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LY2409881 trihydrochloride

Cat. No. M8961
LY2409881 trihydrochloride Structure
Size Price Availability Quantity
5mg USD 130 In stock
10mg USD 215 In stock
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Quality Control
  • Current batch:
  • Purity >97%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
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.
Concentrations 25 μM
Incubation time ~72 h
Animal Experiment
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
Administration administered intraperitoneally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 594.43
Formula C24H32Cl4N6OS
CAS Number 946518-60-1
Purity >97%
Solubility DMSO: ≥ 16 mg/mL warmed
Storage at -20°C
References

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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  Catalog
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Keywords: LY2409881 trihydrochloride supplier, IκB/IKK, inhibitors

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