In vitro: BAY 61-3606 is a highly selective inhibitor of Syk kinase. Other selected tyrosine kinases, Lyn, Fyn, Src, Itk, and Btk, are not inhibited by BAY 61-3606 in concentrations up to 4.7 μM. BAY 61-3606 is also found to inhibit B cell receptor (BCR)-mediated signaling. Bay 61-3606 is a sensitizer of TRAIL-induced apoptosis. Mcl-1 downregulation by Bay 61-3606 are concentration- and time-dependent in MCF-7 cells. phosphorylation of Syk is reduced by Bay 61-3606 in MCF-7 and T47D cells. Downregulation of Mcl-1 by Bay 61-3606 is independent of Syk in breast cancer cells. Bay 61-3606 promotes the ubiquitin/proteasome-dependent degradation of the Mcl-1 protein in MCF-7 cells. Bay 61-3606 inhibits the phosphorylation of CDK9, RNA polymerase II, and Mcl-1 expression in MCF-7 cells. Bay 61-3606 inhibits CDK9 kinase activity with an in vitro IC50 of 37 nM. In vivo: After 20 days of drug administration, the volume of the xenografted tumor was significantly (P <0.001) reduced the efficacy of Bay 61–3606 when administered in TRAIL combination. Oral administration of BAY 61-3606 to rats significantly suppresses antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuates antigen-induced airway inflammation in rats.
|Cell lines||MCF-7 cells|
|Preparation method||MCF-7 cells are exposed to TRAIL (indicated concentrations:0, 12.5, 25, 37.5 ng/ml) with or without Bay 61-3606 (2.5 μM) for 24 h; After exposure to the agents for 12 h, MCF-7 cells are subjected to immunocytochemistry using an active Bak antibody; Caspase activity is measured in MCF-7 cells exposed to Bay 61-3606 (5 μM) with or without TRAIL (50 ng/ml) for 24 h.|
|Concentrations||2.5 μM or 5 μM|
|Incubation time||12 h or 24 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||92 mg/mL in DMSO|
Effect of Narrow Spectrum Versus Selective Kinase Inhibitors on the Intestinal Proinflammatory Immune Response in Ulcerative Colitis.
Biancheri P, et al. Inflamm Bowel Dis. 2016 Jun;22(6):1306-15. PMID: 27104822.
Bay 61-3606 Sensitizes TRAIL-Induced Apoptosis by Downregulating Mcl-1 in Breast Cancer Cells.
Kim SY, et al. PLoS One. 2015 Dec 31;10(12):e0146073. PMID: 26720004.
BAY 61-3606, CDKi, and sodium butyrate treatments alter gene expression in human vestibular schwannomas and cause cell death in vitro.
Mitra R, et al. Ecancermedicalscience. 2012;6:285. PMID: 23304241.
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