网站主页 >> CAS数据库列表 >> 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
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- CAS号:
- 732983-37-8
- 英文名:
- BAY 61-3606
- 英文别名:
- CS-2745;BAY-61-360;BAY 61-3606;SYK INHIBITOR IV;BAY 61-3606 free base;Syk Inhibitor IV, BAY 61-3606;Syk Inhibitor IV, BAY 61-3606 HCl;BAY 61-3606 hydrate hydrochloride;Syk Inhibitor IV,
BAY 61-3606: sc-202351
hydrochloride;2-[[7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-3-pyridinecarboxamide
- 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
- 中文别名:
- 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
- CBNumber:
- CB1497948
- 分子式:
- C20H18N6O3
- 分子量:
- 390.4
- MOL File:
- 732983-37-8.mol
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2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺化学性质
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密度:
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1.41
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储存条件:
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2-8°C
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溶解度:
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H2O: soluble
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形态:
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solid
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颜色:
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yellow
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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
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。
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
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Cell Line:
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SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells
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Concentration:
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0.01, 0.1, 1, and 10 μM
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Incubation Time:
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48 hours
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Result:
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Significantly reduced the cell viability of both cell lines in a dose-dependent matter.
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Western Blot Analysis
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Cell Line:
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SH-SY5Y cells
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Concentration:
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0.4 and 0.8 μM
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Incubation Time:
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4 or 24 hours
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Result:
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Reduced the phosphorylation of ERK1/2 and Akt after a 4 or 24 h treatment.
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Western Blot Analysis
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Cell Line:
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K-rn cell lysates
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Concentration:
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2 μM
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Incubation Time:
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2 hours
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Result:
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Induced a large decrease of Syk phosphorylation.
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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.
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Animal Model:
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Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograft
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Dosage:
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50 mg/kg
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Administration:
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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
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Result:
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Led to efficacious reductions in tumor growth.
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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
上下游产品信息
上游原料
下游产品
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
生产厂家
732983-37-8, 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 相关搜索:
- 抑制剂
- BAY 61-3606 游离碱
- BAY 61-3606游离
- 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
- Spleen tyrosine kinase,Syk,inhibit,BAY 61 3606,Apoptosis,Inhibitor,BAY 613606,BAY 61-3606
- 3-Pyridinecarboxamide, 2-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-
- SYK INHIBITOR IV
- CS-2745
- BAY 61-3606 free base
- Syk Inhibitor IV, BAY 61-3606
- BAY-61-360
- 2-[[7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-3-pyridinecarboxamide
- BAY 61-3606 hydrate hydrochloride
- BAY 61-3606
- Syk Inhibitor IV, BAY 61-3606 HCl
- Syk Inhibitor IV,
BAY 61-3606: sc-202351
hydrochloride