LY2409881CAS# 946518-60-1 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 946518-60-1 | SDF | Download SDF |
| PubChem ID | 68856073 | Appearance | Powder |
| Formula | C24H32Cl4N6OS | M.Wt | 594.43 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO | ||
| Chemical Name | 2-[5-chloro-2-[3-(4-methylpiperazin-1-yl)propylamino]pyrimidin-4-yl]-N-cyclopropyl-1-benzothiophene-4-carboxamide;trihydrochloride | ||
| SMILES | CN1CCN(CC1)CCCNC2=NC=C(C(=N2)C3=CC4=C(C=CC=C4S3)C(=O)NC5CC5)Cl.Cl.Cl.Cl | ||
| Standard InChIKey | IEXCRLAGBWKVPW-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C24H29ClN6OS.3ClH/c1-30-10-12-31(13-11-30)9-3-8-26-24-27-15-19(25)22(29-24)21-14-18-17(4-2-5-20(18)33-21)23(32)28-16-6-7-16;;;/h2,4-5,14-16H,3,6-13H2,1H3,(H,28,32)(H,26,27,29);3*1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
LY2409881 Dilution Calculator
LY2409881 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.6823 mL | 8.4114 mL | 16.8228 mL | 33.6457 mL | 42.0571 mL |
| 5 mM | 0.3365 mL | 1.6823 mL | 3.3646 mL | 6.7291 mL | 8.4114 mL |
| 10 mM | 0.1682 mL | 0.8411 mL | 1.6823 mL | 3.3646 mL | 4.2057 mL |
| 50 mM | 0.0336 mL | 0.1682 mL | 0.3365 mL | 0.6729 mL | 0.8411 mL |
| 100 mM | 0.0168 mL | 0.0841 mL | 0.1682 mL | 0.3365 mL | 0.4206 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases.
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The novel IKK2 inhibitor LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-kappaB.[Pubmed:25355930]
Clin Cancer Res. 2015 Jan 1;21(1):134-45.
PURPOSE: To evaluate the pharmacologic activity of a novel inhibitor of IkappaB kinase beta (IKK2), LY2409881, in preclinical models of B- and T-cell lymphoma, as a single agent and in combination with histone deacetylase (HDAC) inhibitors. EXPERIMENTAL DESIGN: The in vitro activity of LY2409881 was determined using an ATP-based growth inhibition assay and flow cytometric assay of apoptosis in lymphoma cell lines. The in vivo activity of LY2409881 was determined using SCID-beige xenograft mouse model. The mechanism of action was determined using immunoblotting, immuofluorescence, and electrophoretic mobility shift assay. Synergy of LY2409881 with other drugs active in lymphoma was determined by calculating relative risk ratio (RRR) and combination index (CI). RESULTS: LY2409881 inhibited constitutively activated NF-kappaB, and caused concentration- and time-dependent growth inhibition and apoptosis in lymphoma cells. In models of diffuse large B-cell lymphoma (DLBCL), the cytotoxicity of LY2409881 correlated with the overall activation status of NF-kappaB, but not simply in a pattern predicted by the cell-of-origin classification of these cell lines. 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-kappaB subunit p65 in lymphoma cells treated by the HDAC inhibitor romidepsin, underlying a potential mechanism of the marked synergy observed of these two drugs. CONCLUSION: Collectively, these data strongly suggest that targeting the NF-kappaB pathway in combination with romidepsin could represent a novel and potent regimen for the treatment of B- and T-cell lymphoma.
