BAY 61-3606 dihydrochlorideSyk tyrosine kinase inhibitor CAS# 648903-57-5 |
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Quality Control & MSDS
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| Cas No. | 648903-57-5 | SDF | Download SDF |
| PubChem ID | 11784504 | Appearance | Powder |
| Formula | C20H20Cl2N6O3 | M.Wt | 463.32 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | BAY 61-3606 | ||
| Solubility | DMSO : 7.14 mg/mL (15.41 mM; Need ultrasonic) | ||
| Chemical Name | 2-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]pyridine-3-carboxamide;dihydrochloride | ||
| SMILES | COC1=C(C=C(C=C1)C2=CC3=NC=CN3C(=N2)NC4=C(C=CC=N4)C(=O)N)OC.Cl.Cl | ||
| Standard InChIKey | SPMFEULFGGPQLN-UHFFFAOYSA-N | ||
| Standard InChI | 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 | ||
| 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. | ||
| Description | BAY 61-3606 (dihydrochloride) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase (IC50=10 nM) with no inhibitory effect on Btk, Fyn, Itk, Lyn, and Src.In Vitro:BAY 61-3606 inhibits the release of various inflammatory mediators in a concentration-dependent manner. The IC50 values for the FcϵRI-mediated hexosaminidase release from a rat basophilic leukemia cell line, RBL-2H3, and serotonin release from rat peritoneal mast cells are found to be 46 and 17 nM, respectively. BAY 61-3606 inhibits FcϵRI-mediated histamine and tryptase release from HCMCs with IC50 values of 5.1 and 5.5 nM, respectively, in a manner similar to its effect on the degranulation of RBL-2H3 cells and rat peritoneal mast cells. BAY 61-3606 inhibits histamine release from leukocytes in high and low IgE groups equipotently, giving IC50 values of 8.1 and 10 nM, respectively[1]. BAY 61-3606 affects viability in cells expressing mutant K-RAS or B-RAF through a MAPK-independent pathway. Inhibition of SYK is not responsible for the BAY 61-3606 effect on cell viability in colorectal cancer cells. MAP4K2 is a target for BAY 61-3606 that modulates the response of wild-type cells to AZ-628[2]. BAY61-3606 has a 50% Cytotoxicity Concentration (CC50) value of greater than 100 μM, and it inhibits AD169 replication[3].In Vivo:BAY 61-3606 (3, 10, 30, 100 mg/kg, p.o.) dose dependently inhibits the PCA reaction with an ED50 value of 8 mg/kg. In a bronchoconstriction model, BAY 61-3606 dose dependently inhibits the DNP-BSA-induced increase in pulmonary pressure, and the dose of 3 mg/kg shows statistically significant suppression[1]. References: | |||||
BAY 61-3606 dihydrochloride Dilution Calculator
BAY 61-3606 dihydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1583 mL | 10.7917 mL | 21.5834 mL | 43.1667 mL | 53.9584 mL |
| 5 mM | 0.4317 mL | 2.1583 mL | 4.3167 mL | 8.6333 mL | 10.7917 mL |
| 10 mM | 0.2158 mL | 1.0792 mL | 2.1583 mL | 4.3167 mL | 5.3958 mL |
| 50 mM | 0.0432 mL | 0.2158 mL | 0.4317 mL | 0.8633 mL | 1.0792 mL |
| 100 mM | 0.0216 mL | 0.1079 mL | 0.2158 mL | 0.4317 mL | 0.5396 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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BAY 61-3606 is Syk Inhibitor IV. BAY 61-3606 (BAY 61-3606) is a cell-permeable imidazopyrimidine compound that acts as a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki 7.5 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src. BAY 61-3606 has been shown to inhibit Syk-mediated cellular functions such as inhibition of high glucose-tyrosine phosphorylation of I kappa B α and p65 nuclear translocation. In mast cells BAY 61-3606 has inhibited cytokine synthesis, lipid mediation and degranulation. In addition, monocyte and eosinophil activation by B cells and Fc receptors were suppressed by BAY 61-3606.
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The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents.[Pubmed:12766258]
J Pharmacol Exp Ther. 2003 Sep;306(3):1174-81.
Spleen tyrosine kinase (Syk) tyrosine kinase plays essential roles in receptors for Fc portion of immunoglobulins and B cell receptor complex signaling in various inflammatory cells; therefore, inhibitors of Syk kinase may show potential as antiasthmatic/allergic therapeutics. We identified 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]-nicotinamide dihydrochloride (BAY 61-3606), a potent (Ki = 7.5 nM) and selective inhibitor of Syk kinase. BAY 61-3606 inhibited not only degranulation (IC50 values between 5 and 46 nM) but also lipid mediator and cytokine synthesis in mast cells. BAY 61-3606 was highly efficacious in basophils obtained from healthy human subjects (IC50 = 10 nM) and seems to be at least as potent in basophils obtained from atopic (high serum IgE) subjects (IC50 = 8.1 nM). B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes were also potently suppressed by BAY 61-3606. Oral administration of BAY 61-3606 to rats significantly suppressed antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuated antigen-induced airway inflammation in rats. Based on these anti-inflammatory effects of BAY 61-3606 both in vitro and in vivo, it was demonstrated that Syk may play a very critical role in the pathogenesis of allergic reactions.
