5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile
5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile Basic information
- Product Name:
- 5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile
- Synonyms:
-
- 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:
- 2120398-39-0
- MF:
- C18H18FN7O2
- MW:
- 383.38
- Mol File:
- 2120398-39-0.mol
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5-((5-(2-(3-aminopropoxy)-4-fluoro-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile Chemical Properties
- storage temp.
- 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 Usage And Synthesis
Uses
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model[1].
in vivo
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[1].
Chk1-IN-5 (10 mg/kg; via tail vein intravenous injection) displays a longer half-life (T1/2=3.8 hours) and higher exposure (CL=2.3 L/hr?kg; Vss=6.4 L/kg; AUC=4531 ng/ml?h)[1].
| Animal Model: | Baib/c nude mice with HT-29 colon cancer cells[1] |
| Dosage: | 40 mg/kg |
| Administration: | IV; twice a week for 21 days |
| Result: | Inhibited tumor growth. |
| Animal Model: | Male SD rats (280-350 g)[1] |
| Dosage: | 10 mg/kg |
| Administration: | Via tail vein intravenous injection |
| Result: | Displayed a longer half-life (T1/2=3.8 hours) and higher exposure (CL=2.3 L/hr?kg; Vss=6.4 L/kg; AUC=4531 ng/ml?h). |
IC 50
Chk1
References
[1] Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1.
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