中文名 | BAY 61-3606 |
英文名 | BAY 61-3606 |
别名 | BAY 61-3606游离 BAY 61-3606 游离碱 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 |
英文别名 | CS-2745 BAY-61-360 BAY 61-3606 BAY 61-3606 free base Syk Inhibitor IV, BAY 61-3606 HCl BAY 61-3606 hydrate hydrochloride 2-[[7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-3-pyridinecarboxamide |
CAS | 732983-37-8 |
化学式 | C20H18N6O3 |
分子量 | 390.4 |
密度 | 1.41 |
溶解度 | H2O: 可溶 |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | yellow |
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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.562 ml | 12.808 ml | 25.615 ml |
5 mM | 0.512 ml | 2.562 ml | 5.123 ml |
10 mM | 0.256 ml | 1.281 ml | 2.562 ml |
5 mM | 0.051 ml | 0.256 ml | 0.512 ml |
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