Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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Targets |
IKK2 30 nM (IC50)
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ln Vitro |
LY2409881 is an IKK2 inhibitor that prevents NF-κB from being activated by TNFα. LY2409881 has a 30 nM IC50 and potently inhibits IKK2 according to an in vitro kinase test. Conversely, IKK1 and other widely used kinases have an IC50 that is at least one log greater. Using a cell-based experiment, the effect of LY2409881 on TNFα-dependent antiapoptosis activity is investigated in order to better investigate the specificity of LY2409881 for NF-κB signaling. One well-studied upstream stimulation of NF-κB is TNFα. While TNFα at 10 ng/mL has no cytotoxicity against the ovarian cancer cell line SKOV3, LY2409881 exhibits considerable cytotoxicity. On the other hand, compared to LY2409881 alone, coadministration of TNFα plus LY2409881 causes a notably greater amount of cell death. This is because LY2409881 blocks the TNFα-dependent activation of antiapoptotic signals mediated by NF-κB, but does not alter the proapoptotic TNF receptor-associated death domain (TRADD) and FAS-associated death domain (FADD) cascade pathways activated by TNFα[1].
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ln Vivo |
The in vivo activity of LY2409881 is verified using a reputable DLBCL xenograft model. Intraperitoneal injections of LY2409881 at three different doses (50, 100, and 200 mg/kg) are administered twice a week to SCID-beige mice implanted with tumors produced from LY10 cells. The mice show no significant morbidity or mortality as a result of the well-tolerated therapies. A time-dependent graph of each treatment group's average tumor volume is presented. All treatment groups exhibit considerably reduced tumor volume growth rates (P≤0.01) compared to the untreated control group.
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References |
[1]. Deng C, et al. The novel IKK2 inhibitor LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-κB. Clin Cancer Res. 2015 Jan 1;21(1):134-45
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Molecular Formula |
C24H29CLN6OS
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Molecular Weight |
485.04
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CAS # |
946518-61-2
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Related CAS # |
LY2409881 trihydrochloride;946518-60-1
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Solubility (In Vitro) |
DMSO :≥ 37 mg/mL (~76.28 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0617 mL | 10.3084 mL | 20.6169 mL | |
5 mM | 0.4123 mL | 2.0617 mL | 4.1234 mL | |
10 mM | 0.2062 mL | 1.0308 mL | 2.0617 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.