| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| Targets |
IKK-2 (IC50 = 0.3 μM); IKK-1 (IC50 = 4 μM)
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| ln Vitro |
BMS-345541 inhibits IKK-2 and IKK-1 in dose-dependent manner. At concentrations as high as 100 M, BMS-345541 is unable to inhibit a panel of serine/threonine and tyrosine kinases. At concentrations as high as 100 μM, MS-345541 is unable to inhibit the phosphorylation of c-Jun by anisomycin, the activation of MAPKAP K2 by LPS in THP-1 cells, the phosphorylation of STAT3 by EGF in H292 cells, or the phosphorylation of c-Jun by STAT3 by anisomycin[1]. Treatment with BMS-345541 inhibits the proliferation of melanoma cells in SK-MEL-5, A375, and Hs 294T cells in a concentration-dependent manner. According to TUNEL staining and nuclear condensation, BMS-345541 (0, 100 μM) exhibits apoptotic characteristics[2].
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| ln Vivo |
BMS-345541 (10 mg/kg, p.o.) causes extended serum drug levels in mice, with concentrations maintained at or above 1 μM for several hours. When animals are challenged with an intraperitoneal dose of LPS, BMS-345541 dose-dependently reduces the production of TNFα as measured in the serum[1]. BMS-345541 effectively inhibits SK-MEL-5 tumor growth in mice at doses of 0, 10, 25, and 75 mg/kg, p.o. SK-MEL-5, A375, and Hs 294T tumor growth is effectively inhibited by treating tumor-bearing mice with 75 mg/kg of BMS-345541 by 86.2.8%, 69.11%, and 67.3.4%, respectively[2]. Both clinical and histological endpoints of inflammation and injury in mice are successfully blocked by BMS-345541 (30 and 100 mg/kg, p.o.)[3].
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| Enzyme Assay |
Assays measuring the enzyme-catalyzed phosphorylation of GST-IκBα are performed by adding enzyme (a final concentration of 0.5 μg/mL) at 30 ℃ to solutions of 100 μg/mL GST- IκBα and 5 μM [33P]ATP in 40 mM Tris HCl, pH 7.5, containing 4 mM MgCl2, 34mM sodium phosphate, 3 mM NaCl, 0.6 mM potassium phosphate, 1 mM KCl, 1 mM dithiothreitol, 3% (w/v) glycerol, and 250 μg/mL bovine serum albumin. The [33P]ATP used in the assay has a specific activity of 100 Ci/mmol. The kinase reactions are stopped after 5 minutes by adding 2× Laemmli sample buffer, which is then heated for 1 minute at 90 °C. After that, the samples are put on NuPAGE 10% BisTris gels. Gels are dried on a slab gel dryer following SDS-PAGE. The bands are then detected using a 445Si PhosphorImager, and the radioactivity is quantified using ImageQuant software. Under these conditions, the degree of phosphorylation of GST-IκBα is linear with time and concentration of enzyme. A 445Si PhosphorImager is then used to identify the bands, and ImageQuant software is used to measure the radioactivity. Under these circumstances, the rate of enzyme concentration and GST-IκBα phosphorylation are linearly related.
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| Cell Assay |
Briefly, BMS-345541 is applied to SK-MEL-5 cells at various concentrations or for various lengths of time. Trypsinization is used to collect the cells, which are then fixed in 70% ethanol for 2 hours on ice and stained with PI solution (PBS containing 2 μg/mL PI, 0.1% Triton X-100, and 125 units/mL RNase A) for 30 minutes at 37°C. Using flow cytometry and filters with 488 nm excitation and 620 nm emission, cell fluorescence is measured. The resulting data are analyzed using the software MultiCycle.
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| Animal Protocol |
BMS-345541 is created as a 2 mg/mL solution in water with 3% Tween 80. Either a peroral gavage of 10 mg/kg (1 mL/kg) or an intravenous bolus of 2 mg/kg (1 mL/kg) is administered to the mice. Individual mice are given whole blood samples at 0, 0.05, 0.25, 0.5, 1.0, 3.0, 6.0, and 8.0 h after dosing by means of an orbital bleed and a cardiac puncture. Centrifuging whole blood for five minutes at 20×103 g. Before being analyzed, serum is kept at 20°C.
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| References |
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| Molecular Formula |
C₁₄H₁₈CLN₅
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|---|---|
| Molecular Weight |
291.78
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| Exact Mass |
291.12507 Molecular Weight
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| Elemental Analysis |
C, 57.63; H, 6.22; Cl, 12.15; N, 24.00
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| CAS # |
547757-23-3
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| Related CAS # |
445430-58-0;547757-23-3 (HCl);445430-59-1 (2HCl);2320261-79-6 (TFA);
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| Appearance |
Solid powder
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| SMILES |
CC1=CC2=C(C=C1)N=C(C3=NC=C(N23)C)NCCN.Cl
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| InChi Key |
MIDKPVLYXNLFGZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H17N5.ClH/c1-9-3-4-11-12(7-9)19-10(2)8-17-14(19)13(18-11)16-6-5-15;/h3-4,7-8H,5-6,15H2,1-2H3,(H,16,18);1H
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| Chemical Name |
N'-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine;hydrochloride
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| Synonyms |
UNII-BXU277OCN5; BMS345541; BMS 345541; BMS-345541
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ~50 mg/mL (~171.4 mM)
DMSO: ~20 mg/mL (~68.5 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2 mg/mL (6.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4272 mL | 17.1362 mL | 34.2724 mL | |
| 5 mM | 0.6854 mL | 3.4272 mL | 6.8545 mL | |
| 10 mM | 0.3427 mL | 1.7136 mL | 3.4272 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.
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