LY2409881 trihydrochloride is a potent and selective IKK2 inhibitor with IC50 of 30 nM. LY2409881 trihydrochloride 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 trihydrochloride is synergistic with doxorubicin and cyclophosphamide in SUDHL2 cell in inhibiting the cell growth, but not in LY1 cell.
In vivo, LY2409881 (50, 100, and 200 mg/kg, i.p.) signiﬁcantly inhibits the tumor growth in SCID-beige xenograft mouse model.
|Cell lines||OCI-LY10 cells|
|Preparation method||Cytotoxicity is evaluated using the CellTiter-Glo Reagent according to the manufacturer's 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.|
|Incubation time||~72 h|
|Animal models||Five- to 7-week-old SCID beige mice|
|Formulation||5% dextrose in water|
|Dosages||50, 100, 200 mg/kg on day 1 and 4 of every week for 4 weeks|
|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: ≥ 16 mg/mL warmed|
The novel IKK2 inhibitor LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-κB.
Deng C, et al. Clin Cancer Res. 2015 Jan 1;21(1):134-45. PMID: 25355930.
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