2120398-39-0
中文名稱
5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile
英文名稱
5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile
CAS
2120398-39-0
分子式
C18H18FN7O2
分子量
383.38
MOL 文件
2120398-39-0.mol
2120398-39-0 結(jié)構(gòu)式
基本信息
中文別名
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 英文別名
Chk1-IN-55-((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]-
常見問題列表
生物活性
Chk1-IN-5 是有效的檢查點(diǎn)激酶 1 (Chk1) 抑制劑。Chk1-IN-5 抑制 Chk1 磷酸化，并在結(jié)腸癌異種移植模型中抑制腫瘤生長。靶點(diǎn)
|
Chk1
|
體外研究
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.
體內(nèi)研究
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). |