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LY2409881

Cat. No. M6088
LY2409881 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 160  USD160 In stock
2mg USD 80  USD80 In stock
5mg USD 120  USD120 In stock
10mg USD 200  USD200 In stock
50mg USD 680  USD680 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

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.

Customer Product Validations & Biological Datas
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.
Protocol
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.
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 485.04
Formula C24H29ClN6OS
CAS Number 946518-61-2
Purity >98.5%
Solubility DMSO 10 mg/mL
Storage at -20°C
References

[1] Deng C, et al. Clin Cancer Res. The novel IKK2 inhibitor LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-κB.

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Keywords: LY2409881 supplier, IκB/IKK, inhibitors

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