product name LY2409881
Description: LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, and with >10-fold selectivity over IKK1 and other common kinases. LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-κB. LY2409881 inhibited constitutively activated NF-κB, and caused concentration- and time-dependent growth inhibition and apoptosis in lymphoma cells.
References: Clin Cancer Res. 2015 Jan 1;21(1):134-45.
594.43
Formula
C24H32Cl4N6OS
CAS No.
946518-60-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (33.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: LY2409881 inhibits constitutively activated NF-ƘB, and causes concentration- and time-dependent growth inhibition and apoptosis in diffuse large B-cell lymphoma (DLBCL) cells. In the ovarian cancer cell line SKOV3, LY2409881 demonstrates moderate cytotoxicity. LY2409881 is synergistic with doxorubicin and cyclophosphamide in SUDHL2 cell in inhibiting the cell growth, but not in LY1 cell. In both SUDHL2 and LY1 cells, LY2409881 is synergistic with the histone deacetylase (HDAC) inhibitor romidepsin in inhibiting the cell growth. Kinase Assay: Cell Assay: Cytotoxicity is evaluated using the CellTiter-Glo Reagent according to the manufacturers manual. Experiments are carried out in 96-well plates, with each treatment in triplicate. Samples are taken at typically 24, 48, and 72 hours after treatment. Cytotoxicity is expressed by the decreasing percentage of live cells in each treatment relative to the untreated control from the same experiment. IC50 for each cell line is calculated using the CalcuSyn Version 2.0 software. |
|---|---|
| In Vivo | In SCID-beige xenograft mouse model, LY2409881 (50, 100, and 200 mg/kg, i.p.) significantly inhibits the tumor growth |
| Animal model | In SCID-beige mice bearing LY10 cell-derived tumors |
| Formulation & Dosage | 50, 100 and 200 mg/kg |
| References | Clin Cancer Res. 2015 Jan 1;21(1):134-45 |
