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Purity: ≥98%
BAY-61-3606 2HCl (BAY 61-3606, BAY 61-3606 dihydrochloride), cell-permeable imidazopyrimidine compound, is a potent and selective, oral, ATP-competitive, reversible inhibitor of Syk (Spleen tyrosine kinase) tyrosine kinase with immunomodulatory effects. It inhibits Syk with a Ki of 7.5 nM. It shows no inhibitory effect on Btk, Fyn, Itk, Lyn, and Src kinases. It has been demonstrated that BAY 61-3606 inhibits Syk-mediated cellular functions, including the inhibition of high glucose-tyrosine phosphorylation of I kappa B α and nuclear translocation of p65. BAY 61-3606 has inhibited degranulation, lipid mediation, and cytokine synthesis in mast cells. Moreover, BAY 61-3606 inhibited the activation of monocytes and eosinophils by B cells and Fc receptors.
| Targets |
Syk (Ki = 7.5 nM); Syk (IC50 = 10 nM)
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| ln Vitro |
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| Enzyme Assay |
In mast cells, BAY 61-3606 inhibited lipid mediator and cytokine synthesis in addition to degranulation (IC50 values ranging from 5 to 46 nM). In basophils taken from healthy human subjects, BAY 61-3606 was very effective (IC50 = 10 nM), and it appears to be at least as potent (IC50 = 8.1 nM) in basophils taken from atopic (high serum IgE) subjects. BAY 61-3606 was also found to potently suppress B cell receptor activation as well as receptors for the Fc portion of IgG signaling in eosinophils and monocytes. In colorectal cancer cells expressing mutant forms of K-RAS, but not in isogenic cells expressing wild-type K-RAS, we found that BAY61-3606 inhibits the proliferation of these cells. Beyond its ability to inhibit cell division in mutant models, BAY61-3606 demonstrated a unique biological characteristic in wild-type cells: it bestowed susceptibility to RAF inhibition. In this instance, BAY61-3606 worked by blocking MAP4K2 (GCK), which in wild-type cells typically triggers NFκβ signaling in reaction to RAF inhibition.
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| Cell Assay |
After a 24-hour period, MCF-7 cells are exposed to TRAIL (specified concentrations: 0, 12.5, 25, and 37.5 ng/ml) with or without Bay 61-3606 (2.5 μM). Following this exposure, the cells undergo immunocytochemistry using an active Bak antibody. MCF-7 cells exposed to Bay 61-3606 (5 μM) with or without TRAIL (50 ng/ml) for a 24-hour period are tested for caspase activity.
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| Animal Protocol |
Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograft
50 mg/kg TRAIL (10 mg/kg), Bay 61-3606 (50 mg/kg), or a combination of both (50 mg/kg) was intraperitoneally injected twice a week; TRAIL was administered two hours following the injection of Bay 61-3606 for a duration of two weeks. |
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| References |
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| Molecular Formula |
C20H18N6O3.2HCL
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| Molecular Weight |
463.32
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| Exact Mass |
462.0973939
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| CAS # |
648903-57-5
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| Related CAS # |
BAY 61-3606;732983-37-8
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| Appearance |
Solid
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| SMILES |
COC1=C(C=C(C=C1)C2=CC3=NC=CN3C(=N2)NC4=C(C=CC=N4)C(=O)N)OC.Cl.Cl
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| InChi Key |
SPMFEULFGGPQLN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H18N6O3.2ClH/c1-28-15-6-5-12(10-16(15)29-2)14-11-17-22-8-9-26(17)20(24-14)25-19-13(18(21)27)4-3-7-23-19;;/h3-11H,1-2H3,(H2,21,27)(H,23,24,25);2*1H
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| Chemical Name |
2-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]pyridine-3-carboxamide;dihydrochloride
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.71 mg/mL (1.53 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 7.1 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: ≥ 0.71 mg/mL (1.53 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 7.1 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1583 mL | 10.7917 mL | 21.5834 mL | |
| 5 mM | 0.4317 mL | 2.1583 mL | 4.3167 mL | |
| 10 mM | 0.2158 mL | 1.0792 mL | 2.1583 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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