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
| 中文名称 | 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 |
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| 中文同义词 | 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;BAY 61-3606游离;BAY 61-3606 游离碱 |
| 英文名称 | BAY 61-3606 |
| 英文同义词 | Syk Inhibitor IV, BAY 61-3606: sc-202351 hydrochloride;Syk Inhibitor IV, BAY 61-3606 HCl;BAY 61-3606;BAY 61-3606 hydrate hydrochloride;2-[[7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-3-pyridinecarboxamide;BAY-61-360;Syk Inhibitor IV, BAY 61-3606;BAY 61-3606 free base |
| CAS号 | 732983-37-8 |
| 分子式 | C20H18N6O3 |
| 分子量 | 390.4 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 732983-37-8.mol |
| 结构式 | ![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](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 性质
| 密度 | 1.41 |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 可溶于水中 |
| 形态 | 固体 |
| 颜色 | 粘黄色 |
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. |
安全信息
| WGK Germany | 3 |
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