TNFa for 2, 20, and 60 minutes in the presence of abundant IkB protein.
In vivo: LY2409881 was safe to mice at three dose levels, 50, 100, and 200 mg/kg, all of which caused significant inhibition of tumor growth. LY2409881 suppressed the activity of the NF-κB subunit p65 in lymphoma cells treated by the HDAC inhibitor romidepsin, underlying a potential mechanism of the marked synergy observed of these two drugs.
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Source | Clin Cancer Res (2015). Figure 2. LY2409881 |
| Method | Vybrant Apoptosis Assay | |
| Cell Lines | SUDHL2 cells | |
| Concentrations | 10 and 20 μmol/L | |
| Incubation Time | 24 h | |
| Results | These results confirm that LY2409881 inhibits constitutively activated NF-κB, leading to cell death in B- and T-cell lymphoma cell lines. |
| Cell Experiment | |
|---|---|
| Cell lines | DLBCL cell line |
| Preparation method | After incubation with LY2409881for 4 hours, the samples were placed on the slides using the Cytospin. After fixation in 10% formalin and 100% methanol, the slides were transferred to the blocking buffer (10% nonfat dry milk) and incubated with primary antibody in the humidity chamber overnight. |
| Concentrations | 10 μmol/L |
| Incubation time | 4 h |
| Animal Experiment | |
|---|---|
| Animal models | SCID beige mice |
| Formulation | 5% dextrose in wate |
| Dosages | 50 mg/kg, 100 mg/kg, 200 mg/kg |
| Administration | i.v. |
| Molecular Weight | 485.04 |
| Formula | C24H29ClN6OS |
| CAS Number | 946518-61-2 |
| Solubility (25°C) | DMSO 10 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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