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,732983-37-8,结构式](https://www.chemicalbook.com/CAS/GIF/732983-37-8.gif)
- CAS号:732983-37-8
- 英文名:BAY 61-3606
- 中文名: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
- CBNumber:CB1497948
- 分子式:C20H18N6O3
- 分子量:390.4
- MOL File:732983-37-8.mol
- 密度 :1.41
- 储存条件 :2-8°C
- 溶解度 :H2O: soluble
- 形态 :solid
- 颜色 :yellow
- WGK Germany :3
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、用途与生产工艺
- 生物活性 BAY 61-3606 是一种有效的，具有口服活性的，ATP 竞争性的，可逆的选择性 Syk 抑制剂，Ki 为 7.5 nM，IC50 为 10 nM。BAY 61-3606 降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化。BAY 61-3606 降低 K-rn 细胞裂解物中 Syk 磷酸化。Bay 61-3606 作用于乳腺癌细胞，通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。
-
靶点
Ki: 7.5 nM (Syk)
IC50: 10 nM (Syk) -
体外研究
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. -
体内研究
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.
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