2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺
![2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺 结构式](https://img.chemicalbook.com/CAS/GIF/732983-37-8.gif)
2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺 用途与合成方法
Ki: 7.5 nM (Syk)
IC50: 10 nM (Syk)
BAY 61-3606 (0.01-10 μM ; 48 hours) significantly reduces the cell viability of SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells in a dose-dependent matter. SH-SY5Y cells expressing high SYK levels are significantly more sensitive to BAY 61-3606 in comparison to SK-N-BEcells expressing very low or no SYK.
BAY 61-3606 (0.4 and 0.8 μM; 4 or 24 hours) inhibits SYK activity by reducing ERK1/2 and Akt phosphorylation in neuroblastoma cell SH-SY5Y.
BAY 61-3606 (2 μM; 2 hours) induces a large decrease of Syk phosphorylation in K-rn cell lysates.
Cell Viability Assay
| Cell Line: | SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells |
| Concentration: | 0.01, 0.1, 1, and 10 μM |
| Incubation Time: | 48 hours |
| Result: | Significantly reduced the cell viability of both cell lines in a dose-dependent matter. |
Western Blot Analysis
| Cell Line: | SH-SY5Y cells |
| Concentration: | 0.4 and 0.8 μM |
| Incubation Time: | 4 or 24 hours |
| Result: | Reduced the phosphorylation of ERK1/2 and Akt after a 4 or 24 h treatment. |
Western Blot Analysis
| Cell Line: | K-rn cell lysates |
| Concentration: | 2 μM |
| Incubation Time: | 2 hours |
| Result: | Induced a large decrease of Syk phosphorylation. |
Bay 61-3606 (50 mg/kg; administered twice a week for two weeks by intraperitoneal injection) alone leads to more efficacious reductions than that of TNF-related apoptosis-inducing ligand (TRAIL; 10 mg/kg) alone in MCF-7 tumor xenograft-bearing BALB/c nude mice. Bay 61-3606 administered in TRAIL combination significantly reduces the volume of the xenografted tumor.
| Animal Model: | Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograft |
| Dosage: | 50 mg/kg |
| Administration: | Injected intraperitoneally twice a week with Bay 61-3606 (50 mg/kg), TRAIL (10 mg/kg) or a combination of Bay 61-3606 (50 mg/kg) and TRAIL (10 mg/kg); TRAIL was given 2 h after the injection of Bay 61-3606; for two weeks |
| Result: | Led to efficacious reductions in tumor growth. |
