5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile
| 中文名称 | 5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile |
|---|---|
| 中文同义词 | 5-((5-(2-(3-氨基丙氧基)-4-氟-6-甲氧基苯基)-1H-吡唑-3-基)氨基)吡嗪-2-甲腈 |
| 英文名称 | 5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile |
| 英文同义词 | 5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile;2-Pyrazinecarbonitrile, 5-[[5-[2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-;Chk1-IN-5;Chk-1-IN-5,Chk1IN5,Chk1 IN 5 |
| CAS号 | 2120398-39-0 |
| 分子式 | C18H18FN7O2 |
| 分子量 | 383.38 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2120398-39-0.mol |
| 结构式 |  |
5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile 性质
| 储存条件 | Store at -20°C |
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5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile 用途与合成方法
Chk1-IN-5 是有效的检查点激酶 1 (Chk1) 抑制剂。Chk1-IN-5 抑制 Chk1 磷酸化，并在结肠癌异种移植模型中抑制肿瘤生长。
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Chk1
|
Chk1-IN-5 (compound 3; 0.4, 1.2, 3.7, 11.1, 33.3, 100 nM) inhibits Chk1 phosphorylation in the HT-29 colon cells.
Chk1-IN-5 (compound 3; 40 mg/kg; IV; twice a week for 21 days) inhibits tumor growth in Baib/c nude mice with HT-29 colon cancer cells.
Chk1-IN-5 (10 mg/kg; via tail vein intravenous injection) displays a longer half-life (T
1/2
=3.8 hours) and higher exposure (CL=2.3 L/hr•kg; V
ss
=6.4 L/kg; AUC=4531 ng/ml•h).
| Animal Model: | Baib/c nude mice with HT-29 colon cancer cells |
| Dosage: | 40 mg/kg |
| Administration: | IV; twice a week for 21 days |
| Result: | Inhibited tumor growth. |
| Animal Model: | Male SD rats (280-350 g) |
| Dosage: | 10 mg/kg |
| Administration: | Via tail vein intravenous injection |
| Result: | Displayed a longer half-life (T 1/2 =3.8 hours) and higher exposure (CL=2.3 L/hr•kg; V ss =6.4 L/kg; AUC=4531 ng/ml•h). |