Molecular Formula | C20H20Cl2N6O3 |
Molar Mass | 463.3172 |
Solubility | DMSO: ≥ 4.6 mg/mL |
Appearance | Yellow solid. |
Storage Condition | -20℃ |
In vitro study | BAY 61-3606 is a highly specific inhibitor of Syk kinase. At a concentration of 4.7 μm, other tyrosine kinases such as Lyn, Fyn, Src, Itk, and Btk were not inhibited by BAY 61-3606. BAY 61-3606 inhibits B- cell receptor-mediated signaling pathways. Bay 61-3606 is also a sensitizer for TRAIL-induced apoptosis. Bay 61-3606 downregulated Mcl-1 in MCF-7 cells in a dose-and time-dependent manner. In MCF-7 and T47D cells, Bay 61-3606 reduced the phosphorylation of Syk. In breast cancer cells, Bay 61-3606 downregulates Mcl-1 independently of Syk. In MCF-7 cells. Bay 61-3606 promotes the degradation of ubiquitin/proteasome-dependent Mcl-1 protein and inhibits the phosphorylation of CDK9, the expression of RNA polymerase Ⅱ and Mcl-1. In Vitro, Bay 61-3606 inhibited CDK9 kinase activity with an IC50 value of 37 nM. |
In vivo study | Bay 61-3606 was administered in combination with TRAIL, and the volume of transplanted tumors was significantly reduced after 20 days. Oral administration of BAY 61-3606(3 mg/kg) to rats significantly transplanted antigen-induced passive cutaneous anaphylaxis, bronchial stenosis, and bronchial edema. In addition, BAY 61-3606 attenuates antigen-induced airway inflammation in rats. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.158 ml | 10.792 ml | 21.583 ml |
5 mM | 0.432 ml | 2.158 ml | 4.317 ml |
10 mM | 0.216 ml | 1.079 ml | 2.158 ml |
5 mM | 0.043 ml | 0.216 ml | 0.432 ml |
biological activity | BAY-61-3606 is a potent and selective Syk kinase inhibitor, ki was 7.5 nM. BAY-61-3606 can induce cell cycle arrest and apoptosis. |
Target | Value |
Syk (Cell-free assay) | 7.5 nM(Ki) |